Pubmed abstracts for Protein-Protein Interaction search result :


Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.51576836
Although previous studies have concluded that the indole ring of Trp 30 is a critical pharmacophore for the interaction of CCK with both its A and B type receptors , we find 2 Nal 30 Ac CCK 7 ( 20 ) to be nearly equipotent to 2 in both CCK binding and as an anorectic agent sensitive to blockade by the Merck CCK A receptor antagonist MK 329 . 0.51576836^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.94201892
Further to these , ( 1S trans ) N [ alpha methyl N [ [ ( 2 methylcyclohexyl ) oxy ] carbonyl ] D tryptophyl ] L 3 ( phenylmethyl ) beta alanine ( 28h ) is a mixed CCK A / CCK B ligand with a CCK A binding affinity of IC 50 = 3 . 9 nM and a CCK B binding affinity of IC 50 = 4 . 2 , producing a CCK A / CCK B ratio of unity . 0.94201892^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.51863502
We conclude that CCK interacts with neural CCK A receptors to cause esophageal muscle contraction . 0.51863502^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK interacts with at least two types of receptor called CCK A and CCK B receptors . ^^^ Moreover , selective nonpeptide antagonists have been developed for CCK A and CCK B receptors . ^^^ CCK A receptors occur predominantly at the peripheral level where they are responsible for the digestive effects of CCK : intestinal and biliary smooth muscle contraction , pancreatic enzyme secretion , trophic effects on gastric and intestinal mucosa and regulation of feeding . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK receptors can be subdivided into at least two subtypes , CCKA and CCKB on the basis of pharmacological studies . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Similarly , i . c . v . administration of CCK8s ( 0 . 1 microgram / kg ) abolished both ES and CRH stimulated colonic motility , an effect reproduced by central injection of JMV 180 , a cholecystokinin ( CCK ) derivative with high affinity for CCKA receptors , ( 1 microgram / kg ) , but not by JMV 170 , a CCK derivative with low affinity for CCKA receptor at similar or higher dose . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pharmacological experiments using selective CCK A and CCK B receptor antagonists demonstrate that CCK B is the prominent CCK receptor subtype in trigeminal and dorsal root ganglia neurons in the rat , rabbit , and monkey . ^^^ In the rat and rabbit spinal cord , CCK B binding sites are the prominent subtype , whereas in the monkey cord , CCK A is the prominent receptor subtype . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Behavioural studies performed after local injection of CCK 8 or BC 264 into the postero median part of the nucleus accumbens have shown the involvement of CCK A receptors in motivation and / or emotional states of rats . ^^^ These results suggest that endogenous CCK could play a critical role in mood modulation through CCK A / CCK B receptor stimulation . ^^^ Dysfunctioning of the CCK A / CCK B pathways could be implicated in anxiety and panic attacks . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Compounds were assessed in binding assays using homogenated rat pancreatic membranes and bovine striatum as the source of CCK A and CCK B receptors respectively and for anorectic activity after intraperitoneal administration to rats . ^^^ The anorectic activity of 21 was blocked by the specific CCK A receptor antagonist MK 329 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In Experiment 3 , the responsibility of endogenous cholecystokinin ( CCK ) for the difference in food intake between the two diets was investigated for 6 h by using a CCK A receptor antagonist , Devazepide ( DVZ , 1 mg / kg b . wt . ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Provided that devazepide acts solely by inhibiting CCK A receptors , we can conclude that endogenous CCK plays an important role in both normal and stimulated growth of the rat pancreas . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Both CCK A and CCK B / gastrin receptors are present on rabbit vagus nerve . ^^^ Autoradiographic studies in rats have demonstrated the presence of CCK A type receptors on vagus nerves . ^^^ A 71378 , a selective CCK A agonist , showed biphasic displacement curves , with the high affinity portion ( less than 10 nM ) accounting for approximately 60 % and the low affinity portion for approximately 40 % . ^^^ Under conditions which selectively examined vagal CCK A or CCK B / gastrin receptors , we demonstrated that a number of CCK subtype selective agonists and antagonists possessed similar affinities for the vagal CCK A and B / gastrin receptors as those found on the guinea pig pancreas ( CCK A ) and cerebral cortex ( CCK B ) , respectively . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To examine the hormonal mediators , the effects of a somatostatin monoclonal antibody and a CCK A receptor antagonist ( L 364718 ) on acid induced inhibition of gastric acid secretion were studied in transplanted rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We evaluated the effects of a potent cholecystokinin ( CCK ) B / gastrin receptor antagonist , L 365 , 260 ( 3R ( + ) N ( 2 , 3 dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepin 3 yl ) N ' ( 3 methylphenyl ) urea ) ; a selective CCK A receptor antagonist , devazepide ( L 364 , 718 ) ; and cimetidine on gastric acid secretion induced by pentagastrin , histamine and bethanechol in anesthetized rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These data support the existence of a CCK receptor , located on raphe neurones in the rat , with a pharmacological profile very similar to that described for the CCKA type . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Incubation of nerve sections in the presence of both antagonists produced an additive effect , indicating that both CCK A and CCK B binding sites are transported towards the periphery . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the present study , we tested whether this action is mediated by CCK A receptors , CCK B receptors , or both . ^^^ Intraventricular administration of the selective CCK A receptor agonist A 71623 at 1 and 10 nmol / kg suppressed 30 min meal size 69 + / 22 % and 75 + / 7 % , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pharmacological responses to CCK are mediated through at least two receptor subtypes termed CCK A and CCK B . ^^^ Using selective antagonists and a behavioural recognition test based on the olfactory discriminative capacities of rats , we found that endogenous CCK acting at CCK A and CCK B receptors modulates olfactory recognition positively and negatively , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist , devazepide , blocks the anorectic action of CCK but not peripheral serotonin in rats . ^^^ We examined the effect of pretreatment with the CCK A antagonist devazepide ( DVZ ) on anorexia produced by peripheral administration of serotonin [ 5 hydroxytryptamine ( 5 HT ) ] or CCK 8 in 3 h food deprived rats consuming a 30 min test meal of sweetened mash . ^^^ These data confirm established findings that the anorectic action of peripheral CCK depends upon CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Devazepide antagonizes the inhibitory effect of cholecystokinin on intake in sham feeding rats . 3S ( ) N ( 2 , 3 Dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepine 3 yl ) 1H indole 2 carboxamide ( devazepide ) , a potent and selective cholecystokininA ( CCKA ) antagonist , has been shown to reverse the inhibitory effect of exogenously administered CCK 8 on food intake . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Analysis of the ability of gastrin 17 1 to inhibit 125I gastrin 1 binding demonstrated that gastrin bound to a single class of receptors with a Kd of 0 . 21 + / 0 . 04 nM and a binding capacity of 184 + / 29 fmol / mg protein . 125I Gastrin 1 binding was inhibited by the specific CCK B receptor antagonist L 365 , 260 approximately 40 times more effectively than by the specific CCK A receptor antagonist L 364 , 718 . ^^^ The three sites meet the criteria for CCK B , high affinity CCK A , and low affinity CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Tetronothiodin inhibited [ 125I ] CCK 8 binding to rat brain CCKB receptors with an IC 50 of 3 . 6 nM , whereas it showed only weak affinity for rat CCKA receptors ( IC 50 = 70 microM ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effect of caerulein ( 5 micrograms / kg ) was antagonized by devazepide , a CCK A antagonist , at 100 micrograms / kg , but not by a CCK B antagonist L 365 , 260 tested at a wide dose range . ^^^ The results probably indicate that CCK A receptor stimulation inhibits TSH secretion at the level of the anterior pituitary gland . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
L 364 , 718 , a selective antagonist of CCK A receptors , caused further increase in gastric HCl and plasma gastrin responses to duodenal peptone but reduced the pancreatic protein outputs in these tests by about 75 % . ^^^ We conclude that CCK released by intestinal peptone meal , containing fat or acid , exerts a tonic inhibitory influence on gastric acid secretion and gastrin release through the CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A series of modifications of the CCK 7 analogue ( des NH 2 ) Tyr ( SO 3 ) Nle Gly Trp Nle Asp Phe NH 2 was prepared and tested for binding to guinea pig CCK A and CCK B receptors and in CCK A mediated functional assays . ^^^ The ( N Me ) Asp 32 and ( N Me ) Leu 31 modifications afforded potent and selective CCK A and CCK B ligands , respectively . ^^^ All of the analogues that showed high affinity ( less than 10 nM ) for the CCK A receptor also were full agonists in amylase release and most were full or nearly full agonists in the phosphoinositide ( PI ) turnover assay , the most notable exception being the delta Z Phe 33 analogue , which showed 69 % of the maximal response in the PI assay . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A 71623 , a selective CCK A receptor agonist , suppresses food intake in the mouse , dog , and monkey . ^^^ The anorectic actions of cholecystokinin ( CCK ) 8 and of a selective CCK A agonist , A 71623 , were examined in CD 1 mice , beagle dogs , and cynomolgus monkeys . ^^^ A 71623 suppressed intakes in all species tested , and the effects were blocked by a selective CCK A antagonist , A 70104 . ^^^ Our results support other evidence suggesting that the anorectic actions of exogenous application of CCK 8 in these species are mediated via stimulation of the CCK A receptor subtype . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Subtype selective antagonists of the peripheral type ( CCK A ) and the central type ( CCK B ) cholecystokinin ( CCK ) receptors were employed to determine the receptor subtype ( s ) mediating the modulatory actions of CCK on dopamine induced changes in exploratory activity at three sites in the mesolimbic pathway of the rat . ^^^ The CCK A antagonist L 364 , 718 ( 10 ng ) blocked CCK potentiation of dopamine induced hyperlocomotion in the medial posterior nucleus accumbens . ^^^ These data indicate a CCK B pharmacology in the cell body and anterior terminal field , and a CCK A pharmacology in the posterior terminal field , of the mesolimbic dopamine pathway . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The amino acid sequence deduced from the cloned cDNA showed 85 . 7 % and 49 . 0 % identity to canine parietal cell gastrin receptor and rat pancreatic CCK A receptor , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This effect was suppressed by the selective CCK B antagonist : L 365 , 260 , but not by the selective CCK A antagonist : MK 329 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK 8 stimulated insulin secretion in vivo is mediated by CCKA receptors . ^^^ The effects of the cholecystokinin A ( CCKA ) receptor antagonist , L 364 , 718 , and the CCKB receptor antagonist , L 365 , 260 , on CCK 8 stimulated insulin secretion were studied in vivo in the mouse . ^^^ It is concluded that the CCK 8 stimulated insulin release in vivo is mediated by CCK receptors of the CCKA subtype . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present study used the substance loxiglumide , which acts as a specific antagonist at the CCK A receptor , to evaluate this hypothesis . ^^^ Therefore , effects mediated by the CCK A receptor do not play a major physiological role in the regulation of the interdigestive and postprandial motility of the left colon . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The brainstem solitary complex , which receives projections from primary sensory afferents of the vagus nerve , appears to be a crucial site for the action of the cholecystokinin octapeptide ( CCK 8 ) , because both peripheral type ( CCKA ) and central type ( CCKB ) binding sites are present in this structure . ^^^ L 364 , 718 , a potent antagonist of CCKA receptors , blocked delayed inhibition and replaced brief CCK 8 induced excitation by prolonged excitation . ^^^ Altogether , these results show that CCK 8 exerts , on neurons of the solitary complex , mixed effects due to simultaneous activation of CCKA inhibitory and CCKB excitatory binding sites . ^^^ The hypothesis that exogenous CCK 8 acts , in the solitary complex , through CCKA sites to slow down the motility of the digestive tract and through CCKB sites to modulate anxiety will be developed . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A and CCK B receptor antagonists , devazepide and L 365 , 260 , enhance morphine antinociception only in non acclimated rats exposed to a novel environment . ^^^ Devazepide , a potent CCK A receptor antagonist , and L 365 , 260 , a selective CCK B receptor antagonist , have been introduced as pharmacologic tools for differentiating the physiologic roles of CCK A and CCK B receptor subtypes . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Satiety induced by endogenous and exogenous cholecystokinin is mediated by CCK A receptors in mice . ^^^ To investigate the relative participation of peripheral ( CCK A ) and central ( CCK B ) cholecystokinin ( CCK ) receptors in satiety induced by endogenous CCK , we examined the effect of the CCK A antagonist MK 329 ( 10 315 micrograms / kg ) and the CCK B antagonist L 365260 ( 0 . 1 315 micrograms / kg ) on intake of a 20 % sucrose solution in mildly food deprived mice . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To further explore the role of CCK in humans , the effect on satiety and eating behavior of a specific CCK receptor antagonist , loxiglumide , that preferentially inhibits peripheral ( CCK A ) receptors was investigated . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Thus , devazepide , a selective CCK A receptor antagonist , produced a dose related inhibition of the CCK 8 stimulated rise in circulating beta endorphin concentrations . ^^^ Less selective CCK A antagonists , including proglumide and lorglumide , produced little or no effect , however . ^^^ Unexpectedly , the CCK B receptor antagonist , L 365 , 260 , enhanced the response to CCK 8 , an effect diametrically opposite to that produced by CCK A antagonists . ^^^ These observations indicate that CCK A and CCK B receptors mediate quite different , if not opposing , roles in regulating corticotroph secretion . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Stimulation of peripheral and central CCK A receptors by the selective CCK A receptor agonist A 71623 suppressed intakes of a liquid diet in both deprived and sated rats . ^^^ Although these results stress the relative importance of the CCK A receptor in the effects of exogenous CCK 8 administration on feeding , stimulation of the CCK B receptor may still be involved in the control of feeding following the endogenous release of CCK . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The ability of the CCKA receptor antagonists , lorglumide and loxiglumide , to inhibit CCK 8s induced contraction was also examined . ^^^ These results indicate that the primate iridial sphincter muscle exhibits a high sensitivity to CCK , and that CCKA receptor antagonists effectively block the CCK induced contraction . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
H ] pBC 264 , a suitable probe for studying cholecystokinin B receptors : binding characteristics in rodent brains and comparison with [ 3H ] SNF 8702 . [ 3H ] Propionyl Tyr ( SO3H ) gNle mGly Trp ( NMe ) Nle Asp Phe NH 2 ( [ 3H ] pBC 264 ) ( 98 100 Ci / mmol ) , a new peptidase resistant cholecystokinin ( CCK ) agonist that is 1000 fold more potent for CCK B than for CCK A receptors , interacts , with a similar subnanomolar affinity , with a single class of binding sites ( Kd , 0 . 15 0 . 2 nM ) in brain membranes of mouse , rat , guinea pig , and cat , in Tris and Krebs buffers . ^^^ The concentration of CCK A receptors in rodent brain was estimated to be 8 10 fmol / mg of protein , by measurement of the Bmax values of the nonselective agonist [ 3H ] propionyl CCK 8 , with or without 10 nM pBC 264 to saturate CCK B sites . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Both CCK A and CCK B / gastrin receptors mediate pepsinogen release in guinea pig gastric glands . ^^^ In contrast , the potency of peptides in stimulating PI hydrolysis in both gastric glands and dispersed chief cells displayed a profile similar to CCK A receptors found in pancreatic acini , i . e . , CCK 8 = A 71378 greater than A 71623 greater than A 70874 much greater than A 72962 = CCK 8 ( desulfated ) greater than gastrin 2 greater than gastrin 1 . ^^^ The inhibitory potency of MK 329 , a selective CCK A receptor antagonist , was similar against either CCK 8 ( 10 nM ) or gastrin 1 ( 10 microM ) , except that a minor portion ( approximately 30 40 % ) of gastrin 1 induced pepsinogen release was insensitive to MK 329 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Subcutaneously administered selective CCK A receptor antagonist , L 364 , 718 ( 1 mg / kg ) , reversed the inhibitory effect of centrally as well as peripherally administered CCK 8 , but the selective CCK B receptor antagonist , L 365 , 260 ( 1 mg / kg ) , did not . ^^^ These results demonstrate that centrally as well as peripherally administered CCK 8 suppresses locomotor activity in mice through an interaction with CCK A , but not CCK B , receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Although it has been demonstrated that the receptors which mediate this action are located in the periphery and are of the CCK A subtype , their anatomical location has not been firmly established . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK B and CCK A binding affinities of these analogues are described and their CCK B affinity and selectivity rationalized by consideration of the pK ( a ) values , charge distribution , and geometry of the respective acid mimics . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The specific CCK A receptor antagonist , MK 329 ( formerly L 364 , 718 ; 1 . 0 nM ) , reversibly blocked the facilitatory effect of CCK 8 on ganglionic transmission . ^^^ These results show that CCK has a presynaptic facilitatory effect on fast synaptic transmission in guinea pig gall bladder ganglia , and that this effect is mediated by presynaptic CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCKA receptor antagonism inhibits mechanisms underlying CCK 8 stimulated insulin release in isolated rat islets . ^^^ It is concluded that insulin secretion , phosphoinositide hydrolysis , Ca2+ and K+ movements stimulated by CCK 8 in isolated islets are all events mediated by CCKA receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The neuroprotective effects of CCK were antagonized by L 365260 , a CCKB receptor antagonist , but not by L 364718 , a CCKA receptor antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK 8 , CCK 4 and gastrin induced contractions in guinea pig ileum : evidence for differential release of acetylcholine and substance P by CCK A and CCK B receptors . ^^^ The cholecystokinin ( CCK ) receptor involved in contraction of guinea pig ileal longitudinal muscle to cholecystokinin is poorly understood ; some studies have suggested that contraction was mediated via a CCK A receptor whereas other studies have implicated CCK B receptors in ileal contraction to CCK . ^^^ Two selective CCK A and CCK B receptor antagonists , L 364 , 718 and L 365 , 260 , respectively , were used to probe further the receptors involved in ileal contraction to this peptide family . ^^^ The CCK A selective antagonist , L 364 , 718 , potently inhibited ileal contractions to CCK 8S ( log KB = 9 . 35 ) with 10 fold lower affinity at receptors mediating contraction to CCK 4 ( log KB = 8 . 25 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptors mediate the effect of cholecystokinin on vasopressin but not on cortisol in pigs . ^^^ To determine whether these endocrine responses involve CCK A or CCK B receptors , this experiment investigated the effect of CCK ( 1 microgram / kg ) in pigs ( n = 7 ) pretreated with the CCK A antagonist L 364718 ( 70 microgram / kg ) or the CCK B antagonist L 365260 ( 10 ng / kg and 10 micrograms / kg ) . ^^^ Thus peripherally administered CCK induces vasopressin release by CCK A receptor activation , in agreement with its inhibitory effect on food intake in this species . ^^^ However , the effect of CCK on cortisol secretion does not appear to involve either CCK A or CCK B receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In contrast , in the mouse CCK JMV 180 potently suppressed intakes on its own , and this effect was blocked by pretreatment with the selective CCK A receptor antagonist , A 70104 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Based on their relative affinities for cholecystokinin octapeptide ( 26 33 ) ( CCK 8 ) , cholecystokinin tetrapeptide ( 30 33 ) ( CCK 4 ) , desulfated CCK 8 , and gastrin , cholecystokinin ( CCK ) receptors have been classified as CCK A ( alimentary ) and CCK B ( brain ) . ^^^ Selective nonpeptide antagonists of CCK A and CCK B receptors , as well as highly selective CCK A and CCK B peptide agonists , have been described . ^^^ In radioligand binding assays , the IC 50 values for A 71623 and A 70874 were 3 . 7 and 4 . 9 nM in guinea pig pancreas ( CCK A ) and 4500 and 710 nM in cerebral cortex ( CCK B ) , respectively . ^^^ Both were agonists in stimulating pancreatic amylase release , and their stimulatory effects were potently inhibited by the CCK A antagonist L 364 , 718 . ^^^ Both peptides also were potent agonists in stimulating CCK A receptors in the ileum . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
G 17I induced amylase secretion was unaffected by 100 nM of the selective peripheral CCK A receptor antagonist L 364 , 718 , suggesting that amylase hypersecretion followed non selective CCK receptor activation , a function normally assumed by selective CCK A receptors in rat pancreatic acini . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To study the interdependence between gastric histamine release and acid secretion , we examined the effects of gastrin ( 1 17 ) [ G ( 1 17 ) ] or cholecystokinin ( 1 33 ) [ CCK ( 1 33 ) ] alone or combined with the gastrin ( CCK B ) antagonist L 365 , 260 or the CCK A antagonist L 364 , 718 in the isolated vascularly perfused rat stomach . ^^^ Gastrin or CCK A antagonist alone did not stimulate histamine release or acid secretion . ^^^ Maximally G ( 1 17 ) or CCK ( 1 33 ) stimulated histamine release and acid secretion was unchanged by the CCK A antagonist , while the gastrin antagonist induced a parallel and concentration dependent decrease in stimulated histamine and acid secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
With Asperlicin as a guide , the new , selective , orally bioavailable , high affinity CCK A antagonist , MK 329 ( L 364 , 718 ; Devazepide ) and CCK B / gastrin antagonist , L 365 , 260 have been developed . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
With increasing age , significant changes were found only in CCK a true neural enteral peptide . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The introduction of potent cholecystokinin ( CCK ) receptor antagonists , selective for either the CCK A or the CCK B subtype , has provided a great impetus to the study of activity of endogenous CCK in relation to the control of feeding . ^^^ This paper reviews experiments in which devazepide ( a selective CCK A receptor antagonist ) and L 365 , 260 ( a selective CCK B gastrin receptor antagonist ) have been used . ^^^ Hence , CCK A type receptors appear to be involved in the anorectic effect of these drugs . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
New ( R ) 4 benzamido 5 oxopentanoic acid derivatives were synthesized by a stereoconservative procedure and evaluated in vitro for their capacity to inhibit the binding of [ 125I ] ( BH ) CCK 8 to either rat peripheral ( CCK A ) or central ( CCK B ) CCK receptors , or the binding of [ 3H ] pentagastrin to rabbit gastric glands , as well as to inhibit , in vivo , the acid secretion induced by pentagastrin infusion in the perfused rat stomach . ^^^ The parent compound of this series ( lorglumide ) is the first nonpeptidic , potent and selective antagonist of the CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin antagonists : ( R ) tryptophan based hybrid antagonists of high affinity and selectivity for CCK A receptors . ^^^ Efforts to include the weak CCK antagonist benzotript into this construct utilizing a similar approach have resulted in a novel series of benzotript based hybrid antagonists N alpha ( 3 ' quinolylcarbonyl ) ( R ) tryptophan di n pentylamide ( 9 , A 67396 ) , N alpha ( 4 ' , 8 ' dihydroxy 2 ' quinolylcarbonyl ) ( R ) tryptophan di n pentylamide ( 23 , A 70276 ) , and N alpha ( 3 ' quinolylcarbonyl ) ( R ) 5 ' hydroxytryptophan di n pentylamide ( 36 , A 71134 ) which possess respectively binding affinities of 23 , 21 , and 11 nM for the pancreatic CCK A receptor and which inhibit CCK 8 induced amylase secretion . ^^^ Compound 9 possesses a selectivity of greater than 500 fold for the pancreatic CCK A receptor over the CCK B receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that CCK acts at CCK A receptors to produce satiety during the dark period in ad lib feeding rats . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This increase in sensitivity to quinpirole was blocked by pretreatment with the nonselective CCK receptor antagonist proglumide and the preferential CCK A receptor antagonist CR 1409 but not by the preferential CCK B receptor antagonist L 365 , 260 . ^^^ The inactivity of CCK 4 and CCK 8U in these tests and the results with the antagonists suggest that the effects of CCK 8S on MADA neuronal activity are mediated by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It is concluded that CCK 8 released after a meal is responsible for the postprandial increase in colonic motility and that these effects may be mediated through activation of central CCKA receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) receptors are currently divided into at least two subtypes : a CCK A subtype , responsive to the sulfated form of cholecystokinin octapeptide ( CCK 8 ) and selectively antagonized by L 364 , 718 , and a CCK B subtype , which shares equal affinities for gastrin and CCK 8 . ^^^ The antagonist potencies of L 365 , 260 ( CCK B selective ) and L 364 , 718 ( CCK A selective ) against CCK 8 were also determined . ^^^ The high selectivity of the tissue for sulfated CCK 8 suggests that the secretory effect of CCK 8 on guinea pig ileal electrolyte transport is mediated by a CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCK B pharmacological profile , established by use of several agonists and antagonists selective for the CCK receptor types , namely compound L 364 , 718 , the Merck CCK antagonist selective for the peripheral CCK receptor ( CCK A ) , and compound L 365 , 260 , the Merck CCK antagonist selective for the central CCK receptor ( CCK B ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
At the end of 40 min , food was removed and rats were injected subcutaneously ( SC ) with devazepide ( DVZ ; 1 ng / kg 1 mg / kg ) , an antagonist selective for the CCK A receptor , or its vehicle , 0 . 5 % carboxymethylcellulose ( CMC ) . ^^^ Furthermore , the effectiveness of a very low dose of DVZ ( 10 ng / kg ) is strong evidence that the effect of DVZ was specific for CCK A receptors . ^^^ These results confirm and extend previous reports that CCK A receptor blockade increases food intake after an oral preload . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Furthermore , specific CCK receptors have been described , and a distinction drawn between CCK A and CCK B receptors . ^^^ Recently , potent , orally active CCK antagonists , which show a high degree of selectivity for either CCK A or CCK B receptors , have been introduced . ^^^ The present report reviews recent evidence obtained in studies using devazepide ( a selective CCK A receptor antagonist ) and L 365 , 260 ( a selective CCK B / gastrin receptor antagonist ) . ^^^ Only devazepide was effective in blocking the feeding suppressant effect of exogenous CCK , indicating that CCK A type receptors mediate this effect . ^^^ Hence , CCK A type receptors appear to be involved in the anorectic effects of these serotonergic drugs . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selective CCK B receptor antagonists CI 988 ( PD 134308 ) and L 365 , 260 produced anxiolytic like effects , whereas MK 329 , a CCK A receptor antagonist , was respectively less potent by factors of 313 and 200 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selective cholecystokinin ( CCK ) B receptor agonist and antagonist , BC 264 and L 365260 , respectively , and the CCK A receptor antagonist , L 364718 , were used to investigate the possible involvement of different classes of CCK receptors in the control of food intake induced by exogenous CCK octapeptide ( CCK 8 ) in the cat with gastric fistula . ^^^ We conclude that exogenous CCK 8 causes satiety in the cat through activation of peripheral CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Agonists and antagonists selective for the brain type [ cholecystokinin ( CCK ) B ] and the peripheral type ( CCK A ) CCK receptor were used to localize the site ( s ) of action at which CCK inhibits food consumption . ^^^ L 364 , 718 , an antagonist selective for the CCK A receptor , blocked completely the action of centrally administered CCK , whereas L 365 , 260 , a selective CCK B receptor antagonist , had no effect on the ability of centrally administered CCK to inhibit feeding . ^^^ Intraventricularly administered CCK thus appears to reduce feeding in the rat through a mechanism involving a CCK A receptor subtype in the periphery . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These findings indicate that CER stimulates the release of ir beta END from the adenohypophysis through CCK A receptors and that elevated plasma ir beta END levels is partly involved in some behavioural effects induced by CER . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Nonpeptide antagonists selective for the CCKA and CCKB receptors have recently been developed , and provide long awaited tools to test hypotheses about the role of endogenous CCK as a modulator of dopaminergic function , and the potential of CCK based drugs as treatments for neuropsychiatric disorders . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Hypolocomotion induced by peripheral or central injection of CCK in the mouse is blocked by the CCKA receptor antagonist devazepide but not by the CCKB receptor antagonist L 365 , 260 . ^^^ The pharmacological mechanisms underlying the hypolocomotion induced by intraperitoneal ( i . p . ) and intracerebroventricular ( i . c . v . ) injections of cholecystokinin octapeptide sulphated ( CCK ) in the mouse were examined using selective CCKA and CCKB receptor antagonists . ^^^ The hypolocomotion induced by i . p . injection of 10 micrograms / kg CCK and i . c . v . injection of 3 . 5 micrograms CCK was reversed by the selective CCKA antagonist devazepide , but not by the selective CCKB antagonist L 365 , 260 . ^^^ This suggests that CCK induced hypolocomotion is mediated by CCKA receptors . ^^^ CCK may be due to leakage of the peptide from the brain and subsequent activation of peripheral CCKA receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
They are significant pharmacological tools for the study of CCK A ( peripheral ) and CCK B ( central ) receptors , their biological actions and their associated intracellular messengers . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
According to `` in vitro ' ' binding studies and functional test , nearly all the compounds behaves as CCK antagonists ; moreover some compounds are able to interact differentially with CCK A and CCK B receptor subtype . ^^^ In particular , compounds 2c , 2g , and 2h possess a high affinity for the CCK A receptor subtype coupled with a low affinity for the CCK B subtype . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effects of the CCK A receptor antagonist CR 1409 on the activity of rat midbrain dopamine neurons . ^^^ This suggested that a peripheral type ( CCK A ) CCK receptor mediates this effect . ^^^ Proglumide does not discriminate between CCK A and CCK B ( central type ) receptors . ^^^ In the present study , rats were treated acutely or repeatedly ( 14 days ) with the selective CCK A antagonist CR 1409 . ^^^ Repeated treatment with 5 mg / kg ( IP ) increased the number of spontaneously active DA cells in the A 10 ( ventral tegmental area ) but not the A 9 ( substantia nigra zona compacta ) region , which suggests that these DA populations are differentially affected by prolonged CCK A receptor blockade . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The suppressive effect of ceruletide on barrel rotation could be partially countered by MK 329 , a selective peripheral CCK ( CCK A ) receptor antagonist . ^^^ These findings suggest that ceruletide specifically suppresses the barrel rotation evoked by SMS 201 995 in a long lasting manner possibly acting through CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The specific CCK A antagonist ( L 364 , 718 ) increased gastric emptying of protein rich meals . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Tifluadom , a kappa opioid agonist and cholecystokinin A ( CCK A ) receptor antagonist , was utilized as a model to prepare a series of 2 ( aminomethyl ) and 3 ( aminomethyl ) 1 , 4 benzodiazepines . ^^^ All compounds with IC 50 ' s less than 100 microM proved to have greater affinity for the CCK A receptor , with the most potent analogue , 6e , having an IC 50 of 0 . 16 microM . ^^^ The benzodiazepines described in this study are simultaneously CCK A and opioid receptor ligands . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In homogenate binding studies , L 365 , 260 displayed nanomolar affinity for CCK B receptors in the cerebral cortex of several species including man ( pIC 50 congruent to 8 . 2 ) but showed low affinity for CCK A receptors in the rat pancreas ( pIC 50 congruent to 6 . 3 ) . ^^^ By contrast , the CCK A antagonist MK 329 showed the reverse selectivity ( cortex : pIC 50 congruent to 6 . 9 , pancreas : pIC 50 = 9 . 6 ) . ^^^ L 365 , 260 inhibited binding to most areas of the brain , but in the rat medial nucleus tractus solitarii and the monkey nucleus tractus solitarii . dorsomedial nucleus and infundibular hypothalamic nuclei together with the dorsomedial aspects of the caudate nucleus , where CCK A sites are present , L 365 , 260 failed to displace all 125I BH CCK binding . ^^^ In the primate spinal cord , L 365 , 260 was a relatively weak inhibitor of 125I BH CCK binding ( pIC 50 congruent to 6 . 0 ) whereas MK 329 showed high affinity for the CCK A sites present there ( pIC 50 congruent to 9 . 6 ) . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of the selective CCK A antagonist L 365 , 031 and the selective CCK B antagonist L 365 , 260 on morphine analgesia and opiate tolerance and dependence in rats were examined . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Synthesis and biological activity of new cholecystokinin ( CCK ) analogs with a special CCK A receptor antagonistic effect ] . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This effect was reversed by prior treatment with MK 329 , a selective antagonist of CCK at alimentary type CCK ( CCK A ) receptors . ^^^ Thus , endogenous , small intestinal CCK can cause satiety in the neonatal rat and this effect involves CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In vitro autoradiography was performed in order to visualize cholecystokinin A ( CCK A ) receptors in sections of Cynomolgus monkey brain . ^^^ CCK A receptors were defined as those which displayed high affinity for the selective non peptide antagonist MK 329 ( L 364 , 718 ) and were detected in several regions by selective inhibition of 125I Bolton Hunter CCK using MK 329 or direct labeling with 3H MK 329 . ^^^ In the caudal medulla , high densities of CCK A sites were present in the nucleus tractus solitarius , especially the caudal and medial aspects , and also the dorsal motor nucleus of the vagus . ^^^ CCK A sites were localized to a number of hypothalamic nuclei such as the supraoptic and paraventricular nuclei , the dorsomedial and infundibular nuclei as well as the neurohypophysis . ^^^ The mammillary bodies and supramammillary nuclei also contained CCK A receptor sites . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A 71378 : a CCK agonist with high potency and selectivity for CCK A receptors . ^^^ Receptors for the brain and gut peptide cholecystokinin ( CCK ) have been classified into two classes , CCK A and CCK B . ^^^ To date , peptide analogues with selectivity for the CCK B receptors have been identified , and selective antagonists for CCK A and CCK B receptors have been reported as well ; until now , there have been no reports of highly selective CCK A agonists . ^^^ Herein we describe the properties of A 71378 [ desamino Try ( SO3H ) Nle Gly Trp Nle ( N methyl ) Asp Phe NH 2 ] , a highly selective CCK A receptor ligand . ^^^ The IC 50 values of A 71378 for the pancreatic CCK A , cortical CCK B , and gastrin receptor were 0 . 4 nM , 300 nM , and 1 , 200 nM , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effect of intracerebroventricular and systemic injections of caerulein , a CCK analogue , on electrical self stimulation and its interaction with the CCKA receptor antagonist , L 364 , 718 ( MK 329 ) . ^^^ It is concluded that self stimulation performance may be subject to modulation by CCK receptors distributed predominantly in the peripheral nervous system and that some but not all of these receptors are CCKA receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the present study , we analyzed the proliferative effects of cholecystokinin ( CCK ) and gastrin peptides on a rat tumoral pancreatic cell line , AR42J , which possesses both CCKA and CCKB receptor subtypes . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In contrast , after administration into the postero median nucleus accumbens , the hypoexploration , the increase of emotionality of rats , or the potentiation of dopamine induced hyperlocomotion were obtained after injection of CCK 8 but not of BC 264 , supporting the involvement of peripheral CCKA receptors in these CCK 8 responses . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine the role of CCK A receptors in the cholecystokinin ( CCK ) induced suppression of locomotor activity in the rat , the ability of the selective CCK A receptor antagonist L 364 , 718 to block these responses was investigated . ^^^ It is concluded that L 364 , 718 is a potent antagonist of the actions of CCK 8 and caerulein on locomotor activity , suggesting that the effects of these peptides are mediated by a CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Distinct requirements for activation at CCK A and CCK B / gastrin receptors : studies with a C terminal hydrazide analogue of cholecystokinin tetrapeptide ( 30 33 ) . ^^^ Using 125I Bolton Hunter cholecystokinin octapeptide ( 26 33 ) ( 125I Bolton Hunter CCK 8 ) as the radioligand , A 57696 was found to be selective for cortical CCK B receptors ( IC 50 = 25 nM ) , compared with pancreatic CCK A receptors ( IC 50 = 15 microM ) . ^^^ The Kd of A 57696 at gall bladder CCK A receptors was 19 microM . ^^^ Stimulatory actions of CCK 8 and A 57696 were reversed by the CCK B selective ( R ) L 365 , 260 ( 100 nM ) , whereas at the same concentration , the CCK A selective ( S ) L 365 , 260 was ineffective . ^^^ A 57696 represents a new class of CCK A peptide antagonist at guinea pig pancreas a new class of CCK A peptide antagonist at guinea pig pancreas and gall bladder . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Intracerebral , but not i . p . , injection of a low dose of a CCK antagonist , reversed the effect of peripheral CCK 8 on food intake as did i . p . injection of peripheral CCK A receptor antagonists . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK 8 effects on motivational and emotional states of rats involve CCKA receptors of the postero median part of the nucleus accumbens . ^^^ These results support the neuroanatomical heterogeneity in the distribution of CCK and its binding sites in the NAS , but raise the question of the presence of CCKA receptors not detected in binding studies and of the behavioral effects mediated by CCKB receptor stimulation in this structure . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptors have high affinity for sulphated CCK 8 and for MK 329 but low affinity for desulphated CCK 8 and CCK 4 whilst CCK B sites bind MK 329 with low affinity and discriminate poorly between sulphated and desulphated CCK 8 . ^^^ CCK A receptors are found predominantly in peripheral tissues but they also exist in discrete regions of the primate CNS , including the spinal cord . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It is suggested that the variable effects of MK 329 on morphine induced and opioid mediated social conflict analgesia may reflect differential , dose dependent effects at CCK B and CCK A sites respectively , a proposal consistent with the 500 fold potency difference observed between the two models . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Binding sites for 125I cholecystokinin in primate spinal cord are of the CCK A subclass . ^^^ In monkey and human but not rat spinal cord , 125I CCK binding was dose dependently inhibited by low concentrations of the selective CCK A antagonist L 364 , 718 . ^^^ These data indicate that in striking contrast to CCK receptors in rat spinal cord , those in the primate cord are of the CCK A receptor subclass . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The exact locus of this interaction , or whether it involves ' peripheral type ' ( CCK A ) or ' central type ' ( CCK B ) receptors is not known . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptors in the rat interpeduncular nucleus : evidence for a presynaptic location . ^^^ Using autoradiography , ' peripheral type ' or cholecystokinin A ( CCK A ) receptor binding was measured in the interpeduncular nucleus ( IPN ) of rats which had received electrolytic lesions of the habenular nucleus . ^^^ These data suggest that CCK A receptors in rat IPN are localized on presynaptic terminals within the nucleus . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effect of CCK 8 on aspartate levels was significantly inhibited by the CCKB antagonist , L 365 , 260 ( 20 mg kg 1 , s . c . ) , but not by the CCKA antagonist , L 364 , 718 ( 20 mg kg 1 , s . c . ) . ^^^ While the effect of CCK 8 on aspartate is selectively mediated via CCKB receptor subtype , the effect of CCK 8 on glutamate appears to be mediated via both CCKA and CCKB receptor subtypes . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In addition , the effect of continuous subcutaneous infusion of the CCK A receptor antagonist devazepide was studied . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The protective effects of CCK 8 were almost completely abolished by the blockage of CCK A receptors with loxiglumide , whereas the protective effect of pentagastrin was completely abolished by L 365 , 260 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
However , it has not been established that endogenous CCK causes satiety or whether the response is mediated by peripheral type ( CCK A ) or brain type ( CCK B ) receptors . ^^^ The development of potent and selective antagonists for CCK A ( MK 329 ) and CCK B ( L 365 , 260 ) receptors now allows these issues to be addressed . ^^^ The CCK A antagonist MK 329 and the CCK B antagonist L 365 , 260 increased food intake in partially satiated rats and postponed the onset of satiety ; however , L 365 , 260 was 100 times more potent than MK 329 in increasing feeding and preventing satiety . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Tests were undertaken with and without elimination of endogenous CCK by loxiglumide , a selective CCK A receptors antagonist , before and after eradication of H pylori with triple therapy ( omeprazole , amoxicyllin , bismuth ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These effects were induced by 5 nM CCK 8 but not BC 264 and they were blocked by the CCKA antagonist , L 364 , 718 , but not by the CCKB antagonist , L 365 , 260 . 3 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It has been reported that certain N alpha carboxyacyl analogues of CCK 8 and of CCK 7 with a substituted Gly in position 3 or 4 of the peptide possess higher potencies at stimulating pancreatic enzyme secretion than at stimulating gallbladder contraction , suggesting that these analogues are able to differentiate subtypes of CCKA receptors . ^^^ These data demonstrate that the CCKA receptors in the pancreas and on gallbladder smooth muscle possess similar affinities for the various N alpha carboxyacyl analogues of CCK 7 and CCK 8 with a substituted Gly and provide further evidence that the CCKA receptors in gallbladder and pancreas can not be distinguished pharmacologically . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Although the wide distribution , myriad number of functions , and reported pharmacological heterogeneity of CCK receptors would suggest a large number of receptor subtypes , the application of modern molecular biological techniques has identified two CCK receptors , CCK A receptor ( CCK AR ) and CCK B receptor ( CCK BR ) , that mediate the actions of CCK and gastrin ; gastrin receptors have been found to be identical to CCK BR . ^^^ CCK AR , found predominantly in the GI system and select areas of the CNS , have high affinity for CCK and the nonpeptide antagonist L 364 , 718 , whereas CCK BR , found predominantly in the CNS and select areas of the GI system , have high affinity for CCK and gastrin and the nonpeptide antagonist L 365 , 260 . ^^^ Both CCK AR and CCK BR are highly conserved between species , although there is some tissue specific variation in expression . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The inhibitory effect of 10 micrograms / kg ( s . c . ) CCK 8S was prevented by loxiglumide , a mixed type of CCK A and B receptor antagonist , at 1 mg / kg ( intraperitoneal ) and 40 micrograms / rat ( intracerebroventricular , i . c . v . ) ; L 364 , 718 , a CCK A receptor antagonist , at 125 and 250 ng / rat ( i . c . v . ) ; and L 365 , 260 , a CCK B receptor antagonist at 250 ng / rat ( i . c . v . ) . ^^^ These results demonstrate that peripherally administered CCK 8S inhibits spontaneous ACh release from the frontal cortex through both central CCK A ( mainly ) and B receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selectivity ratio of KSG 504 for pancreatic CCK receptor ( CCK A ) was estimated as 400 . ^^^ In the isolated pancreatic acini of rats , KSG 504 caused a parallel rightward shift of the concentration response curve for CCK 8 stimulated amylase release with no change in its maximal response , indicating a competitive antagonism of the drug for the CCK A receptor ( Schild plot analysis ; slope = 0 . 927 , pA 2 = 6 . 9 ) . ^^^ These results demonstrate that KSG 504 is a competitive and selective CCK A receptor antagonist that is effective in vivo after oral administration . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Because the dipeptoid compounds can occupy all available pancreatic CCKA receptors , these compounds must induce a configuration of the receptor different from either CCK 8 or the previously characterized partial agonist CCK JMV 180 , thereby inducing a distinct signaling pattern . ^^^ Because the dipeptoid compounds do not fully mimic CCK actions , it is likely that they interact with only some of the critical binding sites within the CCKA receptor normally occupied by CCK8 . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Our results indicate that CCK receptors present in chicken ileum behave similarly but not identically to the CCK A receptor described in mammals . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selective CCK A antagonist L 364 , 718 ( Devazepide ) antagonized both types of contraction with a pKB of 10 . 10 and 9 . 95 , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
However , it remains unclear whether these growth effects are mediated specifically by CCK A receptors , CCK B receptors , or both . ^^^ METHODS : Rats were subcutaneously injected with either ( 1 ) CCK 8 , a nonselective CCK agonist ( 2 . 50 micrograms / kg body wt ) ; ( 2 ) A 71623 , a selective CCK A agonist , tert butyl oxycarbonyl Trp Lys ( epsilon N 2 methylphenylaminocarbonyl ) Asp ( N methyl ) Phe NH 2 ( 1 . 84 micrograms / kg body wt ) ; ( 3 ) SNF 8815 ; a selective CCK B agonist , [ ( 2R , 3S ) beta MePhe 28 , N MeNle 31 ] CCK 26 33 ( 2 . 40 micrograms / kg body wt ) ; or ( 4 ) saline ( control ) for 21 days . ^^^ Likewise , selective CCK A agonist significantly increased pancreatic weight , protein , RNA , and DNA contents , protein DNA ratio , RNA DNA ratio , pancreatic area per nucleus , and number of mitoses per 10 , 000 acinar cells . ^^^ CONCLUSION : These findings indicate that pancreatic growth is mediated specifically by CCK A receptors in the rat in vivo . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In order to investigate a possible direct agonist effect of the CCK B / gastrin receptor antagonist , we studied amylase release from isolated rat pancreatic acini in response to PD 136450 and sulfated CCK 8 alone and in combination with the specific CCK A receptor antagonist MK 329 . ^^^ The specific CCK A receptor antagonist MK 329 dose dependently inhibited CCK 8 and PD 136450 induced amylase release . ^^^ In conclusion , the new CCK B / gastrin receptor antagonist PD 136450 exhibited profound agonist actions on the rat pancreas mediated via CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK B / gastrin receptor antagonist L 365 , 260 abolished the stimulating effect of cionin on both histamine release and acid secretion , whereas the CCK A receptor antagonist L 364 , 718 only had a faint effect . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK antagonists reveal that CCK 8 and JMV 180 interact with different sites on the rat pancreatic acinar cell CCKA receptor . ^^^ The ability of CCKA antagonists to inhibit full and partial CCK agonists of the rat pancreatic acinar cell CCKA receptor has been studied . ^^^ Concurrent superfusion of either L 364 , 718 ( 0 . 1 microM ) or lorglumide ( 10 microM ) , chemically distinct , specific , potent antagonists of the CCKA receptor , resulted in a rapid inhibition of the [ Ca2+ ] 1 signal initiated by all concentrations of CCK 8 . ^^^ A model is proposed to reconcile this data , based on the assumption that JMV 180 and CCK 8 interact with discrete sites on the CCKA receptor , which are differentially affected by the binding of antagonists . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It has been previously demonstrated that guinea pig pancreas possesses both cholecystokinin A ( CCK A ) receptors and CCK B ( gastrin ) receptors . ^^^ In contrast to guinea pig pancreas , it is not known whether CCK receptors in rat pancreas are CCK A receptors , CCK B ( gastrin ) receptors , or both . ^^^ Thus , in the present study , we characterized CCK receptors in rat pancreas at the receptor and mRNA level . 125I Bolton Hunter labeled CCK octapeptide ( 125I BH CCK 8 ) , the specific CCK A and CCK B ( gastrin ) receptor antagonists L 364 , 718 and L 365 , 260 , and 125I labeled gastrin 1 were utilized to characterize CCK receptors in normal rat pancreas . ^^^ Additionally , we utilized 32P labeled cDNA probes of the CCK A receptor and CCK B ( gastrin ) receptor coding regions in order to examine the expression of CCK receptor subtypes in normal rat pancreas at the mRNA level . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) is a gut hormone that regulates pancreatic endocrine functions via CCKA receptors . ^^^ The data indicate that some of the synthetic tetrapeptides exhibit a high affinity for the CCK receptor of the endocrine pancreas and that they are highly selective for this ( peripheral ) CCKA receptor subtype . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We showed on AR 4 2J cells that : a minority of CCKA R ( Kd = 0 . 7 nM ) , a classical CCKB R ( Kd = 0 . 93 nM ) and a new high affinity gastrin binding site ( Kd = 2 . 1 pM ) coexisted ; CCK through CCKA R and CCKB R , was more potent to stimulate amylase secretion ( EC 50 = 34 pM ) and Ca2+ mobilization ( EC 50 = 30 pM ) than to occupy its receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The protective effects of CCK were dose dependent and almost completely reversed by pretreatment with the specific CCKA receptor antagonist , loxiglumide , while the CCKB receptor antagonist , L 365 , 260 , was not effective . ^^^ We conclude that CCK exerts protective activity against ethanol induced damage and that this effect is mediated through specific CCKA receptors and hyperemia involving NO . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Expressions of the CCK A and B receptor genes in fetal and adult pancreas of OLETF rats were examined by the reverse transcriptase polymerase chain reaction followed by Southern blot hybridization . ^^^ CCK A receptor mRNA was not expressed in the fetal pancreas of either strain or in the adult pancreas of OLETF rats , but was expressed in the adult pancreas of LETO rats . ^^^ These results suggest that OLETF rats are a new model of a congenital defect of the CCK A receptor gene and should be useful for determining CCK receptor function . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that CCK JMV 180 distinguishes between the CCKA receptors associated with pancreatic exocrine secretion in the acini and those involved in contraction of the isolated gallbladder smooth muscle in rabbits . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pancreatic growth and secretion were not inhibited by CCKA receptor blockade , which suggests that the effects of CCK mediated by the CCKA receptor are not essential for growth or development of the pancreatic amylase secretory response in the neonatal guinea pig . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We examined whether the short term administration of KSG 504 ( KSG ) , a synthetic CCK A receptor antagonist , inhibited the regeneration of pancreatic acinar cells after ethionine induced acute pancreatitis in rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The cyclic analogue 1a has Ki values of 4 . 5 and > 5000 nM at delta and mu opioid receptors , respectively ; and IC 50 values of 1 . 6 and > 10 , 000 nM for CCK A and CCK B receptors , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Therefore , we studied the effect of prolonged suppression of gallbladder emptying with a cholecystokinin ( CCK A ) receptor antagonist on bile formation in Richardson ground squirrels fed a trace versus a 1 % cholesterol diet . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The results confirm that the rainbow trout gallbladder CCK receptor does not distinguish sulfated CCK from sulfated gastrin as do modern CCKA receptors , but does distinguish sulfated from nonsulfated forms of both . ^^^ Finally , studies with antagonists known to be specific for either CCK or gastrin receptors in mammalian systems indicate that this ancient receptor behaves more like a mammalian CCKB receptor than as a CCKA receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To relate specific effects on growth and transformation to activation of specific affinity states of the CCKA receptor stably expressed in CHO cells we compared responses to the CCK analogues JMV 180 and CCK 8 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Identification of a region of the N terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK . ^^^ These results identify for the first time a part of the N terminal , close to the membrane , of the human CCKA receptor that is essential for the high affinity interaction with CCK . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We suggest that ( a ) pancreatic adaptation to high dietary protein is not mediated via CCK A receptors and ( b ) the stimulation of pancreatic protein secretion by a meal or by exogenous CCK 8 is mediated partly by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that both peptides induced the synthesis of the secretory enzyme after occupancy of CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Since L 364 , 718 is known to be a powerful selective antagonist to the peripheral CCK A receptors , these data suggest that the effects produced by exogenous CCK are due to peripheral receptors that project to the NTS . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of the partial muscarinic agonist pilocarpine on physiological responses were investigated in rat pancreatic acinar cells and compared with carbachol , a full muscarinic agonist , together with previous results using JMV 180 , a partial agonist of CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Lack of satiety effect of cholecystokinin ( CCK ) in a new rat model not expressing the CCK A receptor gene . ^^^ We examined whether the CCK A and B receptor genes were expressed in the brain ( hypothalamus ) of OLETF rats in comparison with control ( Long Evans Tokushima Otsuka = LETO ) rats . ^^^ CCK A receptor mRNA was detected in the hypothalamus of LETO rats but not OLETF rats . ^^^ These results show that in OLETF rats the absence of CCK A receptor gene expression in the hypothalamus results in hyperphagia because of lack of satiety . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Therefore , we characterized CCK binding properties and CCK A receptor mRNA expression in pancreatic carcinomas and dysplastic pancreata from the Tg ( Ela 1 , SV40E+Ela 1 , neo ) Bri 19 strain of ELSV transgenic mice . ^^^ RT PCR and Southern blot analysis confirmed the 125I BH CCK 8 binding studies by demonstrating CCK A receptor mRNA expression in the ELSV transgenic pancreatic carcinomas and dysplastic pancreas , as well as in normal nontransgenic mouse pancreas . ^^^ In conclusion , pancreatic carcinomas and dysplastic pancreas from ELSV transgenic mice and normal nontransgenic mouse pancreas all bind 125I BH CCK 8 and express mRNA for the CCK A receptor . ^^^ In contrast to chemically induced pancreatic tumors in the rat , ELSV transgenic mouse pancreatic tumors do not appear to significantly overexpress CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Identification of CCK A receptors on chief cells with use of a novel , highly selective ligand . ^^^ Functional studies suggest that guinea pig chief cells have both cholecystokinin A ( CCK A ) and CCK B receptors ( CCK A R and CCK B R , respectively ) . ^^^ However , all efforts to directly characterize the specific CCK A R using binding have been unsuccessful . ^^^ Recent studies describe specific CCK A R agonists such as A 71378 ( [ desamino Nle 28 , 31 ( N methyl ) Asp 32 ] CCK heptapeptide ] . ^^^ In the present study , [ D Tyr Gly ] A 71378 was synthesized , which has > 300 fold selectivity for CCK A R and can be iodinated . [ D Tyr Gly ] A 71378 was equipotent to A 71378 in stimulating pepsinogen release from purified guinea pig chief cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In a double blind , placebo controlled study , we investigated the effect of the specific CCK A receptor antagonist loxiglumide on food intake ( carbohydrate rich meal ) and on subjective hunger feelings scored with visual analogue scales and food selection lists in seven healthy obese women and in seven healthy lean women . ^^^ In conclusion , in the present study during infusing the CCK A receptor antagonist loxiglumide we found no increase in preprandial satiety nor in food intake of a carbohydrate rich meal nor in postprandial satiety in lean and obese women . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Receptors for cholcystokinin ( CCK ) can be pharmacologically classified into at least two distinct subtypes , CCKAR and CCKBR . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Both somatostatin and CCK A receptor antagonists inhibit stimulation of the gallbladder by CCK . ^^^ The aim of this study was to compare the effect of somatostatin and the CCK A receptor antagonist loxiglumide ( CR 1505 ) on gallbladder volume at baseline and after feeding . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These studies were undertaken to investigate if CCK A and CCK B receptors were perhaps mediating the mitogenic effects of gastrin on Swiss 3T3 cells . ^^^ Receptor antagonists that inhibit the biological effects and binding of peptides to the CCK A ( L 364 , 718 ( L 18 ) ) and CCK B ( L 365 , 260 ( L 60 ) ) receptors were ineffective toward inhibiting the binding and proliferative effects of gastrin on Swiss 3T3 cells . ^^^ Radiolabeled L 18 and L 60 demonstrated no binding to the cells , indicating that CCK A and CCK B receptors may be absent on Swiss 3T3 cells . ^^^ Possible mRNA expression of CCK A and CCK B receptor subtypes by gastrin responsive rodent intestinal and fibroblast cell lines ( Swiss 3T3 , IEC 6 , CA ) was measured by the methods of Northern blot analysis and reverse transcriptase polymerase chain reaction . mRNA from rat pancreas , AR42J cells , and rat antrum served as positive controls . ( ABSTRACT TRUNCATED AT 400 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The behavioral responses induced by BDNL were not significantly blocked by L 365 , 260 , but were suppressed by CI 988 , another selective CCK B antagonist , and by high doses of L 364 , 718 , a selective CCK A antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that peripherally administered CCK 8S has stimulatory effects on the dopaminergic system in the PNAc , and raise the possibility that the effect appears to be mediated via CCKA receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Use of the compound JMV 180 indicated CCK was acting through the low affinity state of the CCKA receptor to reduce CT phosphate levels . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
RESULTS : Exogenous CCK significantly reduced food intake in gastrectomized rats ; this was blocked by administration of a CCK A but not a CCK B receptor antagonist . ^^^ Chronic treatment with a CCK A or CCK B receptor antagonist after total gastrectomy in rats significantly increased postoperative food intake and body weight . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The cardiac and fundic basal mucosae expressed CCK A receptors . ^^^ CCK 8 infused intravenously ( 0 . 1 1 microgram . kg 1 . h 1 ) dose dependently increased the occurrence of relaxations while it was reduced by the CCK A receptor antagonist devazepide but not the CCK B antagonist L 365260 , both administered intravenously in a dose range of 0 . 1 100 micrograms / kg . ^^^ CONCLUSIONS : CCK is involved in the occurrence of transient lower esophageal sphincter relaxations through peripheral CCK A receptors and an L arginine nitric oxide pathway . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK is also responsible , via the CCK A receptor , for the pancreatic hyperplasia observed following the feeding of protease inhibitors or pancreaticobiliary diversion . ^^^ Although cell proliferation is inhibited by gastrin / CCK receptor antagonists , the spectrum of antagonist affinities is not consistent with binding to either CCK A or gastrin / CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK JMV 180 has been demonstrated to act as a functional agonist at high affinity pancreatic CCKA receptors but as a functional antagonist at CCKA low affinity receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The duration of MMC disruption and the increase in colonic spike burst frequency after spermidine administration ( 20 mumol ) were significantly reduced by CCK A and CCK B antagonists . ^^^ These results indicate that exogenous polyamines disrupt intestinal MMCs and stimulate colonic motility through a release of CCK acting at CCK A and CCK B receptors and suggest that endogenous polyamines are involved in the postprandial control of intestinal motility . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
None of the three ureido acetamides , at concentrations up to 1 microM , significantly blocked CCK 8 evoked contractions of the guinea pig ileum in vitro , a CCKA receptor bioassay . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These findings support the view that exogenous CCK reduces food intake in pigs by acting , primarily , on CCKA receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This response is probably mediated through CCK A receptors because CCK 8S , but not CCK 8US , enhanced MA induced responses . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that 1 ) Both muscularly and neurally located CCK receptors are present on the longitudinal layer of chicken ceca whereas only muscular receptors are present on the circular muscle . 2 ) 5HT2 receptors seem to be involved in the neurally mediated CCK 8s response observed in the longitudinal layer . 3 ) The different potency of CCK 8s , CCK 8ns and CCK 4 to induce contractile effects and of the CCK A and CCK B antagonists to block such effects suggests the existence of two different CCK receptors on the circular layer . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The fact that devazepide is 1000 times more potent as a CCK A receptor antagonist than L 365 , 260 , whereas the two compounds are nearly equipotent at the CCK B receptor subtype , suggests that CCK B rather than CCK A receptors are involved in these effects . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Furthermore , the conditioned stimulus ( the odor ) causes behavioral change either by sensitizing a system that includes the CCKA receptor , by causing the release of endogenous CCK , or by changing some non CCK system that enhances the processing of CCKA receptor mediated information . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCKA receptor antagonist devazepide has previously been shown to inhibit vasopressin release induced in pigs by intravenous ( i . v . ) CCK . 3 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The affinity of YM 022 for gastrin / CCK B receptor was more than 2 orders of magnitude higher than that for rat pancreatic CCK A receptor and various other receptors , such as benzodiazepine . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Previous i . c . v . injection of devazepide , a CCKA receptor antagonist , ( 10 micrograms kg 1 ) antagonized the inhibitory effects of both CCK 8s and igmesine injected i . c . v . on dopamine induced colonic hyperkinesia . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Guinea pig gallbladder and pancreas possess identical CCK A receptor subtypes : receptor cloning and expression . ^^^ Pharmacological and functional studies in pancreas and gallbladder demonstrate a CCK A receptor subtype in both tissues . ^^^ However , some pharmacological studies and affinity cross linking studies of CCK receptors on pancreatic acini and gallbladder suggest that these two tissues possess two different subtypes of the CCK A receptor . ^^^ We cloned these receptors in guinea pig using a cDNA clone of the CCK A receptor from rat pancreas . ^^^ The guinea pig gallbladder CCK A receptor was cloned by hybridization screening of a gallbladder cDNA library using a cDNA probe from the rat CCK A receptor coding region . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cloning and expression of the rabbit gastric CCK A receptor . ^^^ This receptor has been cloned and shown to be a CCK A subtype . ^^^ Using polymerase chain reaction with primers from the known sequence of the rat pancreatic CCK A receptor cDNA , we prepared a 600 bp product from rat and rabbit stomach cDNA . ^^^ From Southern analysis these represented a fragment of a gastric CCK A receptor . ^^^ PCR was then used to amplify a rabbit lambda ZAP 2 gastric epithelial cDNA library with the same primers , and the product was identified by sequencing as representing a CCK A receptor fragment . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We transfected COS cells with cDNA for rat cholecystokinin A ( CCK A ) and different CCK B receptors and measured binding of 125I CCK 8 , [ 3H ] L 364 , 718 and [ 3H ] L 365 , 260 to characterize the different affinity states for each type of CCK receptor . ^^^ Rat CCK A and CCK B receptors , canine CCK B receptors and canine mutant CCK B ( M CCK B ) receptors in which the leucine in position 355 was replaced by valine each existed in three different affinity states for CCK 8 , high affinity , low affinity , and very low affinity . ^^^ In rat CCK A and probably CCK B receptors , most were in the very low affinity state , whereas with canine CCK B and M CCK B receptors , most were in the low affinity state . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Devazepide , a preferential CCKA antagonist , only at a high dose ( 100 micrograms / kg ) tended to increase the action of CCK 8 in the plus maze . ^^^ This peculiar interaction between CCK 8 and CCK antagonists could be explained in the light of the opposite role of CCKA and CCKB receptors in the regulation of motor activity in mice . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Metabolism of cholecystokinin ( CCK ) and the effect of L 364 , 718 , a specific CCK A receptor antagonist , on the metabolism of CCK were examined in dogs . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Microiontophoretic administration of sulfated CCK octapeptide ( CCK 8S , agonist for CCK A and CCK B receptors ) and the selective CCK B receptor agonists , CCK 4 and unsulfated CCK 8 , inhibited the firing rates of a subpopulation of SNr neurons . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To further evaluate the role of cholecystokinin ( CCK ) in regulating acid output in humans , dose response curves were constructed to CCK 8 or G 17 ( 6 . 4 800 pmol kg 1 per h ) with and without a specific CCK A receptor antagonist ( loxiglumide ) . ^^^ These data suggest that CCK 8 directly stimulates acid secretion by binding to a CCK B / gastrin receptor on parietal cells , but at the same time inhibits acid responses by stimulating gastric somatostatin release to a CCK A receptor mediated pathway . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Optimization of this series led to the identification of an azabicyclononane amidine , L 740 , 093 [ N [ ( 3R ) 5 ( 3 azabicyclo [ 3 . 2 . 2 ] nonan 3 yl ) 2 , 3 dihydro 1 methyl 2 oxo 1H 1 , 4 benzodiazepin 3 yl ] N ' ( 3 methylphenyl ) urea ] , that bound with high affinity of CCK B receptors from guinea pig cerebral cortex ( IC 50 of 0 . 1 nM ) and had a CCK B / CCK A receptor selectivity of 16 , 000 . ^^^ In comparison , L 365 , 260 had 85 fold lower affinity ( 8 . 5 nM ) and was only 87 fold selective for CCK B over CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To examine the possible contribution of endogenous CCK mechanisms to individual differences in responsivity to AMP treatment , male Wistar rats were divided into low and high AMP responders based on a median split of their locomotor response to AMP and the effects of the selective CCK antagonists L 365 260 ( CCKB ; 0 . 01 , 0 . 1 , 0 . 5 mg / kg ; n = 16 ) and devazepide ( CCKA ; 0 . 001 , 0 . 01 , 0 . 1 mg / kg ; n = 23 ) were determined . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The recent discovery and development of CCK receptor antagonists having selective affinity for either CCKA or CCKB receptors has led to a better understanding of the functional role of CCK and its binding sites in the brain and periphery . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK 8 stimulation was inhibited 80 % by the CCK A selective antagonist L 364 , 718 ( IC 50 = 12 nM ) but not by the CCK B selective antagonist L 365 , 260 . ^^^ The human peptic cell muscarinic cholinergic receptor is not of the M 1 subtype , and the CCK 8 response is predominantly mediated by a CCK A receptor subtype . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This study examined the effect of the CCK A receptor antagonist loxiglumide ( lox ) on gastrin or CCK induced gastric acid secretion and meal stimulated plasma gastrin levels in a placebo controlled study . ^^^ CONCLUSIONS : Blockade of CCK A receptors converts CCK 8 into a potent acid secretagogue and augments postprandial gastrin secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
L 364718 , a CCKB receptor antagonist , had an inhibitory effect against CCK 8 when applied i . c . v . , while L 365260 , a CCKB receptor antagonist , had no influence , suggesting the apparent dominant control of CCKA receptors in the central nervous system on gastric acid secretion . ^^^ The potentiation of the acid secretory response to CCK 8 by the CCKA antagonist was completely blocked by vagotomy or atropine , as well as hexamethonium . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK B antagonist L 365 , 260 ( 10 pmol 1 nmol ) failed to block the gastric vagal afferent response to gastric loads or 100 pmol CCK , while the CCK A antagonist devazepide ( 100 pmol 100 nmol ) competitively and dose dependently attenuated the response to CCK but not to gastric loads . ^^^ These data suggest that 1 ) the vagal afferent response to CCK is mediated through CCK ' s interactions with vagal , rather than pyloric , CCK A receptors , and 2 ) the vagal afferent responses to CCK and to gastric loads are mediated by dissociable , possibly independent , transduction mechanisms . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Gastrin , CCK , and their analogues also inhibit cross linking , and the spectrum of analogue affinities correlates better with the values previously reported for binding to the gastrin / CCK C receptor than with the values reported for binding to either the CCK A or the gastrin / CCK B receptor . ^^^ Cross linking is also inhibited by proglumide and benzotript , but no inhibition is seen with either the CCK A receptor selective antagonist L 364 , 718 or the gastrin / CCK B receptor selective antagonist L 365 , 260 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These facilitatory effects were reversed not only by prior administration of the delta selective antagonist naltrindole ( 0 . 5 mg / kg s . c . ) , but also unexpectedly by the selective cholecystokinin CCK A antagonist MK 329 ( 20 micrograms / kg i . p . ) . ^^^ In addition , the CCK analog [ Boc Tyr ( SO3H ) Nle Gly Trp Nle Asp Phe NH 2 ] ( a mixed CCK A / CCK B agonist ) increased the jump latency and this effect was blocked by MK 329 ( 20 micrograms / kg i . p . ) and by naloxone , but not by the selective CCK B antagonist L 365 , 260 ( 5 mg / kg i . p . ) . ^^^ Taken together , these findings suggest that the potentiating effects of delta agonists on mu mediated analgesia are due to an increase in the release of endogenous CCK interacting with CCK A and CCK B receptors and resulting in positive and negative regulation of the endogenous opioid system . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present study compared the patterns of c fos protein like immunoreactivity ( FLI ) induced in rat brain by CCK and the indirect 5HT agonist dexfenfluramine ( DFEN ) , as well as the ability for devazepide , a CCK A receptor antagonist , to antagonize both anorexia and FLI induced by these agents . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In order to determine receptor domains which are important in conferring specificity for L 365260 and L 364718 we constructed by overlap PCR a rat gastrin / CCK B receptor chimaera which contained the seventh transmembrane domain of the rat CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These changes appear to be mediated by cholecystokinin ( CCK ) because the increases were blocked by infusion of the CCKA receptor antagonist , MK 329 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Gastrin stimulates growth of human colon cancer cells via a receptor other than CCK A or CCK B . ^^^ Two receptors for cholecystokinin ( CCK ) have been isolated which also bind gastrin : CCK A type and CCK B type , both are coupled to phospholipase C ( PLC ) activation . ^^^ The trophic effect was not blocked by receptor antagonists for CCK A ( L 364 , 718 ) or CCK B ( L 365 , 260 ) . ^^^ The gastrin receptor pharmacology on LoVo cells and the lack of appropriate transcripts suggest that gastrin stimulated growth of these cells by a receptor other than CCK A or CCK B type and there likely exists another receptor for gastrin . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of benzodiazepines on cholecystokinin ( CCK ) responses produced following activation of CCKB receptors by pentagastrin in the ventromedial hypothalamus ( VMH ) or CCKA receptors by CCK 8S in the dorsal raphe of the rat brain in vitro have been investigated . 2 . ^^^ In the rat dorsal raphe , where activation of CCKA receptors leads to neuronal depolarization , flurazepam also produced a weak block of the CCK response . 4 . ^^^ At central CCKA receptors , flurazepam blocked CCK 8S responses but the inhibition was not competitive , with a reduction in the peak CCK 8S obtainable in the presence of flurazepam . ^^^ These results suggest that flurazepam acts at a site other than the CCKA receptor itself to block CCK responses in the dorsal raphe . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Observed biological activities of substituted phenyl urea / thiourea tetrapeptides as agonists with the cholecystokinin alimentary canal ( CCK A ) receptor , and ( R ) 4 benzamido 5 oxopentanoic acid derivatives with both peripheral ( CCK A ) and the central ( CCK B ) ( brain ) receptors have been shown to be correlated with various physicochemical , e . g . pi , sigma , and structural , e . g . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We showed in this study that , on guinea pig brain membranes known to possess CCKB and CCKA receptors , [ 125I ] BH [ Leu 15 ] gastrin ( 5 17 ) binds to a single class of high affinity binding sites in a saturable and specific manner . [ 125I ] BH [ Leu 15 ] gastrin ( 5 17 ) interacts with guinea pig brain membranes with a maximal binding capacity that is about three fold lower than that of [ 125I ] BHCCK 8 ( CCK 8 , the C terminal octapeptide of cholecystokinin ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CONCLUSIONS : The stimulation observed after the addition of CCK was the result of activation of the CCK A receptor subtype . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We performed the present studies to distinguish between distinct CCK ( CCK A subtype ) and gastrin ( CCK B / gastrin subtype ) receptors on canine D cells . ^^^ Consistent with this observation was our finding that the CCK A receptor selective antagonist L 364 , 718 dose dependently ( 10 ( 11 ) 10 ( 7 ) M ) inhibited CCK mediated somatostatin release but at the same doses did not alter the effect of gastrin . ^^^ These studies delineate the presence of distinct CCK A and CCK B / gastrin receptors on canine fundic D cells . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Loxiglumide , ( CR 1505 ) , a newly synthesized nonpeptide CCK A receptor antagonist , D . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
With the availability of selective gastrin / CCKB ( L 365 , 260 ) and CCKA ( L 364 , 718 ) receptor antagonists the present study was designed to investigate the role of gastrin and cholecystokinin ( CCK ) receptors in meal stimulated gastric acid secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Concentration response curves to CCK 8S were shifted to the right by low concentrations of the CCKA receptor antagonist , Devazepide , but not by the CCKB receptor antagonist , L 365 , 260 , data which indicate that receptors were of the CCKA subtype . ^^^ An excess of CCK 8S inhibited binding as did Devazepide , but not L 365 , 260 , confirming that binding sites were CCKA subtype receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Tetrapeptide CCK A agonists : effect of backbone N methylations on in vitro and in vivo CCK activity . ^^^ Chem . 1991 , 34 , 2387 2842 ) as a potent and selective CCK A agonist . ^^^ N alpha Methylation at the position corresponding to Asp 32 ( CCK 33 numbering ) was consistent with high affinity , efficacy , and selectivity for the CCK A receptor . ^^^ The observation of parallel structure binding affinity profiles with respect to sites of N methylation in the C terminal regions of tetrapeptide vs heptapeptide CCK analogues suggests that the two series interact similarly with the CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Binding of cholecystokinin 8 ( CCK 8 ) peptide derivatives to CCKA and CCKB receptors . ^^^ The structural requirements for the selective binding of cholecystokinin 8 ( CCK 8 ) related peptides to peripheral ( CCKA ) receptors are not sufficiently understood . ^^^ The pentapeptide derivative of CCK 8 , succinyl Tyr ( SO3H ) Met Gly Trp Met phenethylamide , was found to bind selectively with high affinity to the CCKA receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Expression of the CCK A receptor gene in the pancreas and pancreatic exocrine function was examined in diabetic model rats ( OLETF ) at 5 wks of age . ^^^ Little or no CCK A receptor was detected in the pancreas of OLETF rats . ^^^ These results suggest that OLETF rats are a new experimental model for congenital deficiency of CCK A receptor in the pancreas . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pharmacological experiments using CCK or NPY analogs suggest that both subtypes of CCK ( CCK A and CCK B ) and NPY ( Y 1 and Y 2 ) receptor binding sites are expressed by discrete populations of neurons in the nodose ganglion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Devazepide ( L 364 , 718 ) , a selective antagonist of CCKA receptors , effectively blocked the action of CCK 8 ( s ) , but not that of CCK 4 ( 30 33 ) or SNF 9007 ( phase 1 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCKB pharmacological profile as shown in competition studies by using several CCK related compounds and nonpeptide CCK antagonists discriminating between CCKA and CCKB sites . ^^^ Since rise in [ Ca2+ ] 1 noted by stimulation of C 6 cells with CCK 8S could be blocked by the CCKB receptor antagonist L 365 , 260 ( 100 nM ) but not by the CCKA receptor antagonist L 364 , 718 ( 100 nM ) , CCK induced calcium signal is triggered by activation of CCKB receptors in C 6 cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The protective effects of systemic ceruletide were blocked , partially but significantly , by the preadministration of L 364 , 718 ( 3S ( ) N [ 2 , 3 dihydro 1 methyl 2 oxo S phenyl 1H 1 , 4 benzodiazepine 3 yl ] 1H indole 2 carboxamide , 1 10 mg / kg i . p . ) , a selective CCK A receptor antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The antinociceptive activity of SNF 9007 was not a result of the activation of CCK receptors , as treatment with either CCK A or CCK B receptor antagonist was ineffective in blocking SNF 9007 antinociception . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effect of a novel CCKA receptor antagonist ( 2 NAP ) on the reduction in food intake produced by CCK in pigs . ^^^ The effect of a novel CCKA receptor antagonist 2 naphthalene sulphonyl L aspartyl 2 ( phenethyl ) amide , sodium salt ( 2 NAP ) on the reduction of food intake induced by exogenous CCK , administered centrally or peripherally , has been examined in pigs . 2 NAP is hydrophilic and should not readily cross the blood brain barrier . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This effect of CCK 8 could be reversed by Devazepide , a CCK A receptor antagonist dose dependently at 50 ng and 200 ng , and by L 365 , 260 , a CCK B receptor antagonist at 5 ng and 8 ng administered to the same site . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
After L 364 , 718 , a CCK A receptor antagonist , or ritanserin , 5 HT 2 receptor antagonist , the duration of the ileal postprandial motor pattern was reduced by 60 % . ^^^ In the distal colon , the postprandial response was inhibited by CCK A , CCK B , and 5 HT 2 receptor antagonists , whereas they were inactive in the proximal colon . ^^^ These results suggest that , in rats , CCK 8 is involved in the control of the ileal motor response to feeding through CCK A receptors and in that of the distal colon through both CCK A and CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In a previous study , we developed a new antagonist radioligand , 125I Bolton Hunter labeled JMV 179 , for the CCK A receptor ( CCK AR ) , to analyze CCK antagonist binding sites in pancreatic plasma membranes . ^^^ The binding of 125I ASA JMV 179 to plasma membranes was inhibited by JMV 179 ( IC 50 , 6 + / 2 nM ) , by ( Thr 28 , Ahx 31 ) CCK 25 33 ( IC 50 , 1 . 2 + / 0 . 5 nM ) , and by the nonpeptide CCK AR antagonist L 364 , 718 ( IC 50 , 2 + / 1 nM ) . ^^^ Photoaffinity labeling using pancreatic membranes or acini demonstrated that 125I ASA JMV 179 detected a new 47 50 kDa protein in addition to the 85 100 kDa CCK AR . ^^^ In competition assays using nonsolubilized or solubilized membranes , this protein displayed binding features of the CCK AR and was retained on immobilized wheat germ agglutinin , as was the CCK AR . ^^^ Protease digestions of both the CCK AR and the 47 50 kDa protein yielded identical labeled fragments , demonstrating a structural relationship between the two proteins . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In humans , CCK A antagonists like loxiglumide or L 364 , 718 at doses that completely inhibited the action of supraphysiological doses of exogenous CCK reduced meal stimulated pancreatic enzyme secretion only by approximately 50 % . ^^^ CCK A antagonists caused slight hypotrophy and hypoplasia of the exocrine pancreas . ^^^ However , even after 9 months of effective blockade of the CCK A receptor , mice had normal body weight and an almost normal pancreas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK interaction with the gallbladder smooth muscle CCKA receptor was studied in further detail . ^^^ CCK and the CCKA gallbladder muscularis receptor are main regulators of postprandial gallbladder emptying . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Blocking CCK A receptors accelerates gastric emptying of liquid meals and abolishes the gastrocolonic reflex . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A review of the literature encompassing numerous pharmacological , physiological , and biochemical studies indicates the presence of at least four CCK receptor types , CCKA , CCKB , gastrin , and CG 4 receptors . ^^^ Genomic and cDNA library hybridization as well as Northern and Southern hybridization studies among rat , guinea pig , and human species identifies only two members of the CCK receptor family , CCKAR and CCKBR . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A new CCK A antagonist , KSG 504 , administered intraduodenally , inhibits pancreatic secretion in rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Novel Asp 32 replacement tetrapeptide analogues as potent and selective CCK A agonists . ^^^ These analogues , which lack an acidic residue at the penultimate position , demonstrated surprisingly high CCK A receptor affinity and selectivity . ^^^ The effect of N methylation pattern on CCK A receptor affinity showed consistent trends for analogues in which n = 1 , 2 , or 3 , with the di N methylated analogues having the highest affinity in each case . ^^^ Two conformationally constrained analogues also demonstrated high CCK A receptor affinity and selectivity , as well as nearly maximal agonist activity . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A selective tetrapeptides containing lys ( N epsilon ) amide residues : favorable in vivo and in vitro effects of N methylation at the aspartyl residue . ^^^ Previous structure activity studies on a series of CCK A selective tetrapeptide agonists , typified by A 71623 ( Boc Trp Lys ( CONH Ph o Me ) Asp ( N Me ) Phe NH 2 ) , have shown that replacement of the Lys ( N epsilon carbamoyl ) substituent with N epsilon acyl substituents resulted in partial agonists with moderate to high affinities for the CCK A receptor and that replacement of the C terminal dipeptide with either ( N Me ) Asp Phe or ( N Me ) Asp ( N Me ) Phe was highly favorable to in vitro and in vivo CCK activity . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The results of the present study indicate that activation of both CCKB and CCKA receptors may prevent the development of tolerance to morphine , and the sulfate group in the CCK 8 molecule may be essential for the tolerance inhibition . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Sulfation of the tyrosine residue in CCK 8 is known to be important for its activity at CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
FPL 14294 [ 4 ( sulfoxy ) phenylacetyl ( MePhe 6 ) CCK 6 ] is a CCK analog with enhanced metabolic stability that was comparable to CCK 8 in potency to contract isolated gallbladder and in affinity at the CCK A and CCK B receptor . ^^^ Anorectic activity was inhibited by pretreatment with a CCK A antagonist ( MK 329 ) but not by a CCK B antagonist ( L 365 , 260 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Blocking of CCK A receptors by MK 329 did not significantly change the effect of GRP , whereas prevention of secretin release by removal of the small intestine caused a 13 fold reduction in the GRP induced pancreatic bicarbonate secretion and completely abolished the effect on hepatic bicarbonate secretion but did not change the effect on pancreatic protein secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin octapeptide analogues suppress food intake via central CCK A receptors in mice . ^^^ The selective CCK A receptor antagonist MK 329 reversed the inhibitory effect of the centrally as well as peripherally administered CCK 8 , or of Suc ( Thr 28 , Leu 29 , MePhe 33 ) CCK 7 , whereas the selective CCK B receptor antagonist L 365260 did not . ^^^ These findings suggest the participation of CCK A receptors in the brain in mediating the satiety effect of CCK and the difference in CCK A receptors in the brain and peripheral tissues . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Administration of the selective CCKA receptor antagonist MK 329 , but not the CCKB receptor antagonist L 365 , 260 , prior to CCK injection , prevented oxytocin release as measured by radioimmunoassay and oxytocin neuronal activation as measured by electrophysiology and by the lack of induction of c fos mRNA . 3 . ^^^ We conclude that CCK acts on CCKA receptors , either in the area postrema or on peripheral endings of the vagus nerve , to cause the release of hypothalamic oxytocin and ACTH . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
KSG 504 , a new synthetic cholecystokinin ( CCK ) receptor antagonist derived from proglumide , has superior selectivity and affinity to CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Saturation and competitive binding studies were carried out using sulphated CCK 8 and two selective CCK receptor antagonists : MK 329 , to define type A ( CCKA ) binding sites ; and , L 365 , 260 , to define type B ( CCKB ) binding sites . ^^^ However , both MK 329 ( IC 50 = 18 nM ) and L 365 , 260 ( IC 50 = 45 nM ) competed for vagal 125I CCK binding indicating the presence of CCKA and CCKB binding sites . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Furthermore , the selective CCKA antagonist CAM 1481 inhibited the increase in [ Ca2+ ] 1 induced by CCK 8 ( half maximal inhibitory concentration = 3 nM ) in GLC 19 but not in H 510 cells . ^^^ Thus , the effects of CCK 8 are mediated through CCKA receptors in GLC 19 cells and via CCKB / gastrin receptors in H 510 cells . ^^^ Our results show , for the first time , that CCKA receptors can mediate Ca2+ mobilization and growth in SCLC cells and that SCLC cells express two distinct functional CCK receptor subtypes . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Since cDNA of both the CCK A receptor ( classical pancreatic CCK receptor ) coding region and the CCK B receptor coding region have recently been cloned and sequenced , we investigated the expression of messenger RNA of these receptors in DSL 6 pancreatic carcinoma . ^^^ Our results showed that the 32P labelled cDNA probe of the CCK A receptor coding region hybridized with an approximately 2 . 7 kb mRNA from both DSL 6 pancreatic carcinoma and normal rat pancreas . ^^^ However , the relative expression of the CCK A receptor mRNA in DSL 6 pancreatic carcinoma was approximately 8 fold of that in normal rat pancreas . ^^^ In summary , the CCK A receptor mRNA is overexpressed approximately 8 fold and the gastrin ( CCK B ) receptor mRNA is novelly expressed in DSL 6 pancreatic carcinoma as compared to normal rat pancreas . ^^^ The gene overexpression of the CCK A receptor and the novel gene expression of the gastrin ( CCK B ) receptor may be generated by alterations in gene regulation during carcinogenesis , and may play an important role in promoting tumor growth . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These effects were blocked by the CCK A antagonist MK 329 ( 0 . 02 mg / kg ) , supporting the involvement of CCK A receptors in CCK induced analgesia . ^^^ The results suggest that activation of CCK A receptors by BDNL leads to antinociceptive responses indirectly mediated by stimulation of mu opioid receptors by endogenous enkephalins . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCKA receptor mediates classical CCK like effects on the gut . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Derived by reasoned modification of the CCK A selective 3 carboxamido 1 , 4 benzodiazepine , MK 329 , this paper chronicles the development of potent , orally effective compounds in which selectivity for the CCK B receptor subtype was achieved . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
No binding was detected with the CCK A antagonist [ 3H ] L 364 , 718 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The results show 1 ) that hyperCCKemia raised the histidine decarboxylase ( HDC ) activity of the ECL cells in PCS rats but not in control rats , and the CCK A receptor blockade failed to prevent the enzyme activation ; and 2 ) that PBD prevented the ECL cell hypoplasia and the decrease in HDC activity induced by antrectomy . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We had reported earlier on a novel series of potent and selective tetrapeptide cholecystokinin A ( CCK A ) agonists of the general structure Boc Trp Lys [ epsilon Y ] Asp N ( R ) PheNH 2 [ Y = amides , ureas ; R = H , Me ] that were potent anorectic agents in rats . ^^^ In general , these analogues maintained good potency and selectivity for the CCK A receptor ( guinea pig pancreas ) , as well as potent anorectic activity in rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The use of selective CCK antagonists has allowed to establish that the gastric motor effect of the peptide is direct and mediated through the stimulation of CCK A receptors . ^^^ As a consequence , CCK A antagonism results in acceleration of emptying rate under certain experimental and clinical conditions . ^^^ This peculiar pharmacologic effect of CCK A antagonists , which could be useful in the treatment of functional dyspepsia ( idiopathic or diabetic ) , gastroparesis and gastro esophageal reflux disease ( where patients often display a delayed emptying rate of solid food ) needs to be further investigated , in order to fully explore their potential as gastrokinetic drugs . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In addition , icv administration of CCKA but not CCKB receptor antagonist prevents meal and CCK 8 induced colonic hyperkinesia in dogs . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK A ) and gastrin ( CCK B ) receptors have been demonstrated in the azaserine induced rat pancreatic carcinoma DSL 6 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Recent studies have suggested that this growth promoting effect of CCK was initiated through the occupation of the CCKA receptor . ^^^ As an answer to the first question , rats were infused with CCK JMV 180 , a CCKA high affinity agonist , at doses of 50 , 100 , 150 , and 300 micrograms . kg 1 . h 1 , or Cae ( 0 . 25 micrograms . kg 1 . h 1 ) for 4 days . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In addition , in ARIP cells , the CCK 8 induced increase in cytosolic calcium was abolished by pretreatment with the selective CCK B receptor antagonist L 365 , 260 but not by the CCK A receptor antagonist L 364 , 718 . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Competition experiments indicated that L 365 , 260 , a selective CCK B ( gastrin ) receptor antagonist , was the most potent displacer of 125I CCK 8 , and no significant displacement of binding was found with the selective CCK A receptor antagonist . ^^^ Growth of PANC 1 cells in culture was stimulated by CCK at a concentration consistent with the Kd , and CCK stimulated growth was inhibited by the CCK B receptor antagonist ( L 365 , 260 ) not the CCK A receptor antagonist ( L 364 , 718 ) . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Injection of the CCK A antagonist L 364 , 718 30 min before CCK 8 injection eliminated c fos expression in these regions . ^^^ These findings support the hypothesis that CCK 8 induced c fos expression is mediated by CCK A receptors . ^^^ Meal induced c fos expression was not blocked by the CCK A antagonist L 364 , 718 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The cholecystokinin ( CCK ) family of peptides and receptors are present throughout the brain and gastrointestinal tract and can be pharmacologically subdivided into two subtypes : CCKA and CCKB . ^^^ We used the rat CCKAR cDNA to isolate the human CCK receptor cDNA homologue from human gallbladder which encodes a unique 428 amino acid protein having > 90 % homology to the rat and guinea pig CCKAR . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Neither the CCK A receptor antagonist L 364 , 718 nor the CCK B receptor antagonist L 365 , 260 ( 10 ( 9 ) 10 ( 7 ) moles / kg ) antagonized CCK 8 actions . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Intra accumbens infusion of CCK ( 10 ng ) , or s . c . administration of the CCKA receptor antagonist devazepide had no effect upon response rates . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Energy calculations were performed for CCK 8 ( Asp 26 Tyr ( SO 3 ) 27 Met 28 Gly29 Trp 30 Met31 Asp 32 Phe33 NH 2 , 1 ) and [ desaminoTyr ( SO 3 ) 27 , Nle 28 , 31 ] CCK 7 ( 2 ) , which are nonselective ligands of CCK receptors , and for the CCK A selective analog [ desaminoTyr ( SO 3 ) 27 , Nle 28 , 31 , N Me Asp 32 ] CCK 7 ( 3 ) and the CCK B selective analog [ desaminoTyr ( SO 3 ) 27 , Nle 28 , N Me Leu 31 ] CCK 7 ( 4 ) . ^^^ The proposed models are consistent with the results of biological testing for CCK related peptides including cyclic analogs and CCK A selective tetrapeptides . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selective non peptide CCKB receptor antagonist L 365 , 260 was more potent than the selective CCKA receptor antagonist MK 329 in inhibiting the [ Ca2+ ] 1 mobilization elicited by 10 nM CCK 8 with IC 50 values of 20 + / 8 nM and 400 + / 100 nM , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present study was performed to determine whether these effects are mediated by way of CCK A receptors , CCK B receptors , or both . ^^^ Both CCK octapeptide and the selective CCK A agonist tert butyloxycarbonyl Trp Lys ( epsilon N 2 methylphenylaminocarbonyl ) Asp ( N methyl ) Phe NH 2 stimulated pancreatic growth and the development of acidophilic atypical acinar cell foci and nodules . ^^^ Furthermore , the effect produced by the selective CCK A agonist tert butyloxycarbonyl Trp Lys ( epsilon N 2 methylphenylaminocarbonyl ) Asp ( N methyl ) Phe NH 2 was greater than that produced by CCK octapeptide . ^^^ These findings suggest that the growth of putative preneoplastic lesions ( acidophilic atypical acinar cell foci and nodules ) in the rat pancreas during the early stages of azaserine induced pancreatic carcinogenesis is mediated specifically by way of CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pharmacological analysis using selective agonists and antagonists indicated the expression of the CCK A receptor at birth , whereas the CCK B receptor predominated at postnatal stages . ^^^ Consequently , this study demonstrated 1 ) the differential expression of CCK A and B receptors in developing calf pancreas , 2 ) the predominance of CCK B receptors in normal pancreas , and 3 ) the maturation of CCK B receptors during the weaning period , which includes the glycosylation level . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The role of cholecystokinin ( CCK ) as a central and peripheral satiety factor was studied using the CCK B ( L 365 , 260 ) and CCK A ( MK 329 ) receptor antagonists in esophageal fistula dogs . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Devazepide powerfully blocked responses to CCK 8S with an affinity ( pKB = 9 . 54 ) that was in agreement with reported functional data obtained in pancreatic amylase secretion studies , a system exhibiting CCKA receptor activity . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Neither an inactive analog ( LY 206890 ) nor a CCK A selective analog ( LY 219057 ) affected the number of spontaneously active A 10 DA cells . ^^^ The diphenylpyrazolidinone CCK B antagonists , but neither the inactive nor the CCK A selective analog , also decreased the number of spontaneously active A 9 DA cells ; however , none of these compounds produced catalepsy in awake animals . ^^^ These results indicate that the firing of A 9 and A 10 DA neurons is suppressed specifically by antagonism of CCK B , but not CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The receptor subtype mediating this action of CCK was investigated with selective CCK A and CCK B receptor agonists and antagonists . ^^^ CCK 8 and A 71623 , a potent CCK A selective agonist , were similar in efficacy and potency for stimulating OT secretion . ^^^ MK 329 , a CCK A receptor selective antagonist , at a dose of 20 nmol / kg fully inhibited the action of 20 nmol / kg CCK 8 , while 100 nmol / kg of ( R ) L 365 , 260 , a CCK B selective antagonist , had no effect on the CCK 8 response . ^^^ These results , together with previous lesion studies , suggest that vagal CCK A receptors in the periphery mediate the activation of the oxytocinergic pathway in vivo . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Moreover , neither the response to gastrin 17 nor that to CCK 8s was affected by concomitant infusion of devazepide ( 200 micrograms / kg / h ) , a selective CCK A receptor antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Exogenous CCK 8s and the CCK A receptor antagonist devazepide were infused continuously by means of osmotic minipumps . ^^^ Moreover , the trophic effects of PBD and of the combination of PBD and PCS could be prevented by CCK A receptor blockade ( devazepide infusion ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Operant feeding was recorded in 18 h deprived pigs after peripheral ( 4 ) or central ( ICV ) administration of saline , the CCK A agonist A 71378 , the CCK B agonist pentagastrin , or pentagastrin vehicle . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Extracellular single unit recording techniques were used to study the effects of the cholecystokinin A ( CCK A ) antagonist , L 364 , 718 , and the CCK B antagonist , PD 134308 , on DA neuronal activity in chloral hydrate anesthetized rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In this study we used JMV 180 to evaluate the potential participation of these two CCK A sites in the satiety effect of CCK 8 in rats and mice . ^^^ Both CCK 8 and JMV 180 induced suppression of food intake were attenuated by the CCK A antagonist MK 329 ( 24 . 8 nmol / kg ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Proglumide ( 1 and 10 mg / kg SC ) and devazepide , ( a selective CCK A receptor antagonist ; 0 . 01 and 1 mg / kg SC ) , as well as caerulein ( 0 . 01 , 0 . 1 and 1 microgram / kg SC ) and CCK 4 ( a selective CCK B receptor agonist ; 25 and 50 micrograms / kg SC ) had no reliable effect . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selective CCKA receptor antagonist L 364 , 718 potently inhibited CCK 8S induced slow depolarizations ( IC 50 2 . 9 pM ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Furthermore , 10 micrograms / kg of L 365 , 260 , a CCK B receptor antagonist , and 1 mg / kg of devazepide , a CCK A receptor antagonist , even tended to augment the effect of NMDA in the plus maze . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A selective agonist A 71378 was 85 90 % as efficacious as CCK 8 and was equally potent . ^^^ These results demonstrate that gastrin and CCK 8 can alter chief cell function by interacting with either a CCK A or CCK B / gastrin receptor . ^^^ Activation by CCK related peptides of the CCK A receptor subtype accounts for 85 90 % of the maximal changes in cellular function , and activation of the CCK B / gastrin receptor accounts for 10 20 % of maximal changes . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK stimulated acid secretion was not blocked by L 365 , 260 , a CCKB / gastrin receptor antagonist , and was significantly increased by devazepide , a CCKA receptor antagonist , given alone or together with L 365 , 260 . ^^^ We conclude : 1 ) pentagastrin stimulates acid secretion through a gastrin type receptor , but CCK may not , and 2 ) pentagastrin and CCK can stimulate acid secretion despite simultaneous blockade of CCKB / gastrin and CCKA receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The anorexic effect caused by 4 . 0 micrograms / kg was attenuated by 100 micrograms / kg of the type A CCK receptor antagonist MK 329 but not by 300 micrograms / kg of the type B CCK receptor antagonist L 365 , 260 , suggesting that CCK induced suppression of food intake in this species is mediated by a CCK A receptor . ^^^ Administration of both CCK A and CCK B receptor antagonists alone resulted in no change in meal size . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
COS cells transfected with this cDNA clone bound CCK 8 and L 364 , 718 with high affinities appropriate for the CCKA receptor , and exhibited a transient increase in intracellular calcium in response to CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A antagonist completely blocked LH secretion in response to CCK , whereas the CCK B antagonist had no effect . ^^^ To assess whether endogenous CCK , released in response to food intake , stimulates LH secretion , six monkeys were fasted for 1 day and then provided with a normal meal of monkey chow ( i . e . a refeed meal ) the following day , with either no antagonist , CCK A antagonist , or CCK B antagonist administered 30 min before the meal . ^^^ The refeed meal led to a comparable stimulation of LH secretion regardless of whether monkeys received no antagonist ( 3 . 7 + / 0 . 44 LH pulses / 9 h ) , CCK A antagonist ( 3 . 33 + / 0 . 56 LH pulses / 9 h ) , or CCK B antagonist ( 4 . 0 + / 0 . 78 LH pulses / 9 h ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine if endogenous cholecystokinin ( CCK ) was responsible for the decrease in food intake caused by MCT , birds were injected with the CCK A receptor antagonist devazepide ( DVZ , 1 mg / kg BW ) before diet presentation . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In our study , we used loxiglumide , a potent CCK A receptor antagonist , to investigate the role of CCK A receptors in pancreatic consumption of circulating AAs and enzyme secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A series of new spiroglumide amido acid derivatives was synthesized and evaluated for their ability to inhibit the binding of cholecystokinin ( CCK ) to guinea pig brain cortex ( CCKB receptors ) and peripheral rat pancreatic acini ( CCKA receptors ) , as well as to inhibit in vitro the gastrin induced Ca2+ increase in rabbit gastric parietal cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptor mRNA level was determined by Northern blot analysis with a rat CCK A receptor cDNA probe . ^^^ The level of CCK A receptor mRNA first decreased , reaching the lowest level 7 days after occlusion , and then began to increase . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This study provides evidence that CCK exerts an inhibitory effect on gastric acid secretion and plasma gastrin release as well as a stimulatory influence on the release of PP and somatostatin via CCK A receptors but does not influence directly insulin or glucagon secretion in man . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present results suggest that the activation of CCKA and CCKB receptors by endogenous CCK , could play an opposite role in the control of behavioral responses induced by endogenous enkephalins . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The compounds tested were selective CCK B antagonists [ CI 988 ( 0 . 01 1 mg / kg SC ) , L 365 , 260 ( 0 . 004 2 mg / kg IP ) and LY 262 , 691 ( 0 . 001 1 mg / kg SC ) ] , CCK B agonists [ CCK 4 ( 0 . 01 1 mg / kg SC ) and BC 264 ( 0 . 004 1 mg / kg IP ) ] and CCK A antagonists [ devazepide ( 0 . 001 1 mg / kg SC ) and lorglumide ( 0 . 01 1 mg / kg SC ) ] . ^^^ None of these drugs induced the expected behavioural effects , i . e . an anxiolytic like release of the behavioural suppression with CCK B and , possibly , CCK A antagonists and / or a further reduction of lever pressing with CCK B agonists , indicative of an anxiogenic like potential . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin applied iontophoretically as the sulfated octapeptide ( CCK 8S ) or as highly selective CCKA and CCKB agonists induced excitatory as well as inhibitory effects on dorsal lateral geniculate unit activity . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine what subtype ( s ) of CCK receptors are involved in antagonizing the antinociception induced by these opioids , effect of lorglumide sodium salt ( a CCKA receptor antagonist ) or PD 135 , 158 N methyl D glucamine salt ( a CCKB receptor antagonist ) on opioid induced inhibition of the tail flick response was examined . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Discovery of 1 , 5 benzodiazepines with peripheral cholecystokinin ( CCK A ) receptor agonist activity . 1 . ^^^ Despite decreased affinity for the human CCK A receptor , relative to CCK 8 , some of these compounds are equipotent to CCK as anorectic agents in rats following intraperitoneal administration . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The demonstration that systemic administration of the CCKA receptor antagonist , devazepide , increases food intake in rats has provided the strongest support for the hypothesis that endogenous peripherally released cholecystokinin ( CCK ) acts as a satiety factor . ^^^ The present study was therefore undertaken to confirm the hypothesis that endogenous peripheral CCK is a satiety factor by investigating the effects of a novel CCKA receptor antagonist , 2 NAP , which is unlikely to cross the blood brain barrier , on food intake in rats . 2 . 2 NAP ( 1 16 mg kg 1 , i . p . ) had no significant effects on the intake of a test meal in rats . 3 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In vitro binding studies showed that some derivatives exhibited potent affinity for gastrin CCK B receptor and high selectivity over peripheral CCK ( CCK A ) receptor . ^^^ Structure activity relationship studies of this series suggested that 1 [ ( R ) 2 , 3 dihydro 1 ( 2 , 3 dihydro 1 ( 2 methylphenacyl ) 2 oxo 5 phe nyl 1H 1 , 4 benzodiazepin 3 yl ] 3 ( 3 methylphenyl ) urea ( 35b , YM 022 ) was the optimal compound with IC 50 values of 0 . 17 , 0 . 11 and 150 nM for gastrin , CCK B and CCK A receptors , respectively , and an ED 50 value of 9 . 5 nmol / kg ( i . v . ) in rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The sulphated octapeptide C terminal fragment of cholecystokinin ( CCK 8S ) is present in high concentration in the mammalian brain , where it acts via two types of receptor denoted CCKA and CCKB . ^^^ Using in vivo extracellular unitary recordings of CA 3 pyramidal hippocampal neurons , we compared the effect of SNF 8702 , a potent selective CCKB receptor agonist , to that of CCK 8S , and assessed the effects of selective CCKA and CCKB antagonists . ^^^ Both CCK 8S and SNF 8702 induced activations were suppressed by the microiontophoretic application of the CCKB antagonist CI 988 , but not by that of the CCKA antagonist SR 27897 . ^^^ CCK 8S induced activation was not significantly modified by the intravenous administration of the CCKA antagonists devazepide and SR 27897 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
MATERIALS AND METHODS : Male NMRI mice weighing 12 15 g were assigned to six groups ( 10 mice / group ) which were treated with different combinations of 0 . 9 % NaCl , omeprazole , a CCK A antagonist , a CCK B antagonist , loxiglumide , and L 365 , 260 for 10 days each according to different protocols . ^^^ RESULTS : Omeprazole caused a marked , 10 fold increase in serum gastrin which was not affected by the gastrin antagonist , but markedly reduced by the CCK A antagonist . ^^^ In contrast , the CCK A antagonist significantly decreased pancreatic weight and protein content . ^^^ The inhibitory effect of loxiglumide on omeprazole induced increase in serum gastrin might be explained by recent findings which showed that CCK A antagonists can stimulate gastric acid secretion probably due to a reduction of the inhibitory effect of basal CCK on the D cell and its somatostatin release . ^^^ Probably such a slight stimulation of gastric acid secretion caused by the CCK A antagonist might reduce the gastrin increase caused by omeprazole ' s abolishment of acid secretion . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK B antagonists suppressed CCK 4 induced calcium mobilization more potently than CCK A antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Additional experiments indicated that , as with feeding , CCK 8S inhibits water intake by an action at peripheral CCKA receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To gain a better understanding of the roles of CCK A and CCK B receptors in spinal nociceptive transmission during inflammation , this study evaluated the effects of intrathecally administered FK 480 ( a CCK A receptor antagonist ) and YM 022 ( a CCK B receptor antagonist ) . ^^^ These data indicate that a CCK B receptor antagonist , but not a CCK A receptor antagonist , produces an antinociceptive effect in the rat formalin test . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The two known receptors mediating the actions of cholecystokinin ( CCK ) and gastrin , CCK type A ( CCKAR ) and CCK type B ( CCKBR ) receptors , are G protein coupled receptors having approximately 50 % amino acid homology . ^^^ Both the CCKAR and CCKBR have high affinity for sulfated CCK peptides , while only the CCKBR has high affinity for gastrin peptides . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Both CCK A and CCK B receptor subtypes were visualized in the nucleus of the solitary tract and the area postrema of normal rats , but levels of binding to both of these subtypes were unaffected by the experimental treatments . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We then used the type A cholecystokinin ( CCK A ) receptor antagonist devazepide to assess the importance of CCK in mediating the anorexia produced by oleic acid . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Peptoid CCK receptor antagonists : pharmacological evaluation of CCKA , CCKB and mixed CCKA / B receptor antagonists . ^^^ In radioligand binding assays , the dipeptoid PD 135666 ( ( benzenebutanoic acid , beta [ [ 3 ( 1H indol 3 yl ) 2 methyl 1 oxo 2 [ [ ( tricyclo [ 3 . 3 . 1 . 1 ( 3 , 7 ) ] dec 2 yloxy ) carbonyl ] amino ] propyl ] amino ] , [ R ( + * , S * ) ] ) selectively inhibited [ 125I ] Bolton Hunter CCK 8 binding to CCKB receptors in mouse cerebral cortex ( CCKB IC 50 = 0 . 1 nM ) but was weaker as an inhibitor of CCKA receptor binding in the rat pancreas ( IC 50 = 26 nM ) . ^^^ These data suggest that the anxiolytic effects of CCK receptor antagonists parallel their affinity for the CCKB rather than the CCKA receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The aim of this study was to assess the role of cholecystokinin ( CCK ) A receptors in these changes using a CCK A antagonist loxiglumide . ^^^ CONCLUSIONS : CCK A receptors are involved in the induction of meal like fullness and nausea associated with intraduodenal lipid and gastric distention . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
For example , CCK appears to exert its anti opioid actions mainly through the activation of CCK B receptors , whereas its opioid like effects seem to result from the stimulation of CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK ( 1 nM 1 microM ) caused concentration dependent depolarisations when superfused over the nodose ganglion at 37 degrees C as measured by a silicone grease gap technique , and both CCKA antagonists caused significant rightward shifts in the concentration response curve to CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Expression of CCK A receptor mRNA in the pancreas , small intestine and brain were not detected in OLETF rats by the reverse transcriptase polymerase chain reaction . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We assessed the duration of the anti cholecystokinin ( CCK ) action of FK 480 , a new non peptide CCK A receptor antagonist developed in Japan , in an in vivo study in rats , comparing it with CR 1505 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK XLR shares approximately 50 % homology at the amino acid level with both the human CCK BR and the peripheral CCK A receptor subtypes . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Two types of receptors have been cloned , CCK A and CCK B / gastrin . ^^^ We have examined the occurrence of CCK A and CCK B receptor mRNA in the brain , digestive tract , pancreas , and kidney of the rat and man by Northern blot and reverse transcribed polymerase chain reaction ( RT PCR ) . ^^^ Northern blot and a PCR technique based on Taq polymerase antibody interaction and using CCK A and CCK B receptor specific primers , followed by Southern blot analysis , were the methods used . ^^^ RESULTS : By means of Northern blots , CCK A receptor mRNA was detected in rat fundus mucosa and pancreas but not in the remaining GI tract or brain . ^^^ By means of RT PCR , CCK A receptor mRNA was demonstrated in the brain and the mucosa of the fundus , antrum , duodenum , and colon , kidney , pancreas and pancreatic islets . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
TP 680 showed approximately 2 and 22 times greater selectivity for peripheral CCKA receptors relative to brain CCK ( CCKB ) receptors than MK 329 and loxiglumide , respectively , when IC 50 values for inhibition of [ 125I ] CCK 8 binding in isolated acini and cerebral cortex were compared . 3 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Several roles of CCKA and CCKB receptor subtypes in CCK 8 induced and LiCl induced taste aversion conditioning . ^^^ Because CCK 8 has affinity for both CCKA and CCKB receptor subtypes , we wanted to determine the subtype involved in CCK 8 induced TAC . ^^^ Pretreatment with the selective CCKA antagonist MK 329 ( L 364 , 718 or devazepide ) , at doses of 0 . 1 , 1 . 0 , or 10 . 0 mumol / kg , markedly antagonized ( > 70 % ) CCK 8 induced TAC . ^^^ Considering the existing data on the induction of TAC by various CCK analogues , we consider an action of CCK 8 on peripheral CCKA , but not CCKB , receptors necessary for the induction of TAC . ^^^ Our results of partial antagonism of CCK 8 and LiCl induced TAC by L 365 , 260 , CI 988 , or MK 329 suggest , but do not prove , that both CCKA and CCKB mechanisms may be operative during TAC . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These compounds displayed micromolar affinities for CCK B rather than CCK A receptor and the obtained results confirm that the 4 ( 3H ) quinazolinone nucleous represent a useful template for the development of selective CCK B receptor ligands . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These compounds displayed micromolar affinities for CCK A rather than CCK B receptor and the results have been discussed on the basis of a molecular modelling study . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCKB antagonist PD 135158 reduced the CCK effects in 10 of 14 cells ; the CCKA antagonist KL 1001 reduced the CCK effects in 17 of 36 cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Role of cholecystokinin ( CCK ) A receptor for pancreatic growth after weaning : a study in a new rat model without gene expression of the CCK A receptor . ^^^ The CCK A receptor is known to be involved in regulating pancreatic exocrine function and growth . ^^^ These results suggest that the CCK A receptor plays some role in the increase in cell size associated with normal growth of the pancreas from 5 to 25 weeks of age ( after weaning ) . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) is co localized with dopamine ( DA ) in portions of the mesolimbic system , where it may facilitate the function of DA through the CCKA receptor subtype . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To test whether the mechanism involved is dependent upon action at type A or type B CCK receptors , we examined the ability of CCKA ( devazepide ) and CCKB ( L 365 , 260 ) receptor antagonists to attenuate the suppression of sham feeding by intraintestinal oleic acid , maltotriose , or L phenylalanine . ^^^ Suppression by oleic acid or maltotriose was dose dependently attenuated by intraperitoneal administration of the CCKA receptor antagonist , as was suppression by exogenous CCK . ^^^ These results suggest that suppression of sham feeding by intestinally infused oleic acid and maltotriose is mediated by endogenous CCK acting at CCKA receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In conclusion , it is considerable that postprandial CCK induced gallbladder contractions are controlled through CCK A receptors both on the vagal nerve in stimulating endogenous release of acetylcholine and on the gallbladder directly to stimulate muscle contraction in the dog . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
L 364 , 718 ( a CCK A antagonist ) showed a relative selectivity and a high affinity for those receptors located in central tissues , whereas L 365 , 260 ( a CCK B antagonist ) is almost inactive in all studied tissues . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The actions of all CCK analogues were abolished by L 364 , 718 , indicating mediation by CCK A receptors . ^^^ Therefore , depending on the agonists used , CCK A receptor activation in pancreatic acini may result in differential involvement of second messenger systems , Ca2+ signal transduction , and amylase secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
RNA were extracted for CCK A and CCK B receptor expression using specific cRNA probes . ^^^ Results indicate that pig pancreatic acini are sensitive to Cch and relatively insensitive to caerulein with no response to JMV 180 , a CCKA agonist , or secretin ; MK 329 , a CCK A receptor antagonist , significantly inhibited caerulein induced enzyme secretion from 10 ( 8 ) M . ^^^ The pig pancreas expresses few CCK A mRNA receptors but a majority of CCK B . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCKB receptor preferring agonists gastrin 17 1 , desulfated CCK 8 and CCK 4 had only small stimulatory effects ( < 12 % of maximal CCK 8 effect , EC 50 ' s in the low nanomolar range ) and did not inhibit the CCK 8 response , suggesting that they were acting at CCKB but not , as partial agonists , at CCKA receptors . ^^^ These results suggest that CCK effects on [ Ca2+ ] 1 of porcine chief cells are mainly ( > 80 % ) mediated via CCKA receptors , which differ from guinea pig and rabbit chief cell receptors by a higher distinction capacity between selective CCKA and CCKB , receptor agonists ( A 71378 versus A 72962 ) and antagonists ( L364 . 718 versus L365 . 260 ) and by the apparent lack of activation by desulfated CCK 8 and gastrin 17 1 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Tests were undertaken in 10 DU patients without or with elimination of the action of endogenous CCK using loxiglumide ( LOX ) , a selective CCK A receptor antagonist , before and 4 wk . after eradication of Hp with triple therapy ( omeprazole , amoxycillin and bismuth ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The 2 gastrointestinal peptides cholecystokinin ( CCK ) and gastrin , which act through CCK A receptors ( having high affinity for CCK ) or CCK B / gastrin receptors ( having high affinity for CCK and gastrin ) , are considered to be important tumor growth factors . ^^^ We have evaluated CCK A and CCK B / gastrin receptors in 34 human thyroid cancers using in vitro receptor autoradiography with 2 different radioligands . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It is possible that this effect of EB is due to upregulation of CCKA receptors in the terminals of vagal afferent fibers because these receptors have been implicated in the mediation of the satiating effect of intraperitoneally injected CCK 8 . ^^^ As additional measures of EB ' s effects on CCK receptors , we also characterized EB ' s effects on CCK . 8 binding in the area postrema ( AP ) , a brain region rich in CCKA receptors , the ventromedial hypothalamus ( VMH ) , a region rich in CCKB receptors , and in the pancreas , a gland rich in CCKA receptors . ^^^ Furthermore , competition experiments with 500 nM of the selective CCKA receptor antagonist devazepide or the selective CCKB antagonist L 365 , 260 demonstrated that EB failed to affect CCK receptor subtype number in the medial and lateral divisions of the NTS . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results demonstrate that endogenous and exogenous CCK delays gastric emptying of liquids through stimulation of CCKA receptors and suggest that adaptation of the gastric motor response to CCK does not occur . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The aim of the present experiment was to study the effects on the rat liver and biliary tract of long term stimulation of CCK 8S and the CCK A receptor antagonist devazepide , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We have shown that Otsuka Long Evans Tokushima Fatty ( OLETF ) rats show little or no expression of the CCK A receptor gene in the pancreas . ^^^ We examined whether the CCK A and CCK B receptor genes are expressed in the islets and the role of CCK A receptor in insulin secretion . ^^^ CCK A receptor mRNA was detected in the islets of LETO rats but not OLETF rats . ^^^ These results suggest that the occurrence of pancreatic endocrine dysfunction in OLETF rats may be due to a defect in expression of the CCK A receptor gene , not to insulin deficiency . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Moreover , the levels of expression of CCK A and B receptor genes in the small intestine were examined . ^^^ CCK A receptor mRNA was not expressed in the small intestine of OLETF rats but was in LETO rats . ^^^ The pancreatic responses to various stimuli in OLETF rats were well conserved except for the involvement of CCK A receptor function . ^^^ OLETF rats are confirmed as a new experimental model deficient in CCK A receptor gene expression and represent a useful tool for studying the physiological role of these in vivo . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We therefore studied the effect of the CCK A receptor antagonist loxiglumide on gastric emptying of a high caloric solid liquid meal in humans . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine the role of GABAergic neurotransmission in cholecystokinin octapeptide ( CCK 8 ) induced contraction of the guinea pig ileal longitudinal muscle myenteric plexus preparation , CCKA or CCKB receptors were protected by L 364 , 718 and L 365 , 260 , respectively . ^^^ CCKA receptor protection alone decreased contractile responses to CCK 8 , and additional protection of GABAA receptors resulted in restoration of the contractile responses at high concentrations of CCK 8 . ^^^ The results suggest that the CCKA and CCKB receptors that mediate the contractile action of CCK differ with regard to GABAergic neurotransmission . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
AIMS : The effect of two recently developed CCK receptor antagonists , namely dexloxiglumide and spiroglumide , on gastric emptying and secretion as well as their selectivity towards CCKA and CCKB receptors in vivo was studied in the rat . ^^^ RESULTS : The putative CCKA antagonist , dexloxiglumide , administered by intravenous route , was able to inhibit CCK 8 induced delay of gastric emptying in a dose dependent fashion , with an ID 50 ( 95 % CL ) of 1 . 14 ( 0 . 84 1 . 53 ) mg / kg . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Moreover , both CCKA and CCKB receptor mechanisms have been implicated in CCK ' s effects on feeding . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It is suggested that the decreased exploration in OLETF rats may be due to the lack of CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The binding of labeled CCK 8 was markedly inhibited by CCK 8 and CCK A receptor antagonists , but it was only weakly affected by gastrin and CCK B receptor antagonists . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Evaluation of cholecystokinin , gastrin , CCK A receptor , and CCK B / gastrin receptor gene expressions in gastric cancer . ^^^ In this study , reverse transcription polymerase chain reaction ( RT PCR ) was used to evaluate messenger RNA expression for CCK , gastrin , CCK A receptor , and CCK B / gastrin receptor in surgical specimens of gastric cancers and in normal antrum and body mucosa of the stomach . ^^^ The CCK A receptor mRNA expression was detectable in 5 / 14 ( 36 % ) samples of gastric cancer and in 7 / 12 ( 58 % ) body mucosa . ^^^ Three cases out of 14 ( 21 % ) of gastric cancer expressed both CCK gene and CCK A receptor gene . ^^^ These findings may suggest a greater role for CCK and CCK A receptor than for gastrin and CCK B receptor in gastric cancers . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In contrast , L 364 , 718 , a CCK A antagonist in mammals , shows this effect only at very high dose levels . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine whether this behavior was intrinsic to a single receptor protein we studied the binding affinity of CHO cells stably transfected with a cloned rat CCKA receptor . 125I CCK binding to intact cells at 37 degrees C revealed two affinity states for CCK of Kd values 20 pM and 2 . 4 nM . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
By mapping the distribution of cholecystokinin ( CCK ) receptor types onto an established phylogenetic hypothesis of vertebrate relationships , we tested two hypothesis about the evolution of CCK receptors : ( 1 ) A single CCK receptor type , CCK 10 , is the ancestral receptor , while CCK A and CCK B receptors represent derived receptor types ; ( 2 ) the evolution of two separate CCK receptors is functionally related to the evolution of endothermy . ^^^ Additional competitive inhibition studies showed that the mako CCK 10 receptor has very low affinities for the following nonpeptide agonist and antagonists : A 71623 , L 364 , 718 , A 57696 , A65186 . 72 , Cam 1481 , and SR 27897B ( specific for some mammalian CCK A receptors ) and L 365 , 260 and CI 988 ( specific for some mammalian CCK B receptors ) , confirming the pharmacological differences between the CCK 10 receptor and the CCK A and B receptors . ^^^ CCK A and CCK B , are not part of the suite of characters necessary for evolution of endothermy in fishes . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Suppression of SKF 38393 induced grooming and vacuous chewing movements by CCK 8S was blocked by the selective CCKA receptor antagonist MK 329 ( also known as devazepide or L 364 , 718 ) ( 0 . 1 , 0 . 3 mg / kg i . p . ) but unaffected by the CCKB receptor antagonist L 365 , 260 ( 0 . 1 , 0 . 3 mg / kg i . p . ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The preparation of the dehydropeptides ( 1 , R = Me ; 2 , R = H ) and the cyclopropylpeptides ( 3 , R = Me ; 4 , R = H ) possessing good binding affinities for the CCK A and CCK B receptors is described . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Binding of 125I BH CCK 8 to the pancreas was inhibited by agonists with the affinities ( dissociation constant ) of CCK ( 0 . 11 nmol / L ) approximately gastrin ( 0 . 15 nmol / L ) and by antagonists with the affinities of CCK B receptor antagonist ( L 365 , 260 , 0 . 18 nmol / L ) > CCK A receptor antagonist ( lorglumide , 8 . 1 nmol / L ) . ^^^ The human pancreas predominantly expresses CCK B receptors , whereas only CCK A receptors were localized in the human gallbladder muscle . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The specific CCK A and secretin receptors expressed in normal pancreata were markedly reduced in pancreatic preneoplastic lesions and absent in adenocarcinomas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The antagonist ( 1 microM ) for CCK B receptor , but not CCK A receptor , significantly inhibited the number of GH 3 cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that CCK 8 activates at least two different channels , a Ca ( 2+ ) dependent Cl channel and a non selective cation channel in oocytes expressing the CCKA receptor , while the CCKB receptor elicits only a Ca ( 2+ ) dependent Cl channel . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCKA binding profile as shown in competition studies by using different CCK related compounds and non peptide CCK antagonists discriminating between CCKA and CCKB sites . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The application of modern molecular biological techniques has identified two CCK receptors , CCK A receptor ( CCKAR ) and CCK B / gastrin receptor ( CCKBR ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Soybean lectin stimulates pancreatic exocrine secretion via CCK A receptors in rats . ^^^ Plasma CCK concentrations rose significantly from 6 . 6 + / 1 . 9 to 14 . 3 + / 2 . 9 pmol / l , and the pancreatic response was abolished by CCK A receptor blockade ( 0 . 0 + / 0 . 1 mg / h ) . ^^^ The lectin releases CCK and the effect is mediated by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The overlapping distribution of opioid and cholecystokinin ( CCK ) peptides and their receptors ( mu and delta opioid receptors ; CCK A and CCK B receptors ) in the central nervous system have led to a large number of studies aimed at clarifying the functional relationships between these two neuropeptides . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A variety of experimental evidence suggests that exogenously applied CCK , acting at the CCKA receptor , potentiates the function of DA in the NAC . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The in vivo pharmacological effects of the newly developed serine derivative [ ( R ) 1 [ 3 ( 3 carboxypyridine 2 yl ) thio 2 ( indol 2 yl ) carbonylamino ] propionyl 4 diphenyl methyl piperazine ] ( TP 680 ) , a cholecystokinin type A ( CCK A ) receptor antagonist , on pancreatic , biliary and gastric function were examined in rats and mice . ^^^ Moreover , specificity for CCK A receptor was also demonstrated by the inability of TP 680 to antagonize pentagastrin stimulated gastric acid secretion . ^^^ These results indicate that TP 680 is a potent , competitive and specific CCK A receptor antagonist with long duration of action . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Therefore , we studied the possible presence of alterations also in the parotid glands during TPN , after PBD and during infusion of sulfated cholecystokinin ( CCK 8S ) and the CCK A receptor antagonist devazepide , respectively . ^^^ The CCK A receptor antagonist devazepide induced a reduction in protein and DNA contents in the pancreas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Role of the cholecystokinin ( CCK ) A receptor in pancreatic growth in rats during the suckling period : a study in a naturally occurring CCK A receptor gene `` knockout ' ' rat . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We used the type A cholecystokinin receptor ( CCK AR ) antagonist devazepide to assess the importance of CCK in mediating the anorexia produced by 2 h duodenal infusions of glucose ( 9 . 2 , 11 . 0 , and 18 . 3 mmol . kg 1 . h 1 ) and the glucose dimer maltose ( 4 . 5 , 6 . 7 , and 8 . 5 mmol . kg 1 . h 1 ) at the start of the dark period in nonfasted rats with free access to food . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist devazepide reduced the activation of GVAD induced by bombesin from 107 + / 11 to 63 + / 6 % , while abolishing the CCK response . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A and CCK B like receptors in the gallbladder and stomach of the alligator ( Alligator mississippiensis ) . ^^^ Alligator gallbladder smooth muscle expresses a CCK A receptor subtype , and stomach oxyntic mucosa expresses a distinct receptor subtype , termed CCK B / X because of its similarities to both CCK B and CCK 10 receptors . ^^^ Both the gallbladder and the stomach binding sites have very low affinities for a panel of nonpeptide receptor agonists and antagonists that are selective for mammalian CCK A and CCK B receptors . ^^^ These results suggest that CCK receptor subtypes diverged from the ancestral CCK 10 receptor in an early amniote , prior to the divergence of mammals and reptiles in vertebrate phylogeny , and that CCK A receptors may have evolved before CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The response to 100 pmol CCK was completely abolished by devazepide ( 0 . 5 mg kg 1 ) and by chronic subdiaphragmatic vagotomy performed 10 14 days prior to experimentation , indicating that CCK sensitivity was via CCKA receptors and exclusively mediated via vagal afferents rather than splanchnic or enteric afferents . 4 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
For maximal reduction of endogenous bile output the CCK A receptor antagonist loxiglumide was infused intravenously . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Competition binding by agonists and antagonists of CCKA and CCKB / gastrin receptors demonstrated the presence of two distinct binding components , sites presenting a high affinity for [ Thr , Nle ] CCK 9 , gastrin , PD 135158 , L 365 , 260 and a low affinity for MK 329 , SR 27897 , and sites presenting a high affinity for [ Thr , Nle ] CCK 9 , MK 329 , SR 27897 and a low affinity for gastrin , PD 135158 , L 365 , 260 . 5 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A meal disrupts migrating motor complexes ( MMC ) in the rat intestine through stimulation of peripheral cholecystokinin ( CCK ) B and central CCK A receptors . ^^^ This initiates a reflex including stimulation of central CCK A receptors . ^^^ Exogenous CCK also stimulates peripheral CCK A receptors not located in capsaicin sensitive vagal afferent fibers . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Direct contractile effect of cholecystokinin octapeptide on caecal circular smooth muscle cells of guinea pig via both CCK A and CCK B / gastrin receptors . ^^^ This study strongly suggested the presence of both CCK A and CCK B / gastrin receptors in caecal circular smooth muscle cells of guinea pig , and that the contractile effect of CCK 8 on these cells was mediated via both of these receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A region between residues 38 and 42 of the human cholecystokinin A ( CCK A ) receptor was shown to be involved in the binding of CCK but not in that of JMV 179 and JMV 180 , two peptides closely related to CCK ( Kennedy , K . , Escrieut , C . , Dufresne , M . , Clerc , P . , Vaysse , N . , and Fourmy , D . ( 1995 ) Biochem . ^^^ The modeling of the CCK A receptor and the docking of the peptide agonists [ Thr , Nle ] CCK 9 and CCK 8 indicated that their N terminus was connected to the receptor through a strong bond network involving Trp 39 and Gln 40 thus confirming experimental data . ^^^ These first molecular data identifying the agonist binding site of the human CCK A receptor represent an important step toward the complete delineation of the agonist binding site and the understanding of the molecular mechanisms that govern differential activation of this receptor by CCK related peptides . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These data therefore do not support the postulate that CCK acting via CCKA or CCKB receptors modulates release of GABA under the present experimental conditions . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The ethanol induced increase in amylase output can be completely inhibited by the CCK A receptor antagonist L 364 , 718 and partially inhibited by the muscarinic cholinergic antagonist atropine . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
However , the results obtained with specific CCK A ( peripheral ) receptor antagonists are still controversial . ^^^ The present studies were undertaken to evaluate the involvement of endogenous CCK and the CCK A receptors in the development of severe acute pancreatitis induced in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats that have a selective defect in the CCK A receptor . ^^^ These results suggest that endogenous CCK and CCK A receptors play a role in the development of severe acute pancreatitis in rats . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
From day 3 to day 10 of life , male and female Wistar rat pups were treated with the CCK A receptor antagonist L 364 . 718 and the CCK A + B agonist CCK 8S . 3 . ^^^ These data show that early postnatal treatment with the CCK A receptor antagonist L364 . 718 has an impact on the hypophagic response to CCK 8S in later life . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine the structural basis of CCK A receptor ( CCK AR ) functionally coupled to Gs , a series of chimeric mutants were constructed by replacing exons of human CCK B receptor ( CCK BR ) , from the second to the fifth ( last ) exon , with human CCK AR counterparts . ^^^ However , only the wild type CCK AR and chimeric mutants containing the second exon of CCK AR were able to mediate significantly greater increases in intracellular cAMP content and adenylyl cyclase activity compared with wild type CCK BR . ^^^ A CCK BR mutant was further constructed by replacing five amino acids , Gly Leu Ser Arg ( Arg ) Leu , in the first intracellular loop with the corresponding five CCK AR specific amino acids , Ile Arg Asn Lys ( Arg ) Met . ^^^ These data suggest that the first intracellular loop of CCK AR is essential for coupling to Gs and activation of adenylyl cyclase signal transduction cascade . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In adult rats , cholecystokinin ( CCK ) binds to pancreatic CCK A receptors and stimulates exocrine secretion and pancreatic growth . ^^^ In newborn rats there is very little mature intestinal CCK and few pancreatic CCK A receptors . ^^^ This suggests that enzyme release is probably mediated by the same receptors in both adults and neonates , and in adults previous work has shown this to be the CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pre treatment with intravenous MK 329 , benzodiazepine CCK A receptor antagonist , blocked the duodenal oleate effect on drug plasma levels in a single dog preliminary study . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The aim of the present study was to study the expression of CCK A and CCK B receptor mRNA after porta caval shunting . ^^^ Total RNA was isolated from pancreas and oxyntic mucosa for Northern blot analysis of CCK A and CCK B receptor mRNA . ^^^ Porta caval shunted rats displayed an increased CCK A receptor mRNA concentration in the pancreas ( after stimulation with CCK 8s ) and an increased CCK B receptor mRNA concentration in the oxyntic mucosa . ^^^ In conclusion , the porta caval shunting evoked enhancement of the trophic effect of CCK A receptor activation on the pancreas and of CCK B receptor activation on the ECL cells is associated with enhanced expression of CCK A receptor mRNA in the pancreas and of CCK B receptor mRNA in the oxyntic mucosa . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptors were expressed rarely in tumors except in gastroenteropancreatic tumors ( 38 % ) , meningiomas ( 30 % ) , and some neuroblastomas ( 19 % ) . ^^^ The identified CCK A and CCK B receptors were specific and of high affinity in the subnanomolar range . ^^^ The rank order of potency of various CCK analogues was : sulfated CCK 8 = L 364 , 718 > > nonsulfated CCK 8 = L 365 , 260 > or = gastrin for CCK A receptors and sulfated CCK 8 > gastrin = nonsulfated CCK 8 > L 365 , 260 > L 364 , 718 for CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present study examined roles of endogenous cholecystokinin ( CCK ) and CCK A receptors in the regulation of pancreatic exocrine secretion and gastroduodenal motility in conscious sheep during interdigestive period . ^^^ These results suggest that endogenous CCK contributes to the regulation of interdigestive pancreatic exocrine secretion , omasal contractions and duodenal MMC in the ovine gastrointestinal tract via CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
During the diluting period , inhibition of GB contractions by a CCKA receptor antagonist , atropine or hexamethonium , resulted in concentration of GB bile , whereas during the concentrating period , CCK 8 shifted the concentration process back to dilution . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
BACKGROUND & AIMS : Gastrin and cholecystokinin ( CCK ) are gut brain peptides , with multiple functions in the gastrointestinal tract mediated through CCK B gastrin and CCK A receptors . ^^^ The aim of this study was to investigate the distribution and pharmacological characteristics of CCK A and CCK B receptors in the human upper gastrointestinal tract and compare them with those in the rat and dog . ^^^ CCK A receptors were found in the basal region of the antral and fundic mucosa . ^^^ CCK A receptors were also located in the muscularis propria of antrum , fundus , and gallbladder , whereas CCK B gastrin receptors were only detected in gastric fundic circular muscle . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The mouse cholecystokinin type A receptor ( CCK ( A ) R ) gene was cloned and sequenced , and the exon / intron boundaries were determined by cDNA cloning . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin induced antinociception is not blocked by CCK A or CCK B receptor antagonists . ^^^ To determine the relative importance of CCK A , CCK B , and opioid receptors in mediating the antinociceptive actions of cholecystokinin , we evaluated the actions of selective agonists and antagonists in the mouse hot plate assay . ^^^ The agonists used were CCK ( 1 30 nmol i . c . v . ) , a CCK A receptor agonist ( SNF 9019 ; 0 . 3 10 nmol i . c . v . ) , and a CCK B receptor agonist ( SNF 9007 ; 0 . 3 10 nmol i . c . v . ) . ^^^ The antagonists used were the CCK A receptor antagonist , L 364 , 718 ( 12 . 5 nmol i . c . v . ) , CCK B receptor antagonist , L 365 , 260 ( 2 . 5 25 nmol i . c . v . ) , and the nonselective opioid receptor antagonist naloxone ( 1 mg / kg s . c . ) . ^^^ We conclude that centrally administered CCK produces antinociception in the mouse hot plate assay via opioid receptors , but independent of CCK A or CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Gastric emptying in OLETF rats not expressing CCK A receptor gene . ^^^ We have very recently demonstrated the low acidity of gastric juice and the high susceptibility to the development of gastric ulceration in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats not expressing CCK A receptors . ^^^ We also confirmed with this mutant that CCK delays gastric emptying through the CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Systemic pretreatment with the CCKB antagonist , L 365 , 260 , but not with the CCKA antagonist , L 364 , 718 , significantly antagonised the effect of CCK 8S on cortical dynorphin B and aspartate release . ^^^ Thus , the present results indicate that cortical CCK release exerts a stimulatory modulation on cortical dynorphin B and aspartate release via the CCKB receptor subtype , and on glutamate release via both CCKA and CCKB receptor subtypes . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the second set of experiments , the effect of cholecystokinin ( CCK ) CCKA and CCKB receptor antagonists , devazepide and L 365260 , on citalopram induced decrease of exploratory behaviour in the elevated plus maze was studied . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Unstimulated CCK receptors remained on the surface of both recombinant stable rat CCK A receptor bearing Chinese hamster ovary cell line ( CHO CCKR ) cells and native rat pancreatic acinar cells and did not constitutively internalize . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCKA receptor on pancreatic acini has a greater affinity for sulfated CCK than for gastrin , while the gastrin / CCKB receptor in gastric mucosa and brain has similar affinities for both gastrin and CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The level of CCK mRNA and CCK concentration in the small intestinal mucosa , and the level of CCK A receptor mRNA in the pancreas were examined . ^^^ The CCK A receptor mRNA level also increased with age in LETO rats . ^^^ It is suggested that the long term defect of CCK A receptor may decrease CCK release and transcription . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
IQM 95 , 333 displaced [ 3H ] CCK 8S binding to CCKA receptors from rat pancreas with a high potency in the nanomolar range . ^^^ Like devazepide , IQM 95 , 333 was a more potent antagonist of CCK 8S than of CCK 4 induced contraction of the longitudinal muscle from guinea pig ileum , suggesting selective antagonism at CCKA receptors . 4 . ^^^ IQM 95 , 333 and devazepide were also potent inhibitors of CCK 8S stimulated amylase release from isolated pancreatic acini , a CCKA receptor mediated effect . ^^^ Low doses ( 50 100 micrograms kg 1 , i . p . ) of IQM 95 , 333 and devazepide , without any intrinsic effect on food intake or locomotion , blocked the hypophagia and the hypolocomotion induced by systemic administration of CCK 8S , two effects associated with stimulation of peripheral CCKA receptors . 6 . ^^^ In conclusion , IQM 95 , 333 is a potent and selective CCKA receptor antagonist both in vitro and in vivo with an anxiolytic like activity in two different animal models , which can only be attributed to blockade of this CCK receptor subtype . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Retardation of pancreatic regeneration after partial pancreatectomy in a strain of rats without CCK A receptor gene expression . ^^^ In conclusion , the CCK A receptor is not an absolute requirement for pancreatic normal growth but is important for pancreatic regeneration . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Because in the initial report of naloxone ' s potentiation of CCK a relatively high , nonphysiologic dose of CCK ( i . e . , 13 micrograms / kg ) was used as the training drug , in the current analysis subjects were trained to discriminate 5 . 6 micrograms / kg CCK from its vehicle and the assessments and comparisons of the effects of naloxone and naltrindole were based on this dose . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Fusion of the C terminus of the CCKAR to the N terminus of the GFP did not alter receptor ligand binding affinity , signal transduction , or the pattern of receptor surface expression and receptor mediated cholecystokinin ( CCK ) internalization . ^^^ Newly obtained biologically active fluorescent derivatives of CCK were used for simultaneous observation of receptor and ligand trafficking in CHO , NIH / 3T3 , and HeLa cells stably expressing the fluorescent CCKAR and in transiently transfected COS 1 cells . ^^^ The CCKAR antagonists , L 364 , 718 and CCK 27 32 amide potently inhibited spontaneous internalization of the receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A series of 2 aralkyl 4H pyridothiadiazine 1 , 1 dioxides and 3 aralkylamino 2 aryl 2H pyrido [ 4 , 3 e ] 1 , 2 , 4 thiadiazine 1 , 1 dioxides structurally related to quinazolinone CCK receptor antagonists were synthesized and evaluated as CCK A and CCK B receptor ligands . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
During distensions , saline , CCK ( 30 ng / kg / h ) or the CCK A receptor antagonist loxiglumide ( 10 mg / kg / h ) was perfused in a random double blind order . ^^^ CONCLUSIONS : In humans , CCK A receptor subtype is involved in the occurrence of transient lower oesophageal sphincter relaxations induced by gastric distension . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Acetylcholine and CCK agonists ( the CCKA receptor agonists A 71378 and A 71623 ; the CCKB receptor agonist Suc CCK 4 ) were iontophoretically administered alone and in combination . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To investigate the role of the carboxyl terminus of cholecystokinin ( CCK ) receptors in receptor internalization , the rat wild type ( WT ) CCK A receptor ( WT CCKAR ) and the rat WT CCK B receptor ( WT CCKBR ) were truncated after amino acid residue 399 ( CCKAR Tr 399 ) and 408 ( CCKBR Tr 408 ) , thereby deleting the carboxyl terminal 45 and 44 residues , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of cholecystokinin ( CCK ) CCKA receptor antagonist devazepide ( 10 micrograms / kg and 1 . 0 mg / kg ) , CCKB receptor antagonist L 365260 ( 1 . 0 mg / kg ) , and CCKB receptor agonist CCK tetrapeptide ( CCK 4 , 75 micrograms / kg ) , and their concomitant administration with antidepressants desipramine ( 10 mg / kg ) and citalopram ( 10 mg / kg ) on rat exploratory behaviour were studied in the recently developed exploration box test . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
There are two CCK receptors ; both CCK A and CCK B receptors are stimulated by CCK 8 SE . ^^^ The relative importance of the CCK A and CCK B receptors in the somnogenic and hypothermic effects of CCK 8 SE is not well understood . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin depolarizes guinea pig sphincter of Oddi neurons by activating CCK A receptors . ^^^ CCK induced depolarization was significantly reduced by a CCK A , but not a CCK B , receptor antagonist . ^^^ It is concluded that CCK can act on CCK A receptors to depolarize SO neurons . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
While human CCK A and B receptors have been fully characterized , their relative roles in human pancreatic adenocarcinoma remain unclear . ^^^ Thus , expression of CCK A and B receptors in normal human pancreas , pancreatic adenocarcinomas , and other human extrapancreatic tissues and malignancies was examined , using reverse transcription followed by the polymerase chain reaction ( RT PCR ) . mRNA isolated from 15 normal pancreas specimens , 22 pancreatic adenocarcinomas , and 58 extrapancreatic tissues and tumors was subjected to RT PCR using primers specific for human CCK A and B receptors . ^^^ In contrast , CCK A receptors exhibited a more selective pattern of expression in gall bladder , intestine , brain , ovary , spleen , and thymus . ^^^ Of significance , CCK A receptors were expressed selectively in all pancreatic adenocarcinomas , but not in any normal pancreas specimens . ^^^ In situ hybridization , using receptor specific riboprobes , localized CCK A receptor expression to ductal cells , the presumed origin of most human pancreatic adenocarcinomas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A and CCK B antagonists , devazepide and L 365260 ( 100 micrograms / kg , i . p . ) , respectively , inhibited the postprandial colonic motor response while only L 365260 reduced the CCK induced stimulation . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present study investigated the effects of agonists of the neuropeptide cholecystokinin ( CCK ) on neostriatal neurons in order to confirm the existence of CCK A receptors in the rat caudate putamen . ^^^ The CCK A receptor agonists A 71378 ( desamino Tyr ( SO3H ) Nle Gly Trp Nle ( N methyl ) Asp Phe NH 2 ) , and A 71623 ( Boc Trp Lys ( epsilon N 2 methylphenylamino carbonyl ) Asp ( N methyl ) Phe NH 2 , as well as the CCK B receptor agonist Suc CCK 4 ( Suc Trp ( N methyl ) Nle Asp Phe NH 2 ) were iontophoretically administered with multibarrel capillaries . ^^^ About one third of the neurons responded to the CCK A receptor agonists . ^^^ The results suggest that in the rat neostriatum not only CCK B receptors , but also CCK A receptors seem to mediate the effects of cholecystokinin . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results indicate that CCK A type receptors rather than CCK B receptors may be involved in CCK induced insulin secretion in sheep . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To test the possible role of cholecystokinin ( CCK ) in the decrease of social exploration induced by intraperitoneal ( IP ) injection of lipopolysaccharide ( LPS , 100 microg / kg ) , mice were pretreated with IP or intracerebroventricular ( ICV ) injection of the CCKA receptor antagonist L 364 , 718 ( 3 mg / kg and 10 microg / kg , respectively ) and the CCKB receptor antagonist L 365 , 260 ( 1 mg / kg and 10 microg / kg , respectively ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
All subjects were studied twice , in a randomized , double blind study , during intravenous infusion of either loxiglumide ( CCK A antagonist ) or saline . ^^^ Endogenous CCK or CCK A receptors therefore play a role in the fat induced reduction of intragastric pressure and might also modulate gastric perception after lipid . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We investigated cell proliferation modulated by cholecystokinin ( CCK ) and somatostatin analogue RC 160 in CHO cells bearing endogenous CCKA receptors and stably transfected by human subtype sst 5 somatostatin receptor . ^^^ These effects are positively regulated by CCK and negatively influenced by RC 160 , interacting through CCKA and sst 5 receptors , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A antagonist loxiglumide at 20 mg / kg , a dose which abolished the action of all caerulein doses on food intake , failed to alter the food intake either in obese or in lean rats when given without an agonist . ^^^ However , the failure of the CCK A antagonist to increase food intake questions whether any of the effects of exogenous CCK are of physiological relevance . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Three experiments were performed in random order : intravenous infusion of 1 ) placebo , 2 ) low dose atropine ( 5 micrograms . kg . h 1 ) , and 3 ) the CCK A receptor antagonist loxiglumide ( 22 mumol . kg . h 1 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Full and partial agonist activity of C terminal cholecystokinin peptides at the cloned human CCK A receptor expressed in Chinese hamster ovary cells . ^^^ The agonist activities of the C terminal cholecystokinin peptides sulfated cholecystokinin octapeptide ( CCK 8S ) , non sulfated cholecystokinin octapeptide ( CCK 8NS ) , pentagastrin and CCK 4 at the cloned human CCK A receptor expressed in Chinese hamster ovary cells were evaluated in two functional assays of receptor activation . [ 125I ] CCK 8S displacement studies employing membranes derived from these cells revealed the expected rank order of affinity for a number of CCK receptor ligands . ^^^ Consistent with their lower affinities for CCK A receptors , CCK 8NS , pentagastrin and CCK 4 were weaker agonists in both functional assays . ^^^ These results demonstrate that CCK 8S represents the minimum ligand requirement for both high affinity and full agonist activity at the human CCK A receptor subtype . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Infusion of CCK A receptor mRNA antisense oligodeoxynucleotides inhibits lordosis behavior . ^^^ Neurons in the medial preoptic nucleus ( MPN ) express CCK A subtype receptor mRNA , and site specific infusions of CCK facilitate lordosis , suggesting that CCK A receptor activation positively modulates lordosis . ^^^ In the present study , we demonstrated CCK binding in the central portion of the MPN ( MPNc ) and the disruption of lordosis behavior by reducing the expression of CCK A receptors in this nucleus . ^^^ Antisense oligodeoxynucleotides ( ODN ) specific for CCK A receptor mRNA were infused into the MPN of ovariectomized female rats . ^^^ In vitro , AR42J pancreatic acinar carcinoma cells treated with antisense ODN had lower levels of CCK A and CCK B subtype receptor binding than nonsense ODN treated cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The selective CCK A receptor antagonist , devazepide , ( 0 . 03 3 . 0 mg / kg ) administered alone had no intrinsic effect on gastric emptying . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In AGS cells , gastrin / CCK B receptor antagonists inhibited the effect of G 17 and competitively antagonized 125I G 17 binding , whereas the CCK preferring ( CCK A ) receptor antagonists had no effect . ^^^ In contrast , CCK A receptor antagonists inhibited the stimulatory effect of G 17 in SIIA cells , whereas CCK B receptor antagonists had no effect . ^^^ Gly G stimulated the growth of AGS and SIIA cells ; neither the CCK B nor the CCK A receptor antagonists blocked this effect . ^^^ CONCLUSIONS : G 17 stimulates proliferation of AGS cells through the CCK B receptor ; however , G 17 mediated growth of SIIA acts through a CCK A like receptor . ^^^ Furthermore , Gly G stimulates growth of human gastric cancer cell lines , possibly through a receptor other than the CCK B or CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Leptin CCK action was blocked by systemic capsaicin at a dose inducing functional ablation of sensory afferent fibers and by devazepide , a CCK A receptor antagonist but not by the CCK B receptor antagonist , L 365 , 260 . ^^^ These results indicate the existence of a functional synergistic interaction between leptin and CCK leading to early suppression of food intake which involves CCK A receptors and capsaicin sensitive afferent fibers . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effects of a specific CCK A antagonist , Loxiglumide , on postprandial mood and sleepiness . ^^^ The aim of the study was to test the hypothesis that postprandial sleepiness is mediated by cholecystokinin ( CCK ) acting on CCK A receptors . ^^^ On one day they received an i . v . infusion of Loxiglumide , a CCK A receptor antagonist ( 30 mg / kg / h for 10 min then 10 mg / kg / h for 3 h 10 min ) . ^^^ In conclusion , the results suggest that the postprandial decline in feelings of alertness after a fat rich meal is not mediated solely by CCK acting through CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
High affinity CCK A receptors on the vagus nerve mediate CCK stimulated pancreatic secretion in rats . ^^^ The aim of this study was to identify the vagal CCK A receptor affinity state that mediates the effect of CCK on pancreatic protein secretion . ^^^ Infusion of CCK JMV 180 ( 22 88 micrograms . kg 1 . h 1 ) caused dose dependent increases in pancreatic protein secretion , which were blocked by the CCK A receptor antagonist L 364 , 718 . ^^^ To demonstrate that endogenously released CCK also acts on high affinity CCK A receptors , we showed that in conscious rats intraduodenal infusion of 18 % casein produced a threefold increase in protein secretion and elevated plasma CCK levels from 0 . 7 to 8 . 4 pM . ^^^ In conclusion , we demonstrated that in contrast to their effect on satiety , which is mediated by vagal low affinity CCK A receptors , exogenous CCK and endogenous CCK under physiological conditions act through high affinity CCK A receptors to mediate pancreatic protein secretion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of a synthetic putative luminal cholecystokinin ( CCK ) releasing factor ( LCRF ) fragment ( 1 35 ) on pancreatic exocrine secretion were examined in conscious Wistar rats and a mutant strain of rats lacking the CCK A receptor . ^^^ No significant effect was observed in rats lacking the CCK A receptor . ^^^ The synthetic LCRF fragment stimulated pancreatic secretion via CCK A receptors in conscious rats . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
One half of the hamsters fed a high fat diet received the CCK A receptor antagonist devazepide ( 25 nmol / kg / hr ) for the duration of the experiment . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
When tested by radioreceptor assay , a synthetic replicate of alligator gastrin 49 exhibited a gastrin like pattern of biological activity on mammalian CCK A and CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Peripheral administration of cholecystokinin activates c fos expression in the locus coeruleus / subcoeruleus nucleus , dorsal vagal complex and paraventricular nucleus via capsaicin sensitive vagal afferents and CCK A receptors in the rat . ^^^ Pretreatment with the CCK A receptor antagonist MK 329 ( devazepide ; 1 mg / kg and 2 mg / kg i . p . ) reduced the CCK induced increase in c fos expression in the LC / SC by 54 % and 75 % , respectively ; the CCK B receptor antagonist L 365 , 260 had no effect . ^^^ In comparison , the CCK A antagonist devazepide ( 1 mg / kg and 2 mg / kg i . p . ) reduced the increase in c fos expression by 76 % and 88 % in the PVN , 69 % and 88 % in the NTS , 86 % and 83 % , respectively , in the AP . ^^^ The data indicate that CCK 8S i . p . induces modulation of neuronal activity in the LC / SC , DVC and PVN predominantly by peripheral action of CCK A receptors and capsaicin sensitive vagal afferents . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist MK 329 abolished the pancreatic secretory response to intraduodenally infused LCRF ( 1 35 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Stimulation of both CCK A and CCK B receptors activates MAP kinases in AR42J and receptor transfected CHO cells . ^^^ The present study evaluates whether one or both types of CCK receptors are capable of MAPK activation in pancreatic AR42J acinar cells as well as CHO cells transfected with CCK A or CCK B receptors . ^^^ The CCK B receptor antagonist L 365 , 260 almost totally blocked MAPK activation in AR42J cells after stimulation with gastrin and glycine extended gastrin and substantially reduced the activation of both kinases by CCK 8 , while the CCK A receptor antagonist L 364 , 718 was much less effective . ^^^ The CCK A selective agonist A 71376 , however , was an effective stimulant of MAPK activity . ^^^ In an alternative approach , stably transfected CHO cells bearing either CCK A or CCK B receptors were stimulated with CCK 8 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK 8S induced Ca increases were blocked by the CCKB receptor antagonist PD 135158 ( 100 nM ) but not by the CCKA antagonist lorglumide ( 100 nM ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These behavioural effects , prevented by the prior i . p . administration of the CCK B antagonist L 365 , 260 but not by the CCK A antagonist L 364 , 718 , were shown to depend on dopaminergic systems , since they were blocked by D 1 ( SCH 23390 , 25 microg / kg i . p . ) or D 2 ( sulpiride , 50 or 100 mg / kg i . p . ) antagonists . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
METHODS : The effect of the CCK A antagonist loxiglumide ( LOX ) on GE and motility was studied using magnetic resonance imaging in six healthy volunteers after ingestion of 500 ml Intralipid 10 % ( 550 kcal ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effect of a new CCK A receptor antagonist , dexloxiglumide , on the exocrine pancreas in the rat . ^^^ These results demonstrate the ability of dexloxiglumide to antagonize the effects of CCK on pancreatic secretion and growth , suggesting that this compound is a potent and selective antagonist of CCK A receptors in the pancreas . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist MK 329 ( 0 . 1 mg / kg i . p . ) diminished the FLI increase in LC , NTS , AP , and PVN by 39 100 % ; the CCK B receptor antagonist L 365 , 260 reduced the increased FLI in the AP by 54 % . ^^^ These findings suggest that entry of lipid into the intestine activates c fos in the LCC , NTS , and PVN predominantly via CCK A receptors on vagal afferents and in the AP via vagal and nonvagal pathways , as well as CCK B and CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
METHODS : Thirty day old male rats were pairfed for 10 days with lactalbumin as a control diet or lactalbumin plus PHA or purified soybean trypsin inhibitor ( STI ) as a positive control ( 42 mg / rat / day ) with or without 20 micrograms of the cholecystokinin A ( CCK A ) antagonist MK 329 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Differential expression of the CCK A and CCK B / gastrin receptor genes in human cancers of the esophagus , stomach and colon . ^^^ We have measured the levels of mRNA for CCK A and CCK B / gastrin receptors using quantitative reverse transcription polymerase chain reaction ( RT PCR ) in primary digestive cancers and hepatic metastases . ^^^ CCK A receptor mRNA was detected in 5 out of 8 esophageal cancers ( 0 . 1 1 fg / microg ) , in 5 out of 8 gastric cancers ( 0 . 05 4 . 2 fg / microg ) and in 5 out of 12 colon cancers ( 0 . 1 1 fg / microg RNA ) . ^^^ The expression of the CCK A receptor in esophageal , gastric and colon cancers and of the CCK B / gastrin receptor in the majority of gastric adenocarcinomas screened may be an important indicator of the influence of CCK and gastrin of local or systemic origin on the growth of these cancers . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Synthesis and biological evaluation of potent , selective , hexapeptide CCK A agonist anorectic agents . ^^^ Cholecystokinin ( CCK ) is a 33 amino acid peptide with multiple functions in both the central nervous system ( via CCK B receptors ) and the periphery ( via CCK A receptors ) . ^^^ Inversion of the chirality of Asp 7 in conjunction with N methylation of Phe 8 produces compound 5 which exhibits high affinity and 2100 fold selectivity for CCK A receptors . ^^^ Compound 6 ( Hpa ( SO3H ) Nle Gly Trp Nle MeAsp Phe NH 2 ) , derived from moving the N methyl group from Phe to Asp , decreased CCK B affinity substantially without affecting CCK A affinity , giving a compound with 6600 fold selectivity for CCK A receptors . ^^^ Compound 6 produces potent anorectic activity via the CCK A receptor system . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
At birth lambs received an injection of the CCK A antagonist devazepide ( 0 . 01 or 0 . 1 mg / kg ) , the CCK B antagonist PD 135158 ( 0 . 01 or 0 . 1 mg / kg ) , or saline for the controls ( 1 ml / kg ) . ^^^ The use of a CCK A antagonist , but not a CCK B antagonist , was concluded to prevent the formation of a preferential relationship between the lamb and its mother , most probably by impairing neonatal learning . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The increase in hepatic vagal activity produced by CCK 8 was significantly reduced by i . v . administration of 200 micrograms / kg of the CCKA receptor antagonist devazepide . ^^^ These outcomes demonstrate that activation of CCKA receptors by CCK 8 increases hepatic vagal afferent activity and support the view that the duodenal satiety action of CCK is mediated by the hepatic branch . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) regulates somatostatin secretion through both the CCK A and CCK B / gastrin receptors in sheep . 1 . ^^^ The objectives of the present study were to compare the in vivo potencies of the sulphated ( s ) and non sulphated ( ns ) forms of gastrin heptadecapeptide ( G 17 ) and CCK octapeptide ( CCK 8 ) on SOM secretion , and to determine the nature of the receptors involved by repeating the studies in the presence of the CCK A and CCK B / gastrin receptor antagonists L 364 , 718 and L 365 , 260 , respectively . ^^^ Both the CCK A and CCK B / gastrin receptor antagonists suppressed CCK 8s stimulated SOM output . ^^^ Despite sharing a common biologically active carboxy terminus , CCK stimulates SOM secretion by both the CCK A and CCK B / gastrin receptors , while gastrin acts via the CCK B / gastrin receptor alone . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Receptor gene expression for the CCK B / gastrin receptor , but not for the CCK A receptor , was found by reverse transcription polymerase chain reaction . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In this report , we show that the intraperitoneal administration of a CCK B receptor antagonist , PD 135158 ( 0 . 1 mg / kg ) , but not a CCK A receptor antagonist , lorglumide , inhibited hyperlocomotion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We examined the cholecystokinin ( CCK ) B / gastrin receptor , H+ / K+ ATPase and somatostatin gene expression , the histology and immunohistochemistry of gastrin and somatostatin of the stomach , plasma gastrin levels , and gastric acid secretion in naturally occurring CCK A receptor gene knockout ( Otsuka Long Evans Tokushima fatty , OLETF ) rats . ^^^ The overexpression of CCK B / gastrin receptor mRNA and the hyperfunction of parietal cells were observed in rats without CCK A receptor gene expression . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCKA and CCKB receptor subtypes both mediate the effects of CCK 8 on myenteric neurons in the guinea pig ileum . ^^^ In 5 of these neurons , application of the CCKA antagonist L 364 , 718 ( 100 500 nM ) antagonized the action of CCK 8 and the CCKB antagonist L 365 , 260 ( 500 nM ) had no effect . ^^^ The results demonstrate that the excitatory effects of CCK 8 are mediated by both CCKA and CCKB receptor subtypes . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Six healthy male volunteers were studied in random order on five occasions using : ( a ) IVAA , ( b ) loxiglumide ( CR 1505 , a selective CCK A receptor antagonist ) , ( c ) IVAA plus loxiglumide , ( d ) atropine and ( e ) IVAA plus atropine . ^^^ CONCLUSION : In healthy volunteers intravenous infusion of high doses of amino acids results in a significant gallbladder contraction , which is inhibited by CCK A receptor blockade and by atropine . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
All the compounds were evaluated in vitro towards both CCK B and CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Role of cholecystokinin A ( CCK A ) receptor in pancreatic regeneration after pancreatic duct occlusion : a study in rats lacking CCK A receptor gene expression . ^^^ We examined the role of the cholecystokinin A ( CCK A ) receptor in acute inflammatory and regenerative stages of experimental pancreatitis using a rat model lacking the CCK A receptor [ Otsuka Long Evans Tokushima Fatty ( OLETF ) rats ] . ^^^ Histological examination was performed , and changes in pancreatic wet weight , protein concentration , CCK A and B receptor mRNA levels , tyrosine kinase activities , and plasma amylase and CCK levels were determined . ^^^ These observations indicate that the absence of the CCK A receptor did not modify the acute phase of pancreatitis but significantly retarded regeneration of the pancreatic tissue . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pretreatment with either the CCKA receptor antagonist devazepide or the CCK ( B ) receptor antagonist L 365 , 260 significantly attenuated this effect over a range of doses ( 20 , 100 , 500 microg / kg i . p . ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of loxiglumide ( CAS 107097 80 3 , CR 1505 ) , a novel cholecystokinin A ( CCK A ) receptor antagonist , on pancreatic exocrine secretion stimulated by exogenously administered CCK 8 were examined in conscious dogs with chronic pancreatic fistula . ^^^ These results demonstrated that the selective CCK A antagonist loxiglumide inhibited the increase of pancreatic exocrine secretion stimulated by CCK 8 based on selective blockade of receptor binding of CCK in dogs . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Otsuka Long Evans Tokushima Fatty ( OLETF ) rats develop obesity , hyperglycemia , and non insulin dependent diabetes mellitus and do not express cholecystokinin A ( CCK A ) receptors , the receptor subtype mediating the satiety actions of CCK . ^^^ Together , these data are consistent with the interpretation that the lack of CCK A receptors in OLETF rats results in a satiety deficit leading to increases in meal size , overall hyperphagia , and obesity . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To compare the roles of CCK receptors , the effects of the CCK A receptor agonist A 71378 , the CCK A / B receptor agonist CCK 8S and the CCK B receptor agonist BOC CCK 4 on anxiety related behavior and the 5 HT release in the prefrontal cortex were determined . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Furthermore , we emphasize the important physiologic roles of CCK and CCK receptors by the discovery of disrupted CCK A receptor gene in rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of loxiglumide ( CAS 107097 80 3 , CR 1505 ) , a novel cholecystokinin A ( CCK A ) receptor antagonist , on pancreatic exocrine secretion stimulated by meal were examined in conscious dogs with chronic pancreatic fistula . ^^^ These results show that the selective CCK A antagonist loxiglumide may inhibit the increase of pancreatic exocrine secretion based on selective blockade of receptor binding of CCK endogenously induced by meal in dogs . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Radioligand displacement assay was performed to characterize the selectivity of loxiglumide to CCK A ( cholecystokinin A ) receptor ( rat pancreas and bovine gallbladder ) and CCK B / gastrin receptors ( guinea pig cerebral cortex and guinea pig gastric parietal cell ) . ^^^ These results indicate that the affinity of loxiglumide to CCK A receptor is at least 63 times greater than that to CCK B / gastrin receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Loxiglumide ( ( + / ) 4 ( 3 , 4 dichlorobenzamido ) N ( 3 methoxypropyl ) N pentylglutaramic acid , CAS 107097 80 3 , CR 1505 ) is a cholecystokinin A ( CCK A ) receptor antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Suppression of sham feeding by exogenous CCK 8 or intraintestinal oleate infusion is attenuated by peripheral administration of the CCK A receptor antagonist , devazepide , but not by the CCK B antagonist , L 365260 . ^^^ Although originally categorized as a `` peripheral ' ' receptor subtype , the CCK A receptor is also present in the brain . ^^^ Our results do not support participation of brain CCK A receptors in the suppression of food intake by exogenous CCK , or by endogenous CCK released after intraintestinal oleate infusion , or food intake . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The gastrin / cholecystokinin ( CCK ) B and CCK A receptor antagonist activities of these compounds were evaluated by investigation of their affinities for human gastrin / CCK B receptors and human CCK A receptors , respectively . ^^^ It was found that N methyl N phenyl 2 [ 2 [ N ( N methyl N phenyl carbamoylmethyl ) N [ 2 [ 3 ( 3 methylphenyl ) ureido ] acetyl ] amino ] phenoxy ] acetamide ( 20k , DZ 3514 ) exhibited high affinity for gastrin / CCK B receptors and high selectivity over CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCKB binding profile as shown in competition studies by using different CCK related compounds and non peptide CCK antagonists discriminating between CCKA and CCKB sites . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The compounds were selective for CCK B receptors as they did not bind with high affinity to CCK A receptors expressed in human tumors ( meningiomas or gastroenteropancreatic tumors ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Thus far , two CCK receptors have been molecularly identified to mediate the actions of CCK and gastrin , CCK A and CCK B receptors ( CCK AR and CCK BR , respectively ) . ^^^ The regulation of CCK AR and CCK BR affinity by guanine nucleotides and the receptor activation of G protein dependent stimulation of phospholipase C and adenylyl cyclase suggested that they were guanine nucleotide binding protein coupled receptors [ G protein coupled receptors ( GPCRs ) ] ; however , the eventual cloning of their cDNAs revealed their heptahelical structure and confirmed their membership in the GPCR superfamily . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The objectives of the present study were to determine the separate effects of CCK and gastrin on fundic and antral SOM secretion and to assess the type of receptor involved , using CCK A ( L 364 , 718 ) and CCK B / gastrin ( L 365 , 260 ) receptor antagonists . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We previously reported a synergistic interaction between leptin and cholecystokinin ( CCK ) to reduce food intake through CCK A receptors in lean mice fasted for 24 h . ^^^ Devazepide ( a CCK A receptor antagonist , 1 mg / kg , i . p . ) prevented the increase in Fos expression induced by leptin CCK in the PVN and by CCK alone in the PVN , CeA and NTS / AP . ^^^ These results indicate that in fasted mice , i . p . injection of CCK increases Fos expression in specific brain nuclei through CCK A receptors while leptin alone had no effect . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A 40 % increase in cell numbers was observed in the presence of 10 ( 10 ) MCCK 8 and this increase was inhibited by the addition of 25 microM CCK A receptor antagonist ( CR 1505 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results indicate that CCKA receptors within the SPD arterial bed mediate the satiating action of CCK , consistent with local action of duodenal CCK . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Selective N methylation of a racemic precursor with [ 11C ] iodomethane and subsequent optical resolution of the racemate with HPLC afforded optically pure [ 11C ] L 365 , 260 and [ 11C ] L 365 , 346 , which are selective for CCK B ( central type ) receptors and CCK A ( peripheral type ) receptors , respectively . ^^^ These preliminary results suggest that the nonpeptide CCK antagonist [ 11C ] L 365 , 346 may be useful for probing pancreatic CCK A receptors by PET . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This tactic yielded a series of monocyclic 2 oxopyrrolidine derivatives 4 with selectivity for CCK A or CCK B receptors and with slightly improved binding affinity at the CCK A receptor subtype with respect to the model 3 oxoindolizidines . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A bolus injection of the CCK A receptor antagonist , loxiglumide , CR 1505 ( 0 . 1 , 0 . 5 and 1 . 0 mg / kg ip ) , prior to clinimeal blocked the inhibitory action of CCK on the motor activity in a concentration dependent manner . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A series of phenoxyacetanilide derivatives was synthesized and their antagonist activities for human gastrin / cholecystokinin ( CCK ) B and CCK A receptors were evaluated . ^^^ Among the compounds synthesized , 2 [ 3 [ 3 [ N [ 2 ( N methyl N phenylcarbamoylmethoxy ) phenyl ] N ( N meth yl N phenylcarbamoylmethyl ) carbamoylmethyl ] ureido ] phenyl ] acetic acid ( 20i , DA 3934 ) exhibited high affinity for gastrin / CCK B receptors and high selectivity over CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The lectins wheat germ agglutinin ( WGA ) and Ulex europaeus agglutinin ( UEA 1 ) are used for affinity chromatography to isolate the highly glycosylated CCK A receptor of pancreatic acinar cells . ^^^ The results are discussed with respect to a possible influence of both lectins on the interaction of CCK or cerulein with the CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Sulfation of the tyrosine at the seventh position from the C terminus of cholecystokinin ( CCK ) is crucial for CCK binding to the CCK A receptor . ^^^ Using three dimensional modeling , we identified methionine 195 of the CCK A receptor as a putative amino acid in interaction with the aromatic ring of the sulfated tyrosine of CCK . ^^^ The high affinity sites of the wild type CCK A receptor were highly selective ( 800 fold ) toward sulfated versus nonsulfated CCK , whereas low and very low affinity sites were poorly selective ( 10 and 18 fold ) . ^^^ This interaction is essential for CCK dependent transition of the CCK A receptor to a high affinity state . ^^^ Our data should represent an important step toward the identification of the residue ( s ) of the receptor in interaction with the sulfate moiety of CCK and the understanding of the molecular mechanisms that govern CCK A receptor activation . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In 7 additional volunteers , the effect of cholestyramine was studied during intravenous perfusion of saline or the CCK A receptor antagonist loxiglumide . ^^^ These actions seem mediated by extrasphincteric CCK A receptors that override a direct contractile effect of CCK on the LES muscle . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Augmentation of the inhibitory effect of FK 480 , a CCK A receptor antagonist , on pancreatic exocrine secretion by achlorhydria . ^^^ FK 480 ( CCK A receptor antagonist ) inhibited pancreatic exocrine secretion dose dependently at doses of 0 . 01 1 . 0 mg / kg . ^^^ These findings suggest that inhibition of gastric acid secretion leads to the suppression of pancreatic exocrine secretion through mechanisms mediated by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A critical appraisal of this research indicates that while it is clearly demonstratable that exogenous peripheral CCK can alter food intake by acting on CCKA receptors , the mechanism involved may be more closely related to the induction if aversion and nausea , rather than satiety . ^^^ Moreover , CCKA receptor antagonist which do not cross the blood brain barrier fail to increase meal size , as would be expected if peripheral CCK was an effective satiety factor . ^^^ These studies show that CCK administered intracerebroventicularly , or by micoinjection into discrete brain regions , also inhibits feeding via a CCKA receptor mechanism . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The cholecystokinin ( CCK ) receptor types A and B ( CCKAR and CCKBR ) are G protein coupled receptors with approximately 50 % amino acid identity ; both have high affinity for the sulfated CCK octapeptide ( CCK 8 ) , whereas only the CCKBR has high affinity for gastrin . ^^^ Alanine substitution of the equivalent amino acids in the CCKAR corresponding to each of the five amino acids in ECL 1 and ECL 2 affecting CCK 8 affinity for the CCKBR revealed only two mutations , L103A and F107A , that decreased CCK 8 affinity ( 68 and 2885 fold , respectively ) . ^^^ These data suggest that CCK 8 interacts at multiple contact points in the extracellular domains of CCK receptors and that the CCKAR and CCKBR have distinct binding sites despite their shared high affinity for CCK 8 . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The present study sought to determine the roles of CCK A and CCK B receptor activation in the PAG in modulating defensive rage behavior . ^^^ Administration of the CCK A antagonist , PD 140548 ( 34 nmol / 0 . 25 microliter ) , into the PAG failed to alter response latencies for defensive rage behavior . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effect of lintitript , a new CCK A receptor antagonist , on gastric emptying of a solid liquid meal in humans . ^^^ We studied the role of endogenous CCK in the emptying of a solid / liquid meal administering the new , highly specific and potent CCK A receptor antagonist lintitript . ^^^ The study demonstrates for the first time the marked gastrokinetic properties of the new CCK A receptor antagonist lintitript in humans . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Measurements were made of the release of cholecystokinin ( CCK ) stimulated by potassium chloride in the hypothalamus after ( a ) gamma irradiation ( 60Co ) , ( b ) treatment with the CCK A and CCK B antagonists L 364 , 718 and L 365 , 260 with and without radiation , ( c ) bilateral abdominal vagotomy , and ( d ) vagotomy with and without radiation and with and without L 364 , 718 . ^^^ These results demonstrate that radiation increases the release of CCK in the hypothalamus , and that this effect is inhibited by vagotomy and the administration of a CCK A receptor antagonist . ^^^ A CCK A receptor antagonist may be used to mitigate a radiation induced deficit in food intake . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These stimulations were fully prevented by the presence of 10 pM YM 022 , a G / CCK B receptor antagonist , but unaffected by L 364 , 718 , a CCK A receptor antagonist . ^^^ CCK A and G / CCK B receptors mRNA were detected in the cells . ^^^ The evidence for secreted gastrin and CCK A and B receptors mRNA may further suggest the existence of an autocrine loop involving a stimulatory gastrin / CCK B receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effect of FK 480 , a CCK A receptor antagonist , on spontaneously developed chronic pancreatitis in WBN / Kob rats . ^^^ The effect of FK 480 , a cholecystokinin A ( CCK A ) selective receptor antagonist , on spontaneously developed chronic pancreatitis was examined in WBN / Kob rats . ^^^ Although blockade of the CCK A receptor could be considered to exacerbate chronic pancreatitis due to possible inhibition of the trophic action of CCK , our results suggest that CCK A receptor antagonists may not be detrimental to chronic pancreatitis . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Two receptor subtypes , CCK A and CCK B , have been identified by both pharmacological characterization and molecular cloning . ^^^ The CCK A receptor is the predominant peripheral CCK receptor subtype and the CCK B receptor is the predominant central CCK receptor . ^^^ In addition , there are discrete populations of CCK A receptors in the brain and CCK B receptors are present in gastric mucosa . 3 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The stimulation of CCK A or CCK B receptors is implicated in the physical and psychological responses of CCK to stress . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Binding studies showed the overexpression of two classes of CCK A receptors of low and high affinity when compared to the normal pancreas which was less sensitive to CCK 8 . ^^^ CONCLUSIONS : CCK 8 exerts a biphasic growth response on the acinar pancreatic carcinoma , mediated by two classes of CCK A receptors overexpressed in the tumour . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that there are discrete , noninteractive populations of jejunal afferents that possess either 5 HT 3 or CCK A receptors but not both . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We detected the expression of mRNA encoding CCK A and CCK B receptors in eight human pancreatic tumour cell lines using reverse transcription polymerase chain reaction ( RT PCR ) , but not by RNase protection assays . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
It describes the effects of CCK 8 infused intravenously ( i . v . ) at physiological doses and endogenous CCK released by intraduodenal ( i . d . ) oleate on gastric mucosal damage , as brought about by ethanol without or with pretreatment with loxiglumide , a selective CCK A receptor antagonist . ^^^ This occurs through activation of CCK A receptors and is associated with an increased gastric luminal release of somatostatin . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A 12 carbon but not a 10 carbon long chain fatty acid reduced antral contractile amplitude , an effect that was abolished by loxiglumide ( a specific CCK A receptor antagonist ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Two types of CCK receptors have been identified : ( 1 ) CCK A receptors are mainly located in the periphery , but are also found in some areas of the CNS ; and ( 2 ) CCK B receptors are widely distributed in the brain . ^^^ It is shown that anxiety like symptoms can only be induced by a selectively acting CCK B agonist , whereas mixed CCK A and B agonists and selective CCK A agonists fail to change behavior in anxiety tests . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
BACKGROUND : Recently , it has been shown that infusion of the CCK A receptor antagonist devazepide induced proliferation of hepatocytes and bile duct epithelium in the rat liver . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Although CCK acts through CCK A receptors to increase the TLESRs induced by gastric distension , the respective roles of endogenous CCK and fundic tone in triggering postprandial TLESRs remain unknown . ^^^ The aim of this study was to determine the effect of the CCK A receptor antagonist , loxiglumide , on postprandial LES function and fundic tone in humans . ^^^ We concluded that endogenous CCK is involved in the postprandial control of both LES function and fundic tone through activation of CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Moreover , the affinity of the different compounds towards the cholecystokinin CCK A and CCK B receptors was evaluated . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This study was designed to compare the effect of CCK 8 and intraduodenal ( i . d . ) instillation of sodium oleate , or diversion of the pancreatic biliary secretions that are known to release CCK , on the gastric mucosal lesions induced by topical application of 100 % ethanol or acidified aspirin ( ASA ) in rats with or without the pretreatment with a CCK A receptor antagonist , loxiglumide , or with L 365 , 260 to block CCK B receptors . ^^^ Both protection and accompanying hyperemia were completely abolished by blockade of CCK A receptors with loxiglumide , whereas L 365 , 260 , an antagonist of CCK B receptors , had no effect . ^^^ We conclude that endogenous CCK released by oleate or diversion of pancreatic secretion exerts a potent gastroprotective action on the stomach involving predominantly CCK A receptors and depending on vagal activity , and hyperemia mediated by NO and sensory nerves but unrelated to acid secretory effects and endogenous PG . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effect of intermittent injections of CCK 8S and the CCK A receptor antagonist devazepide on cell proliferation in exocrine rat pancreas . ^^^ When studying the influence of stimulation and inhibition of the CCK A receptor on cell proliferation in the exocrine pancreas , not only are the drugs and doses of importance but also the mode of administration . ^^^ BACKGROUND : Continuous infusion of CCK 8S or the CCK A receptor antagonist devazepide induces transient changes in acinar cell proliferation in rat pancreas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We therefore investigated , by in situ hybridization , whether CCK A or CCK B receptor mRNA could be detected in normal rat pancreatic islets and in the rat insulinoma cell line , RINm5F . ^^^ The CCK A , but not the CCK B , receptor transcript was detected in both islets and RINm5F cells . ^^^ Islet CCK A receptors were mostly confined to the center of the islets corresponding to the distribution of the B cells . ^^^ We conclude that the CCK A , but not the CCK B , receptor subtype is expressed in both normal rat islets and in the rat insulinoma derived cell line RINmS5F . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
High gastrin and cholecystokinin ( CCK ) gene expression in human neuronal , renal , and myogenic stem cell tumors : comparison with CCK A and CCK B receptor contents . ^^^ In addition , CCK A and CCK B receptors were evaluated in the same group of tumors with receptor autoradiography . ^^^ CCK A and CCK B receptors were not frequently found in these tumors , except for leiomyosarcomas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A systemic administration of cholecystokinin ( CCK ) increases gastric vagal afferent activity via type A CCK receptors ( CCKAR ) . ^^^ In the present study , the response of gastric vagal afferent activity to an intravenous administration of CCK was investigated in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which lack CCKAR , and compared with its control strain , Long Evans Tokushima Otsuka ( LETO ) rats . ^^^ The responses were not influenced by the pretreatment with L 365 , 260 , a type B CCK receptor ( CCKBR ) antagonist , while they were significantly diminished by pretreatment with MK 329 , a CCKAR antagonist . ^^^ These results demonstrate that neither CCKAR nor CCKBR contributes to the response of the afferent activity of the gastric vagal nerve to a systemic administration of CCK in OLETF rats , suggesting an involvement of novel ( non A , non B ) CCK receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
PYY antibody ( anti PYY ) at a dose of 0 . 5 mg / kg or CCK A receptor antagonist ( devazepide ) at a dose of 0 . 1 mg / kg was administered alone or in combination 10 min before the proximal half of the gut was perfused with 60 mM oleate or buffer . ^^^ We found that 1 ) peptone induced gastric acid secretion was inhibited by intestinal fat ( P < 0 . 0001 ) , 2 ) inhibition of acid secretion by intestinal fat was reversed by CCK A receptor antagonist ( P < 0 . 0001 ) but not by anti PYY , and 3 ) slowing of gastric emptying by fat was reversed by CCK A antagonist ( P < 0 . 05 ) but not by anti PYY . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The role of cholecystokinin ( CCK ) , CCK A or CCK B receptor antagonists in the spontaneous preference for drugs of abuse ( alcohol or cocaine ) in naive rats . ^^^ These results indicate that the CCK A or B receptors are selectively involved in the modulation of alcohol or cocaine intake , respectively , and suggest an involvement of the CCKergic system in the drug seeking behavior . ^^^ The selective effect of the CCK antagonists on reducing the drug intake of ED or CD rats further supports this view , as it suggests that CCK antagonists may modify the individual sensitivity towards drugs of abuse set by the stimulating effect of high endogenous CCKergic tone over CCK B or CCK A receptors in spontaneous ED or CD rats , respectively . ^^^ In particular , the data imply a CCK A receptor mechanism in the regulation of individual sensitivity towards ethanol and a CCK B receptor mechanism in the regulation of individual sensitivity towards cocaine . ^^^ Thus , a potential therapeutic role for CCK A antagonists in the treatment of ethanol abuse and for CCK B antagonists in the treatment of cocaine abuse is proposed . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The sensory experience evoked by lipid was diminished by both topical mucosal anaesthesia and CCK A receptor blockade . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The response to CCK was mediated via the CCKA receptor as shown by the antagonistic action of devazepide . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptor antagonists have selective effects on nutrient induced food intake suppression in rats . ^^^ To provide additional support to the hypothesis that only dietary protein ( Pro ; chicken egg albumin ) and not amino acids ( AA ; patterned after albumin ) , carbohydrates ( CHO ; cornstarch ) , or fats ( Fat ; corn oil ) produces a satiating effect via CCK receptors , two CCK A receptor antagonists ( PD 140 , 548 and devazepide ) were coadministered with each nutrient . ^^^ These studies provide additional evidence that CCK A receptors play a role in Pro ( albumin ) but not AA , CHO ( cornstarch ) , or Fat ( corn oil ) induced food intake suppression in rats . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Highly constrained dipeptoid analogues containing a type 2 ' beta turn mimic as novel and selective CCK A receptor ligands . ^^^ Conformationally constrained dipeptoid analogues containing the type 2 ' beta turn mimic ( 2S , 5s , 11bR ) 2 amino 3 oxohexahydroindolizino [ 8 , 7 b ] indole 5 carboxylate framework in place of the alpha MeTrp residue , show high binding affinity and selectivity for CCK A receptors , suggesting that a turn like conformation could contribute to the bioactive conformation at this CCK receptor subtype . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
However , the results obtained with CCK or CCKA receptor antagonists in different species ( rats , mice ) and different models of acute pancreatitis ( cerulein pancreatitis , hemorrhagic pancreatitis induced by choline deficient , ethionine supplemented diet , arginine induced pancreatitis , sodium taurocholate induced pancreatitis ) produced variable results . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In animal strains which do not have a CCK A receptor due to a genetic abnormality AP induced by a certain noxious factor does not develop to the same severity when compared to animals with a normal CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Localization of CCK A receptor in the human duodenum . ^^^ The autoradiographic study of CCK A and B receptors in the human duodenum and pancreas was examined in vitro . ^^^ To determine the subtypes to CCK receptors in the pancreas or duodenum , we studied the abilities of CCK A and B receptor agonists ( CCK 8 and gastrin ) and antagonists ( loxiglumide , L 364 , 718 and L 365 , 260 ) to inhibit binding of 125I CCK 8 . ^^^ CCK A receptor mRNA was not expressed in the human pancreas , but was expressed in the gallbladder and duodenum , although it was expressed in the pancreas by RT PCR . ^^^ Using autoradiography , high concentrations of CCK A receptors were detected in the duodenal mucosa , although in the pancreas only CCK B receptors were detected by this method . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A , CCK B , neurotensin , somatostatin and VIP receptors were localized by in vitro receptor autoradiography with iodinated radioligands on histological sections of surgical samples of 27 gastric and 25 colonic adenocarcinomas . ^^^ CCK A , CCK B and neurotensin 1 receptors were found in a minority of both tumor types . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) is a multifunctional regulatory peptide , which acts through two main subtypes of receptors , named CCK A and CCK B . ^^^ The simultaneous administration of equimolar doses of a selective CCK A receptor antagonist blocked the effect of CCK , while a CCK B antagonist was ineffective . ^^^ These findings indicate that CCK exerts a marked CCK A mediated proliferogenic effect on both adrenal cortex and thymus in the rat , the physiological relevance of which , however , remains to be demonstrated . ^^^ In fact , the administration of the CCK A antagonist alone was ineffective , thereby casting doubts on the role played by endogenous CCK in the maintenance and stimulation of adrenal and thymus growth . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We investigated the pharmacologic characteristics of a newly developed benzodiazepine derivative ( S ) ( ) N [ 2 , 3 dihydro 2 oxo 5 phenyl 1 [ ( 1H tetrazol 5 yl ) methyl ] 1H 1 , 4 benzodiazepine 3 yl ] 2 indolecarboxamide ( TS 941 ) , a cholecystokinin type A ( CCK A ) receptor antagonist , in the isolated rat pancreatic acini and compared with those of well known CCK A receptor antagonists , devazepide and loxiglumide . ^^^ TS 941 had a fivefold lower selectivity than devazepide for pancreatic CCK ( CCK A ) over brain CCK ( CCK B ) receptors but fourfold greater than loxiglumide when IC 50 values for inhibition of [ 125I ] CCK 8 binding in isolated acini and cerebral cortex were compared . ^^^ These results indicate that TS 941 is a potent , competitive , and selective CCK A receptor antagonist for the pancreas . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Inhibition of gastric emptying in response to 50 mg lipid in the proximal small intestine was unaffected by administration of PYY antibody but was abolished by administration of the CCK A receptor antagonist devazepide ( 0 . 1 mg / kg ip ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
High affinity CCK A receptor agonists JMV 180 and CCK OPE ( 1 1 , 000 nM ) did not increase the intensities of the RhoA band , suggesting that stimulation of RhoA is mediated by the low affinity CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Defects of cholecystokinin ( CCK ) A receptor gene expression and CCK A receptor mediated biological functions in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats . ^^^ Recent studies in genetically obese and diabetic Otsuka Long Evans Tokushima Fatty ( OLETF ) rats suggest defects of cholecystokinin ( CCK ) A receptor gene expression and CCK A receptor mediated biological functions such as pancreatic juice , protein , and gastric acid secretion . ^^^ The present studies were undertaken to further examine CCK A receptor gene expression and CCK A receptor mediated biological functions in the pancreas , stomach , and brain of OLETF rats . ^^^ Expression of the CCK A receptor gene could not be detected in the stomach , pancreas and brain by the reverse transcription polymerase chain reaction ( RT PCR ) method and Southern blotting of the PCR products . ^^^ Southern blot analysis of genomic DNA from OLETF and control Long Evans Tokushima Otsuka ( LETO ) rats with CCK A receptor fragment as a probe revealed different restriction bands . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
High affinity CCK receptors are divided in two main subtypes : the CCK A ( A for ( A for `` alimentary ' ' ) and the CCK B ( B for `` brain ' ' ) receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The responses to both CCK and CAH were abolished by the CCKA antagonist devazepide . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Single or double substitutions of the four nonconserved amino acids in the first intracellular loop of the CCK BR were made with their CCK AR counterparts to determine which residues are critical in Gs coupling . ^^^ Single substitution of Ser 82 to Asn , produced maximal cAMP responses comparable with the chimeric CCK BR containing the entire first intracellular loop of the CCK AR . ^^^ Finally , CCK AR reverse mutants were studied to compare them with their corresponding CCK BR mutants that showed increased cAMP responses . ^^^ Substitution of CCK AR residue Arg 68 to Leu resulted in a complete loss of cAMP response , whereas Asn 69 to Ser or Met 72 to Leu showed markedly diminished cAMP responses . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The dose range of activity ( 0 . 5 60 micrograms / kg ) together with the evidence that another CCK B receptor antagonist , L 365 , 260 ( 5 micrograms / kg ) increased , while devazepide ( a CCK A receptor antagonist ; 20 micrograms / kg ) decreased non REM sleep and total sleep time , support the original hypothesis that the activity of GV 150013 on sleep progress through CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Similar results were observed in binding studies with the CCK A receptor antagonist [ 3H ] L 364 , 718 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK 8 interacts with nanomolar affinities with two different receptors designated CCK A and CCK B . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Exogenous CCK and gastrin stimulate pancreatic exocrine secretion via CCK A but also via CCK B / gastrin receptors in the calf . ^^^ Specific CCK A and CCK B / G receptor antagonists ( SR 27897 and PD 135158 , respectively ) were used to identify the CCK receptor subtype involved in exogenous CCK and gastrin induced exocrine pancreatic responses . ^^^ Although CCK A receptors are not predominantly expressed , they seem to play a major role in the response of pancreatic exocrine secretion to CCK . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK receptors have been classified into two subtypes : CCK A and CCK B . ^^^ We identified a new polymorphism for the CCK A receptor gene , and tested it in our sample , with negative results . ^^^ We report here a study of polymorphisms in the CCK pre pro hormone gene ( CCK ) , CCK AR , and CCK BR in DSM 4 panic patients ( n = 99 ) vs controls matched for gender and ethnicity . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the jejunum , CCK 8 induces an inhibitory response that is mediated by both CCK A and B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The cholecystokinin A receptor ( CCK AR ) is a G protein coupled receptor that mediates important central and peripheral cholecystokinin actions . ^^^ Residues of the CCK AR binding site that interact with the C terminal part of CCK that is endowed with biological activity are still unknown . ^^^ Here we report on the identification of Arg 336 and Asn 333 of CCK AR , which interact with the Asp 8 carboxylate and the C terminal amide of CCK 9 , respectively . ^^^ Identification of the two amino acids was achieved by dynamics based docking of CCK in a refined three dimensional model of CCK AR using , as constraints , previous results that demonstrated that Trp 39 / Gln 40 and Met 195 / Arg 197 interact with the N terminus and the sulfated tyrosine of CCK , respectively . ^^^ This study also allowed us to demonstrate that ( 1 ) the identified interactions are crucial for stabilizing the high affinity phospholipase C coupled state of the CCK AR . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
As OLETF rats lack CCK A receptor because of a genetic abnormality , we examined whether learning and memory were impaired in these animals using an elevated eight arm radial maze . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist loxiglumide completely abolished the effect of cerulein on DNA fragmentation . ^^^ These effects are mediated by CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK acts with three different receptor subtypes termed as CCK A , CCK B , and gastrin receptor , which can be found in peripheral system , brain , and stomach , respectively . ^^^ However , the binding sites in CCK A receptor seem to be slightly rigid as compared to those in CCK B or gastrin receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Resected tissue specimens of pancreatic adenocarcinomas were therefore studied by both reverse transcriptase polymerase chain reaction ( RT PCR ) and in situ hybridization for the presence of CCK A receptors . ^^^ Ninety percent of studied tumors demonstrated CCK A expression by RT PCR , and this expression was localized to neoplastic cells by in situ hybridization . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Studies with CCK receptor binding , hybridization with radiolabeled complementary DNA ( cDNA ) probes , or reverse transcription polymerase chain reaction have shown that CCK A receptors also are present in rat pancreatic putative preneoplastic lesions and cancer tissue , rat pancreatic cancer cell lines , pancreatic carcinomas in transgenic mice , hamster pancreatic cancer , and human pancreatic cancer cell lines and tumors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Expressions of CCK A and CCK B receptor messenger RNA ( mRNA ) were studied in human midtrimester fetus ( 14 15 weeks ' gestation ) , infant ( 50 days old ) , and adult pancreas by reverse transcription polymerase chain reaction ( RT PCR ) followed by Southern blot analysis . ^^^ Northern blot analysis showed a strong signal for CCK B receptor mRNA in adult pancreas , but no detectable signal for CCK A receptor mRNA . ^^^ However , RT PCR / Southern blotting showed the presence of CCK A receptor mRNA in adult pancreas . ^^^ RT PCR / Southern blot analysis also showed CCK A and CCK B receptor mRNA expression in fetal and infant pancreas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Electrical physiological evidence for highand low affinity vagal CCK A receptors . ^^^ We have demonstrated that under physiological conditions CCK acts through vagal high affinity CCK A receptors to mediate pancreatic secretion . ^^^ The CCK A receptor antagonist CR 1409 , but not the CCK B antagonist L 365260 , blocked the vagal response to endogenous CCK stimulation . ^^^ In conclusion , under physiological conditions , CCK acts on both high and low affinity CCK A receptors present on distinct vagal afferent fibers . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
OBJECTIVE : To characterise the cholecystokinin ( CCK ) receptor subtypes in medullary thyroid cancer by measuring the expression of CCK A and CCK B / gastrin receptor mRNA . ^^^ MAIN OUTCOME MEASURE : Presence of CCK A and CCK B / gastrin receptors . ^^^ CCK B / gastrin receptors but not CCK A receptors were detected by RT PCR in all six biopsy specimens . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Sulfated CCK derivatives performed significantly better but also displayed a comparably high uptake in normal CCK A receptor expressing tissues . ^^^ This effect was probably due to their similar affinity for both CCK A and CCK B receptors . ^^^ Nonsulfated gastrin derivatives may be preferable because of their CCK B receptor selectivity , hence lower accretion in normal CCK A receptor expressing organs . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Acceleration of ulcer healing by cholecystokinin ( CCK ) : role of CCK A receptors , somatostatin , nitric oxide and sensory nerves . ^^^ In addition , the effects of antagonism of CCK A receptors ( by loxiglumide , LOX ) or CCK B receptors ( by L 365 , 260 ) , an inhibition of NO synthase by N ( G ) nitro L arginine ( L NNA ) , or sensory denervation by large neurotoxic dose of capsaicin on CCK induced ulcer healing were examined . ^^^ Detectable signals for CCK A and B receptor mRNAs as well as for cNOS mRNA expression were recorded by RT PCR in the vehicle control gastric mucosa . ^^^ The expression of CCK A receptor mRNA and cNOS mRNA was significantly increased in rats treated with CCK 8 and camostate , whereas CCK B receptor mRNA remained unaffected . ^^^ We conclude that CCK accelerates ulcer healing by the mechanism involving upregulation of specific CCK A receptors , enhancement of somatostatin release , stimulation of sensory nerves and hyperemia in the ulcer area , possibly mediated by NO . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The role of CCK in mediating neuronal activity in the brain in response to dietary carbohydrate was measured by detecting Fos immunoreactivity in response to duodenal glucose load in rats after administration of the CCK A receptor antagonist devazepide . ^^^ These results indicate that central neuronal activation is elicited by dietary glucose in the intestinal lumen and that activation of neurons in the NTS and AP is mediated by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Rat adipocytes exclusively contain gastrin / CCK B receptor mRNA , but not CCK A receptor mRNA . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Role of CCK A receptor in the regulation of pancreatic bicarbonate secretion in conscious rats : a study in naturally occurring CCK A receptor gene knockout rats . ^^^ Whether cholecystokinin ( CCK ) has a direct action on duct cells and the role of CCK A receptor in bicarbonate secretion were examined by comparing the results obtained from OLETF ( CCK A receptor deficient rats ) and control ( LETO ) rats . ^^^ In conclusion , intravenous injection of CCK did not stimulate bicarbonate secretion , and the lack of CCK A receptor decreased bicarbonate secretion in response to luminal stimulants . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Since CCK B / G subtype receptor is predominant over the CCK A subtype in the human pancreas , we hypothesized that it could be expressed by islet cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Decreased responsiveness to dietary fat in Otsuka Long Evans Tokushima fatty rats lacking CCK A receptors . ^^^ Adult Otsuka Long Evans Tokushima fatty ( OLETF ) rats lack functional cholecystokinin A ( CCK A ) receptors , are diabetic , hyperphagic , and obese , and have patterns of ingestion consistent with a satiety deficit secondary to CCK insensitivity . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Devazepide and L 365 , 260 were used to block CCKA and CCK ( B ) receptors and ondansetron and tropisetron to block 5 HT 3 and 5 HT 4 receptors , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Thus pretreatment of rats with a CCK A receptor antagonist ( L 364718 ) attenuated the immediate ( < or = 90 min ) pancreas secretory response to PHA but could not prevent a PHA associated increase in digestive enzyme output in the longer term ( after 90 min ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor gene possibly associated with auditory hallucinations in schizophrenia . ^^^ The present study suggests that the CCK A receptor gene may be associated with auditory hallucinations in schizophrenia . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A and B and neurotensin receptors were not detected in HCC . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To determine whether the inhibition of gastric emptying by BN like peptides is mediated by a CCK dependent mechanism , we examined the ability of the CCK A receptor antagonist , devazepide , to block the inhibition of saline gastric emptying produced by BN , GRP 18 27 and NMB . ^^^ These results suggest that BN like peptides inhibit gastric emptying through an indirect mechanism that is dependent upon CCK A receptor activation . ^^^ In contrast , the suppression of food intake by BN , in this experimental paradigm , is independent of CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The aim of this study was to elucidate the cellular sites of expression of CCK A receptor in the rat stomach and small intestine . ^^^ METHODS : We developed and characterized an antibody to the N terminal region ( LDQPQPSKEWQSA ) of rat CCK A receptor and used it for localization studies with immunohistochemistry . ^^^ RESULTS : Specificity of the antiserum was demonstrated by ( 1 ) detection of a broad band at 85 95 kilodaltons in Western blots of membranes from CCK A receptor CHO transfected cells ; ( 2 ) cell surface staining of CCK A receptor transfected cells , ( 3 ) translocation of CCK A receptor immunostaining in CCK A receptor transfected cells after exposure to CCK ; and ( 4 ) abolition of tissue immunostaining by preadsorbtion of the antibody with the peptide used for immunization . ^^^ CCK A receptor immunoreactivity was localized to myenteric neurons and to fibers in the muscle and mucosa . ^^^ Many CCK A receptor myenteric neurons contained the inhibitory transmitter vasoactive intestinal polypeptide , and some were immunoreactive for the excitatory transmitter substance P . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Sulfated CCK derivatives performed significantly better but additionally displayed a high uptake in normal , CCK A receptor expressing tissues ( such as the liver / gallbladder , pancreas , and bowel ) . ^^^ Nonsulfated gastrin derivatives may be preferable because of their CCK B receptor selectivity , and hence , lower accretion in normal CCK A receptor expressing organs . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Our aim was to identify the amino acid of the cholecystokinin A receptor ( CCK AR ) binding site in an interaction with the sulfate of CCK , which is crucial for CCK binding and activity . ^^^ A three dimensional model of the [ CCK AR CCK ] complex was built . ^^^ Wild type and mutated CCK AR were transiently expressed in COS 7 cells for pharmacological and functional analysis . ^^^ The mutant was approximately 1 , 470 and 3 , 200 fold less potent than the wild type CCK AR to activate G proteins and to induce inositol phosphate production , respectively . ^^^ These data , together with those showing that the mutated receptor failed to discriminate nonsulfated and sulfated CCK while it retained other pharmacological features of the CCK AR , strongly support an interaction between Arg 197 of the CCK AR binding site and the sulfate of CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
HSP 27 expression regulates CCK induced changes of the actin cytoskeleton in CHO CCK A cells . ^^^ We investigated how heat shock protein 27 ( HSP 27 ) and its phosphorylation are involved in the action of cholecystokinin ( CCK ) on the actin cytoskeleton by genetic manipulation of Chinese hamster ovary ( CHO ) cells stably transfected with the CCK A receptor . ^^^ To further evaluate the role of HSP 27 , CHO CCK A cells were transfected with expression vectors for either wild type ( wt ) or mutant ( 3A , 3G , and 3D ) human HSP 27 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Here , we tested whether CCK A receptors mediate the inhibition of fat on food intake . ^^^ Second , 12 subjects received either intraduodenal fat or saline perfusion plus a concomitant infusion of saline or loxiglumide , a specific CCK A receptor antagonist , together with a preload of banana shake . ^^^ This effect is mediated by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In contrast , LPC 1 responded with increased cell number to CCK 8S and decreased cell number to the CCK A receptor antagonist devazepide . ^^^ A blockade of the CCK A and CCK B receptors by their antagonists led to an increased , an unaffected , or a decreased cell number of the cell lines . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Small intestinal and pancreatic microstructures are modified by an intraduodenal CCK A receptor antagonist administration in neonatal calves . ^^^ The aim of the present study was to investigate the role of CCK on the upper gut and pancreas microstructure and on pancreatic juice secretion in neonatal calves assessed by a repetitive intraduodenal administration of FK 480 , a CCK A receptor antagonist , during the first 6 days of life . ^^^ In conclusion , the blockade of CCK A receptors during early life both reduced pancreatic exocrine secretion and induced complex changes in pancreatic microstructure . ^^^ The influence of CCK on the upper gut microstructure in neonatal calves could be either direct via activation of CCK A receptors located in the mucosa of the upper gut or indirect by modulation of the secretion of pancreatic juice . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Our study provided the possibility that polymorphism in the promoter region of the CCK A receptor gene may be one of genetic factors affecting fat deposition . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In particular , CCK co localized with mesolimbic DA cells originating in the ventral tegmental area potentiates DA function in the medial posterior nucleus accumbens ( mpNA ) through CCK A receptors . ^^^ Recently , a strain of rats lacking the CCK A receptor , Otsuka Long Evans Tokushima Fatty ( OLETF ) , has been discovered making it possible to study the mesolimbic DA regulatory role of CCK A receptors . ^^^ OLETF ( CCK A mutants ) and Long Evans Tokushima Otsuka ( LETO ) rats ( controls ) were given subcutaneous injections of either saline or AMPH ( 5 . 0 mg / kg ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Inhibition of the hypothalamic pituitary adrenal axis in food deprived rats by a CCK A receptor antagonist . ^^^ CCK 8 reduces food intake by acting on CCK A receptors subtype . ^^^ We studied the effect of CCK A and CCK B receptor antagonists on food intake during the first period of the dark cycle . ^^^ Under these conditions we observed that the CCK A receptor antagonist , SR 27897 ( 0 . 3 mg kg ( 1 ) ) , but not the CCK B receptor antagonist , L 365260 ( 1 mg kg ( 1 ) ) , increases food intake . ^^^ These results indicate that CCK A receptor blockade during fasting prevents the activation of the HPA axis . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To assess the role of endogenous cholecystokinin in the control of gastric emptying of peptone solutions and Intralipid suspensions , we examined the ability of a dose range of the CCK A antagonist , devazepide to accelerate the gastric emptying of various caloric concentrations of peptone and Intralipid in rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Therefore , in this article we ( 1 ) review evidence for CCK ' s participation in control of meal size , ( 2 ) document involvement of CCK A receptors located on vagal sensory neurons in control of food intake by exogenous and endogenous CCK , ( 3 ) point out apparent discrepancies in the experimental record , which auger for non endocrine sources of CCK and non vagal sites of CCK action , and ( 4 ) summarize recent observations , suggesting mechanisms by which CCK could participate in the control of daily food intake and body weight regulation . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The specific CCK B receptor antagonist L 740 , 093 blocks the gastrin but not the CCK response , indicating that both the CCK B and the CCK A receptor can mediate ICER gene activation . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the present study we investigated the presence of CCK A and CCK B , as well as somatostatin 2 ( SSTR 2 ) receptors by RT PCR , and studied the actions of EGF , CCK and octreotide on DNA synthesis in the human pancreatic adenocarcinoma cell line Capan 2 . ^^^ By means of RT PCR analysis we were able to demonstrate SSTR 2 expression , but not CCK A or CCK B receptor mRNA in Capan 2 cells . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
SUBJECTS AND METHODS : Three sequential double blind , three period crossover studies were performed in 12 healthy males each : ( 1 ) subjects received intraduodenal fat with or without 120 mg of tetrahydrolipstatin , an inhibitor of gastrointestinal lipases , or saline ; ( 2 ) volunteers received intraduodenal long chain fatty acids , medium chain fatty acids , or saline ; ( 3 ) subjects received long chain fatty acids or saline together with concomitant intravenous infusions of saline or loxiglumide , a specific CCK A receptor antagonist . ^^^ CONCLUSIONS : Generation of long chain fatty acids through hydrolysis of fat is a critical step for fat induced inhibition of food intake ; the signal is mediated via CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A scattered distribution of CCK A and B receptor immunopositive varicose fibers were visualized throughout the N . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Intact acini were stimulated with cholecystokinin ( CCK ) 8 , carbachol ( CCh ) and the high affinity CCK A receptor agonist , CCK OPE , and the cell lysates were used for REA . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptor activation induces fos expression in myenteric neurons of rat small intestine . ^^^ Neither has the role of CCK A receptors in the activation of rat myenteric neurons been investigated . ^^^ Neuronal Fos responsiveness in both brain and myenteric neurons was mediated by CCK A receptors , as CCK induced Fos expression was eliminated in rats pretreated with a CCK A receptor antagonist . ^^^ We conclude that CCK activates small intestinal myenteric neurons , via CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A ( cholecystokinin A ) receptor is selectively expressed by human pancreatic adenocarcinomas , suggesting a possible role in pancreatic tumorigenesis . ^^^ This study examined the temporal expression of CCK receptors in human fetal , postnatal , and adult pancreas to determine whether the appearance of CCK A receptors in pancreatic adenocarcinomas reflected oncofetal antigen or pancreatic neoantigen expression . ^^^ CCK A receptor mRNA was selectively expressed only in pancreatic adenocarcinomas . ^^^ These data suggest that selective CCK A receptor expression in pancreatic adenocarcinomas reflects neoantigen expression in humans . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist might be therapeutically useful in acute pancreatitis by stopping the vicious circle . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These pancreatic changes by the diets were abolished by treatment with devazepide , a CCK A receptor antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Gastrin / CCK B and CCK A receptors recently were demonstrated in human pancreatic adenocarcinomas , but to the authors ' knowledge expression of their ligands to date have not been adequately investigated . ^^^ Moreover , CCK , CCK A receptor , and gastrin / CCK B receptor mRNA were measured by reverse transcriptase polymerase chain reaction . ^^^ CCK A receptor mRNA was detected in most tumors , but neither the mature ligands ( alpha amidated and O sulfated CCK peptides ) nor their precursors were expressed in carcinoma and normal pancreatic tissue . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To test the possibility that cholecystokinin ( CCK ) mediates anorexia induced by IL 1 beta and LPS , mice trained to poke their noses in a hole to obtain a food reward according to a fixed ratio ( 1 reward per 20 actions ) were pretreated with the CCK A receptor antagonist L 364 , 718 ( at 1 mg / kg ) or with the CCK B receptor antagonist L 365 , 260 ( 50 microg / kg ) before being injected with LPS ( 100 microg / kg ) or IL 1 beta ( 20 microg / kg ) . ^^^ In spite of its ability to block the effects of exogenous CCK 8 on food motivated behavior in mice , the CCK A receptor antagonist did not block the depressive actions of LPS and IL 1 beta on food motivated behavior . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In conclusion , CCK 8 blocked ascending contraction elicited by electrical field stimulation of duodenal mucosa by means of simultaneous activation of CCK A and CCK B receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK peptides with combined features of hexa and tetrapeptide CCK A agonists . ^^^ Selective CCK A agonist activity has been reported to induce satiety in a variety of animals , including man , and thereby suggests a therapeutic role for CCK in the management of obesity . ^^^ To date , three general classes of CCK A agonists have been reported , the full length , sulfated hepta and hexapeptides , a series of tetrapeptides , and most recently a series of benzodiazepines . ^^^ The SAR of the hexa and tetrapeptide classes suggests that the Hpa ( SO ( 3 ) H ) and Tac groups may not interact at the CCK A receptor in the same location . ^^^ However , the C terminal dipeptide part of the hexapeptides and tetrapeptides appear to interact at the CCK A receptor in a similar manner . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) and gastrin exert their effects through two receptors , the CCK A and CCK B receptors . ^^^ Prenatal expression of both CCK A and CCK B receptors in various tissues was analyzed by RT PCR . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist devazepide was used to antagonize the effect of CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We have therefore investigated a possible role for vagal CCK A and 5 HT ( 3 ) receptors in the febrile response after intraperitoneal human recombinant interleukin 1beta ( IL 1beta ) or lipopolysaccharide ( LPS ) . ^^^ In other experiments , rats were treated with either antagonists to the 5 HT ( 3 ) receptor ( ondansetron HCl ; 100 microgram / kg ) or the CCK A receptor ( L 364 , 718 , 100 or 200 microgram / kg ) in combination with LPS or IL 1beta . ^^^ CCK administration caused a short lived hypothermia , but interference with the action of endogenous CCK at CCK A receptors was without effect on IL 1beta or LPS induced fever . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The obtained micromolar affinities for CCK A rather than CCK B receptor confirm that the anthranilic acid dimer represents a useful template for the development of selective CCK A receptor ligands . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Interaction between CCK and a preload on reduction of food intake is mediated by CCK A receptors in humans . ^^^ We therefore tested the hypothesis that alimentary CCK ( CCK A ) receptors mediate the interaction of CCK with an appetizer on food intake in humans . ^^^ CCK octapeptide ( CCK 8 , 0 . 75 microgram infused over 10 min ) or saline ( placebo ) with concomitant infusions of saline ( placebo ) or loxiglumide , a specific CCK A antagonist , was infused into 16 healthy men with use of a double blind , four period design . ^^^ These effects are mediated by CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
BACKGROUND : Infusion of sulphated cholecystokinin 8 ( CCK 8S ) in rats transiently increased the proliferation of pancreatic acinar cells , whereas the CCK A receptor antagonist devazepide decreased such proliferation . ^^^ The aim of this study was to examine the effect of continuous infusion of CCK 8S and devazepide on CCK A receptor gene expression . ^^^ The pancreas was dissected , and indirect immunofluorescence for BrdU and CCK A receptor was performed . ^^^ In situ hybridization to CCK A receptor mRNA was performed for examination and semiquantification of receptor gene expression . ^^^ Immunofluorescence for the CCK A receptor showed a decreased labeling intensity after CCK 8S infusion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In vitro we found that 1 ) 55 / 70 gastric vagal afferents ( GVAs ) were polymodal , responding to CCK 8 and mechanical stimuli , 13 were mechanoreceptive , and 2 were CCK responsive ; 2 ) sequential or randomized intra arterial injections of CCK 8 ( 0 . 1 200 pmol ) dose dependently increased firing rate and reached the peak rate at 100 pmol ; 3 ) the action was suppressed by CCK A ( Devazepide ) but not by CCK B ( L 365 , 260 ) receptor antagonist ; 4 ) neither antagonist blocked the mechanosensitivity of GVA fibers . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
At least two different G coupled high affinity receptors have been identified : the CCK A and the CCK B receptors . ^^^ This article reviews the main biological role of CCK , the therapeutic potential of CCK A and CCK B receptor agonists and antagonists and the common compounds from the different families of ligands . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Using a multi fistulated model , plasma PYY levels were compared in 6 dogs after 60 mM oleate was perfused into the proximal one half of the small intestine following i . v . administration of saline or devazepide , a CCK A antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We have also demonstrated that when the tryptophan residue is connected to the C or N terminal sides of the anthranilic acid dimer , compounds with similar micromolar CCK A receptor affinities are obtained . ^^^ Among the compounds synthesized , the N 1H indol 3 propionyl derivative exhibited an improved , at the micromolar range , affinity for the CCK A receptor in comparison to that of either , the N unsubstituted derivative and asperlicin . ^^^ The lead compound emerging from this key step of our investigation represents the new starting point for the development of a new class of CCK A receptor ligands . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We observed that peripheral gastric effects of CCK ( 300 nM ) produced a mean activation response of 271 + / 3 . 9 % compared with control level ( 100 % ) in 33 ( 60 % ) neurons tested ( P < . 01 ) , and this response was abolished by a CCK A receptor antagonist . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
When CCK acts on CCK A receptors in the gastrointestinal tract , food intake is suppressed . ^^^ Rats that lack the CCK A receptor become obese , but transgenic mice lacking CCK A receptors do not become obese . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cefaclor , a cephalosporin antibiotic , delays gastric emptying rate by a CCK A receptor mediated mechanism in the rat . ^^^ The CCK A antagonist SR 27897B ( 1 mg kg ( 1 ) , i . p . ) reversed the delay induced by 10 mM cefaclor , whereas the CCK B antagonist CI 988 ( 1 mg kg ( 1 ) , i . p . ) had no significant effect . ^^^ Cefaclor delays gastric emptying via capsaicin sensitive afferent pathways , which involve CCK A receptor interaction . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The potentiating effect induced by the co injection of ip CCK and leptin to inhibit food consumption in mice is mediated by the CCK A receptor and capsaicin sensitive afferents . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effects of cholecystokinin octapeptide ( CCK ( 8 ) ) , the CCK A receptor antagonist , MK 329 , and the CCK B receptor antagonist , L 365 , 260 , microinfused into the paraventricular nucleus of hypothalamus ( PVN ) on colonic motor function was investigated in awake rats , chronically implanted with a microinjection cannula into the PVN and a catheter into the proximal colon . ^^^ Microinfusion of the CCK A antagonist into in the PVN did not affect colonic transit . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pancreatic secretory response to feeding in the calf : CCK A receptors , but not CCK B / gastrin receptors are involved . ^^^ The present study was aimed at determining both the role of external stimuli in the outset of the prefeeding phase and the implication of pancreatic CCK A and CCK B / gastrin receptors in the mediation of pancreatic response to feeding . ^^^ The first objective was studied by suppressing external stimuli associated with food intake ( unexpected meal ) and the second by infusing highly specific and potent antagonists of CCK A ( SR 27897 ) and CCK B / gastrin ( PD 135158 ) receptors during the prandial period . ^^^ The expectancy of a meal seemed to elicit an increased pancreatic response right before a meal and CCK A receptors may mediate this information via neural pathways . ^^^ The implication of CCK and CCK A receptors in mediating the postfeeding pancreatic response was also demonstrated . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
RNA was extracted , reverse transcribed , and cDNAs were amplified with primers for human CCK A and B receptors . ^^^ The potency of the contraction induced by CCK 8 , desulphated CCK 8 , and gastrin 1 , and the effect of the CCK A ( loxiglumide and SR 27897 ) and the CCK B ( YM 022 and L 365 260 ) specific receptor antagonists were compared . ^^^ Both CCK A and CCK B receptor mRNAs were found in functional lower oesophageal sphincter strips . ^^^ The CCK 8 induced contraction was blocked by the CCK A receptor antagonists loxiglumide ( IC 50 11 micromol L 1 ) and SR 27897 ( IC 50 74 nmol L 1 ) but not by CCK B receptor antagonists ( 1 micromol L 1 ) . ^^^ Our data suggest that , although the human lower oesophageal sphincter expresses both CCK A and CCK B receptors , the contractile effect of CCK 8 on the circular muscle is mainly due to the activation of CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NAP , a peripheral CCK A receptor antagonist , modulates the development of a preference for the mother by the newborn lamb . ^^^ No major side effects were observed after the injection , however , there was a trend for lambs receiving CCK A antagonists to be more vocal in the first 2 h and to loose more weight between birth and 3 h . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lacked CCK A receptors ( CCKAR ) because of a genetic abnormality . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The relative affinity of CCK to its receptor has been characterized in various biological and pharmacological studies and it is now well established that CCK has a higher affinity to the CCKA than to the CCKB receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Reviews describe the regulation of CCK gene expression and CCK release , the nature of the hormone binding site of the CCK A receptor , interaction of CCK , dopamine and GABA , the role of CCK in thermoregulation , sexual behavior and satiety in rodents and humans . ^^^ The research articles document features of cardiovascular regulation , reduced cocaine sensitization and decreased satiety in rats that lack the CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In rodents exposed to cold a dose dependent hypothermia has been observed on peripheral injection of CCK probably acting on CCKA receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We investigated the effects of a CCK A receptor antagonist on the development of mother preference . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Attenuated satiation response to intestinal nutrients in rats that do not express CCK A receptors . ^^^ Pharmacological experiments suggest that satiation associated with intestinal infusion of several nutrients is mediated by CCK A receptors . ^^^ Otsuka Long Evans Tokushima Fatty , ( OLETF ) , rats do not express CCK A receptors and are insensitive to the satiation producing effects of exogenous CCK . ^^^ To further evaluate the role of CCK A receptors in satiation by intestinal nutrient infusion , we examined intake of solid ( pelleted rat chow ) or liquid ( 12 . 5 % glucose ) food intake , following intestinal infusions of fats ( oleic acid or fat emulsion ) , sugars ( maltotriose or glucose ) , or peptone in OLETF rats and Long Evans Tokushima Otsuka control rats ( LETO ) . ^^^ Furthermore , pretreatment with the CCK A receptor antagonist , devazepide , attenuated intestinal nutrient induced reduction of food intake only in LETO , but not OLETF rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Full length cDNA clones encoding the human CCK A and CCK B / gastrin receptor are expressed in peripheral blood mononuclear cells from healthy volunteers without haematopoietic malignancy . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In order to identify the site ( s ) of action of CCK in the gastropyloric region , we performed immunohistochemistry using an antibody directed to the C terminal region of the cholecystokinin A receptor ( CCKAR ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The aim of this study was as follows : ( 1 ) to compare the effect of continuous infusion and of intermittent injections of CCK 8S on cell proliferation , weight gain , and induction of apoptosis and ( 2 ) to examine the effect of injections of CCK 8S on CCK A receptor gene expression in the rat pancreas . ^^^ The pancreas was dissected and immunohistochemistry was performed for analysis of the expression of the apoptosis promoting protein bax and the apoptosis inhibiting protein bcl 2 , and for BrdU and CCK A receptor localization . ^^^ In situ hybridization ( ISH ) was used for examination and semiquantification of CCK A receptor mRNA expression . ^^^ Immunofluorescence and ISH for the CCK A receptor and its gene expression , respectively , showed a lowest intensity at 3 hours after CCK 8S injections . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Although these compounds exhibited a regnylogical type organization similar to that of CCK 4 , they are characterized by about 1000 fold greater affinity for CCK A receptor than the C terminal tetrapeptide . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the present study we investigated the influence of WGA and UEA 1 on CCK 8 induced alpha amylase secretion of the rat pancreatic tumor cell line AR42J , which expresses both CCK A and CCK B receptors . ^^^ The simultaneous application of the lectins with CCK antagonists L 364 , 718 or L 365 , 260 led to a reduction of secretion , but the assignment to CCK A or CCK B receptors was not possible . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To investigate the roles of endogenous NT and CCK , we administered [ ( 3 ) H ] TC into the rat duodenum or lower jejunum and tested the effect of the NT antagonist SR 48692 ( 2 nmol 10 kg ( 1 ) 10 min ( 1 ) ) or CCK A antagonist lorglumide ( 100 nmol 10 kg ( 1 ) 10 min ( 1 ) ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Moreover , the cells responded to CCK agonists after adenoviral mediated gene transfer of CCK A or CCK B receptors . ^^^ Quantitative RT PCR indicated that the message levels for CCK A receptors were approximately 30 fold lower than those of CCK B receptors , which were approximately 10 fold lower than those of m 3 Ach receptors . ^^^ In situ hybridization indicated the presence of m 3 Ach receptor and insulin mRNA but not CCK A or CCK B receptor mRNAs in adult human pancreas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Polymorphisms of the CCK , CCKAR and CCKBR genes : an association with alcoholism study . ^^^ We analyzed genetic variations in the promoter and coding regions of the CCK , CCKA receptor ( CCKAR ) and CCKB receptor ( CCKBR ) genes , and performed association analyses with alcoholism . ^^^ RESULTS : A total of 8 variants in the CCK gene , 11 variants in the CCKAR gene and 9 variants in the CCKBR gene were detected in the present study . ^^^ CONCLUSIONS : Our data suggest that polymorphisms of the CCK , CCKAR and CCKBR genes do not play a major role in alcohol withdrawal symptoms ( even though significant associations were found among polymorphisms at the 388 and 333 loci of the CCKAR gene and hallucinations , the rate was nonsignificant after Bonferroni correction ) . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The effect of oleate was abolished by the CCK A receptor antagonist Devazepide ( 0 . 5 mg / kg ) , whereas the effect of butyrate persisted despite pretreatment with either Devazepide or a combination of the calcium channel inhibitors nifedipine ( 1 mg / kg ) and the omega conotoxins GVIA and SVIB ( each 25 microg / kg ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Acid inhibition by intestinal nutrients mediated by CCK A receptors but not plasma CCK . ^^^ We examined the role of CCK A receptors in acid inhibition by intestinal nutrients . ^^^ The CCK A antagonist MK 329 ( 1 mg / kg 4 ) reversed acid inhibition caused by CLD , lipid , and dextrose . ^^^ Lipid and carbohydrate inhibit acid secretion by activating CCK A receptors but not by altering plasma CCK concentrations . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Those present in peripheral system have been termed as CCK A receptors and those present in central nervous system as CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cellular expression of CCK A and CCK B / gastrin receptors in human gastric mucosa . ^^^ Expression of CCK receptor subtypes was detected in individual cells of the gastric mucosa by reverse transcription ( RT ) PCR in situ , immunohistochemistry and confocal laser scanning microscopy , using antisera against the CCK A or CCK B / gastrin receptor subtype . ^^^ Both CCK A and CCK B receptors were detected in antral and oxyntic mucosa at the mRNA and protein level . ^^^ In fundic mucosa , CCK A receptor mRNA and protein mapped to D cells ( 37 . 4+ / 7 . 7 ) . ^^^ Besides , individual chief cells , mucous neck cells and parietal cells ( 12 . 3+ / 4 . 7 % ) expressed CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Importance of CCK A receptor for gallbladder contraction and pancreatic secretion : a study in CCK A receptor knockout mice . ^^^ Bile and pancreatic secretions were determined in a CCK A receptor deficient mouse mutant generated by gene targeting in embryonic stem cells . ^^^ In some CCK A receptor ( + / ) animals , LacZ staining was performed . ^^^ CCK 8 significantly increased amylase and bile acid outputs in CCK A receptor ( + / + ) and ( + / ) mice , whereas no response was observed in ( / ) mice . ^^^ Neuromedin C and acetylcholine increased amylase secretion in CCK A receptor ( / ) mice similar to ( + / ) and ( + / + ) mice . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Evidence suggests that endogenous cholecystokinin ( CCK ) , a neuropeptide that modulates brain dopamine function , may contribute to the therapeutic and motor effects of antipsychotic drugs via activation of CCK A receptors in the mesolimbic and nigrostriatal pathways , respectively . ^^^ To determine if CCK modulates the effects of antipsychotic drugs through CCK A receptors , we measured the haloperidol induced zif 268 mRNA response in the nucleus accumbens ( NA ) shell , NA core , and dorsal lateral striatum ( DLS ) in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats that lack CCK A receptors due to a spontaneous mutation . ^^^ These data suggest that CCK A receptor mechanisms may contribute to the therapeutic and the extrapyramidal motor effects associated with antipsychotic drug treatment . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Nine neonatal Friesian calves ( five controls and four treated intraduodenally with FK 480 , a CCK A receptor antagonist ) were surgically fitted with a pancreatic duct catheter and a duodenal cannula before the first colostrum feeding . ^^^ Immunocytochemistry indicated an association of mucosal CCK A and B receptors with neural components of the small intestine . ^^^ In conclusion , periodic activity of the exocrine pancreas exists in neonatal calves soon after birth and local neural intestinal CCK A receptors could be partly responsible for the modulation of neonatal calf pancreatic secretion . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
METHODS : CCK 8S or the CCK A receptor antagonist devazepide were infused subcutaneously by osmotic minipumps for 4 weeks in 11 and 7 hamsters , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The consensus structure between CCK 15 and CCK 8 shows a good superposition of the side chains of residues 12 14 with crucial moieties of two non peptidic CCK A antagonists . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To test the validity of this hypothesis , we determined gastric acid secretion in the CCK 1 ( CCK A ) receptor deficient Otsuka Long Evans Tokushima fatty ( OLETF ) rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The authors characterize the behavioral properties of Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which lack the CCK A receptor because of a genetic abnormality . ^^^ The results suggest that the OLETF rats showed a spatial memory deficit , hypoactivity and anxiety due , at least in part , to the lack of CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Vagotomy abolished the effects of CCK on MAP and SSND as did the CCK A receptor antagonist devazepide ( 0 . 5 mg / kg 4 ) . ^^^ RVLM neurons inhibited by exogenous CCK acting via CCK A receptors on vagal afferents may control sympathetic vasomotor outflow to the gastrointestinal tract vasculature . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Role of CCK A receptor for pancreatic function in mice : a study in CCK A receptor knockout mice . ^^^ The CCK receptors can be pharmacologically subdivided into two subtypes : CCK A and CCK B . ^^^ CCK A receptor is enriched in the pancreas of mice . ^^^ AIMS : To determine pancreatic functions in a CCK A receptor deficient mouse mutant generated by gene targeting in embryonic stem cells . ^^^ CONCLUSION : The CCK A receptor is important for pancreatic exocrine secretion , but not essential for maintaining glucose concentration and pancreatic growth in mice . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor is involved in satiety , food intake and behavior , whereas the B receptor is involved in anxiety . ^^^ We recently produced CCK A , B and AB receptor knockout mice to study the role of these receptors in energy metabolism . ^^^ Daily energy intake and expenditure were significantly greater in CCK BR ( / ) and CCK AR ( / ) BR ( / ) mice than CCK AR ( / ) and wild type [ CCK AR ( + / + ) BR ( + / + ) ] mice . ^^^ Relative liver and kidney weights ( g / kg body ) were significantly greater in CCK AR ( / ) BR ( / ) mice than in wild type mice . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The amount of mRNA expression of CCK A and CCK B receptors was determined by reverse transcription polymerase chain reaction . ^^^ The results show that CCK A receptors are significantly more expressed in non responders than responders , whereas CCK B receptor expression is similar in both groups . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
AIMS : The therapeutic efficacy of a CCK A receptor antagonist , loxiglumide , in patients with painful acute attacks of chronic pancreatitis was evaluated . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
INTRODUCTION : In humans , cholecystokinin ( CCK ) stimulates pancreatic secretion , and CCK A receptor antagonists prevent it in vivo . ^^^ High concentrations of CCK A receptors were detected in the mucosa as well as in smooth muscle of the duodenum by microautoradiography . ^^^ Neither CCK A nor CCK B receptor mediates amylase release from human pancreatic acini in vitro . ^^^ Pancreatic secretion in humans in vivo may be regulated indirectly by CCK ( via CCK A receptors ) . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Administration of MK 329 , a CCK A receptor antagonist , significantly reduced the number of postprandially activated neurons in both gastrectomized and control rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To achieve a better understanding of the mechanism by which supersaturated bile impairs the contractility , we studied changes in the expression levels of gallbladder cholecystokinin ( CCK A ) receptor messenger ribonucleic acid ( mRNA ) in prairie dogs fed a high cholesterol diet . ^^^ The mRNA levels of the CCK A receptor were determined by reverse transcription polymerase chain reaction ( RT PCR ) . ^^^ However , in contrast to the decreased contractility , the steady state mRNA levels of the gallbladder CCK A receptor were significantly increased in the animals fed a high cholesterol diet in comparison with the corresponding control animals . ^^^ Up regulation of the CCK A receptor mRNA in the gallbladder of animals fed a high cholesterol diet associated with decreased contractility may be due to an impairment of CCK signaling related to increased membrane cholesterol contents and its related reaction of biological compensation in order to increase the receptor concentration . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK is a major mediator of the sensitisation of gastric perception by lipids in patients with functional dyspepsia as the CCK A receptor antagonist dexloxiglumide markedly diminishes this effect . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Rats lacking DMN CCK A receptors are obese and have increased expression of NPY in the DMN , supporting earlier data that CCK may act at the DMN to suppress food intake . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Our aim was determine the relationship between cholecystokinin ( CCK ) A receptor blockade , glucose levels , insulin secretion and gastric emptying in humans , and to assess the effect of CCK A blockade on pancreatic polypeptide secretion . ^^^ In a second experiment , a continuous intravenous infusion of loxiglumide ( 7 . 5 mg kg h ( 1 ) ) was started 60 min before and continued until 120 min after test meal ingestion to block the CCK A receptors . ^^^ Blockade of peripheral CCK A receptors accelerates gastric emptying of liquids with an increase in postprandial insulin levels . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Actions of CCK in the controls of food intake and body weight : lessons from the CCK A receptor deficient OLETF rat . ^^^ The OLETF rat , lacking CCK A receptors , provides an important model for identifying roles for CCK in the controls of food intake and body weight . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In the present study , we determined whether oral administration of camostat showed a trophic effect in mice as observed in rats and whether the trophic effect , if substantial , was mediated via the CCK A receptor , using CCK A receptor gene targeting mice . ^^^ Three and seven day treatments with camostat did not affect pancreatic wet weight in CCK A receptor ( + / ) mice . ^^^ After 14 day treatment , the ratio of pancreatic wet weight / body weight was significantly lower in CCK A receptor ( / ) than ( + / + ) mice . ^^^ The protein and chymotrypsin contents were lower and amylase content was higher in CCK A receptor ( / ) mice , compared to ( + / + ) mice . ^^^ Camostat has a trophic effect on the pancreas in mice and this effect is mediated via the CCK A receptor , but is less potent than in rats . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We previously reported genetic variations in the promoter and coding regions of the CCKA receptor ( CCKAR ) , CCKBR , and CCK genes and a possible association between polymorphisms of the CCKAR gene and alcoholism . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist , devazepide ( which reverses protein induced food intake suppression ) , when given at 0 . 25 mg / kg , i . p . , 60 min before preloads of each of three soy hydrolysates , also blocked suppression of food intake , but the strength and duration of the interaction depended on the preparation . ^^^ We conclude that peptides arising from digestion contribute to satiety by independent activation of both opioid and CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
MK 801 [ ( + / ) 5 methyl 10 , 11 dihydro 5 H dibenzo [ a , d ] cyclohepten 5 , 10 imine maleate ] , a competitive N methyl D aspartic acid ( NMDA ) receptor antagonist , or CNQX ( 6 cyano 7 nitroquinoxaline 2 , 3 dione ) , a non NMDA receptor antagonist , muscimol ( a GABA ( A ) receptor agonist ) , or baclofen ( a GABA ( B ) receptor antagonist ) , or sulfated cholecystokinin ( CCK 8 s ; CCK A receptor agonist ) , injected i . c . v . significantly reduced the inhibition of the tail flick response induced by platycodin D administered i . c . v . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Anxiogenic effects were observed in the elevated plus maze in rats when pure CCKB receptor agonists ( CCK 4 and CCK 8 non sulfated ) or CCK 8S , a CCKB / CCKA agonist , were injected into the lateral ventricle . ^^^ In contrast , CCK 33 , a CCKA agonist or CCK ( 1 21 ) and CCK ( 26 29 ) were ineffective . ^^^ Furthermore , the anxiogenic effects of CCK 8S were prevented by blocking CCKB but not CCKA receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
L 364 , 718 , an antagonist for the CCK A receptor , blocked [ Ca ( 2+ ) ] ( 1 ) response to CCK 8 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Type A CCK receptor ( CCKAR ) antagonists differing in blood brain barrier permeability [ devazepide penetrates ; the dicyclohexylammonium salt of Nalpha 3 quinolinoyl d Glu N , N dipentylamide ( A 70104 ) does not ] were used to test the hypothesis that duodenal nutrient induced inhibition of gastric emptying is mediated by CCKARs located peripheral to the blood brain barrier . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The response was eliminated by the CCK A receptor antagonist lorglumide . ^^^ These results demonstrate that CCK acts at the low affinity site of the CCK A receptor to trigger the entry of extracellular calcium into vagal afferent neurons . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Systemic injection of CCK A receptor antagonists , devazepide ( 0 . 1 and 1 mg / kg , i . p . ) , 30 min before cocaine priming , significantly attenuated cocaine induced reinstatement of CPP , while CCK B receptor antagonist , L 365 , 260 ( 0 . 1 and 1 mg / kg , i . p . ) , did not show a similar effect . ^^^ In another experiment , CCK A or B receptor antagonists were infused into nucleus accumbens or amygdala to determine which brain area are involved in the role of different CCK receptors in stress or drug induced relapse to cocaine seeking . ^^^ These findings demonstrate that CCK A and B receptor have different roles in relapse to drug craving and further suggest that the brain areas involved in the CCK receptors on reinstatement of drug seeking are not identical . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Using a multifistulated model , intestinal transit was measured in four dogs , while 60 mM oleate was delivered into the proximal gut with either 0 or 6 mg naloxone , and 0 . 1 mg / kg devazepide ( a peripheral CCK A receptor antagonist ) administered intraluminally and intravenously , respectively . ^^^ Compared to the jejunal brake ( marker recovery of 50 . 1 + / 2 . 6 % ) , intestinal transit was slowed by the CCK A antagonist ( 36 . 4 + / 8 . 3 % ; P < 0 . 05 ) and accelerated by naloxone ( 82 . 0 + / 6 . 8 % ; P < 0 . 05 ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Type A cholecystokinin receptor ( CCKAR ) antagonists differing in blood brain barrier permeability were used to test the hypothesis that duodenal delivery of protein , carbohydrate , and fat produces satiety in part by an essential CCK action at CCKARs located peripheral to the blood brain barrier . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
RATIONALE : Converging evidence has demonstrated that cholecystokinin ( CCK ) inhibits mesolimbic brain dopamine ( DA ) function via activation of CCK A ( CCK 1 ) receptors . ^^^ Most research on the antipsychotic like drug effects of CCK has used CCK or CCK analogues that nonselectively activate both CCK A and CCK B ( CCK 2 ) receptors , which may produce opposite effects . ^^^ SR 146131 , a CCK A selective nonpeptide agonist , has recently been developed ( Sanofi Synthelabo ) . ^^^ CONCLUSIONS : The lack of an effect of SR 146131 on amphetamine induced disruption of PPI suggests that a selective nonpeptide CCK A agonist may not produce antipsychotic like effects on dopamine transmission . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We showed that STC 1 cells expressed CCKAR as well as its peptide ligand , CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pharmacological analysis suggests that this inhibition is mediated by CCK A receptors and involves PKC phosphorylation . ^^^ Pharmacology similarly demonstrated that these calcium elevations were mediated by CCK A receptors and were dependent on intracellular calcium stores . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These results suggest that OT inhibits gastric emptying in male rats via a mechanism involving CCK stimulation and CCKA receptor activation . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We examined the anxiety related behavior of CCK AR , CCK BR , and CCK ARBR gene knockout ( / ) mice in the elevated plus maze . ^^^ CCK AR ( / ) mice showed a significantly higher frequency of open arm entries than wild type and CCK BR ( / ) mice , whereas the percentage open arm entry values in CCK AR ( / ) mice did not differ from those in wild type mice . ^^^ Thus , this increased frequency in open arm entries for CCK AR ( / ) mice was interpreted to be due to an increase in locomotor activity , rather than to a reduction in anxiety . ^^^ By contrast , CCK BR ( / ) mice showed significantly lower percentage open arm entry values and spent significantly less time in the open arms than wild type and CCK AR ( / ) mice . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
V . ) were compared between wild type Long Evans ( LE ) rats and the CCK A receptor deficient Otsuka LE Tokushima Fatty ( OLETF ) rats . ^^^ We studied whether the normally low phase 3 of LE rats can be enhanced by a CCK A receptor antagonist , sodium lorglumide ( 4 . 3 microg kg 1 min 1 , 120 min , I . ^^^ V . ) , and whether the normally high phase 3 of Wistar rats can be attenuated by a CCK A receptor agonist , sulphated CCK 8 ( up to 0 . 17 microg kg 1 min 1 , 120 min , I . ^^^ We conclude that the exaggeration of phase 3 in OLETF rats reflects a secondary trait of this strain and not the lack of the CCK A receptor per se . ^^^ None of the three known phases of the febrile response of rats to LPS requires the CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Their actions are mediated via the G protein coupled CCK A and CCK B receptors . ^^^ This cell line was used to characterize the agonist dependent regulation of CCK A and CCK B receptor gene expression . ^^^ RESULTS : CCK 8 ( 10 nM ) or gastrin ( 10 nM ) reduced CCK A receptor mRNA expression to 56 % and 53 % , respectively 2 h after hormonal exposure . ^^^ The phorbolester PMA ( 100 nM ) , a protein kinase C activator , downregulated CCK A receptor expression but did not affect CCK B receptor gene transcription . ^^^ Both elevated CCK B and decreased CCK A receptor mRNA expression returned to basal levels 6 h after continuous stimulation . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
BACKGROUND : Different routes of administration of CCK 33 and blockage of CCK A and muscarinic ( m 3 ) receptors are used in this study to evaluate the mechanisms by which cholecystokinin can stimulate the exocrine pancreas . ^^^ METHODS : The experiment was performed on eight anaesthetized pigs during control conditions and after administration of the CCK A and m 3 receptor antagonists , Tarazepide and 4 DAMP , respectively . ^^^ Pancreatic secretion evoked by peripheral CCK 33 in pharmacological doses was independent of m 3 receptors blockade but depended on CCK A receptors located elsewhere than in the duodenum / pancreas . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK peptides exert their action on two distinct receptor subtypes : CCK A ( Alimentary ) now called the CCK1R , mostly expressed peripherally ; and CCK B ( Brain ) , renamed the CCK2R , which is primarily present in the brain . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Numerous techniques have been used to elucidate the structural basis for interaction of cholecystokinin ( CCK ) related peptides with their hormone binding receptor , the CCK A receptor ( CCK AR ) , including structure activity relationship studies , site directed mutagenesis , photoaffinity labeling , and solution NMR analysis of both CCK peptide ligands and peptide fragments derived from the CCK A receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In contrast to gastrin , CCK also recognizes CCK A receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Blockade of CCK A receptors with intraperitoneal MK 329 ( 1 mg / kg ) did not reverse bombesin induced gastroprotection . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Using specific antibodies against CCKA and CCKB receptors , somatostatin , glucagon and insulin , we were able to confirm by Western blot the presence of both CCK receptor protein subtypes in the calf pancreas as a 80 85 kDa CCKA receptor and 40 45 kDa CCKB receptor . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
No difference was observed in the increase of food intake induced by CCK A and CCK B receptor antagonists in both control and post infected rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Association between the CCK A receptor gene and panic disorder . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Intestinal lipid stimulates the release of cholecystokinin ( CCK ) from mucosal entero endocrine cells , and it is proposed that CCK activates CCK A receptors on vagal afferent nerve terminals . ^^^ Functional vagal deafferentation by perineural capsaicin or CCK A receptor antagonist ( devazepide , 1 mg kg ( 1 ) , i . v . ) significantly reduced chylous lymph induced inhibition of gastric motility . ^^^ These data suggest that in the intestinal mucosa , chylomicrons or their products release endogenous CCK which activates CCK A receptors on vagal afferent nerve fibre terminals , which in turn initiate a vago vagal reflex inhibition of gastric motor function . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In donor gallbladders , the CCK contraction was abolished with the CCK A receptor antagonist , L 364718 , and significantly reduced by indomethacin . ^^^ In healthy gallbladder , the contraction provoked by CCK is mediated by CCK A receptors and modulated by prostaglandins . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Evidence on the role of CCK in anxiety related and reward related behaviours in various animal models indicates that CCK B receptors in the basolateral amygdala are important mediators of anxiety related behaviours and that CCK A and CCK B receptors in the nucleus accumbens are important in mediating different aspects of reward related behaviour . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In Experiment 2 , the effects of lecithin and a CCK A receptor antagonist on gastric emptying were examined using a modified phenol red recovery technique . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Type A cholecystokinin receptor ( CCKAR ) antagonists differing in blood brain barrier permeability were used to test the hypothesis that satiety is mediated , in part , by CCK action at CCKARs located peripheral to the blood brain barrier . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The pharmacological profile of CCK CHR resembled that of CCK B receptors using agonists ( CCK 8 , CCK 4 , gastrin 17 ) , whereas CCK CHR showed higher affinity for the CCK A receptor antagonist , devazepide , than for the CCK B receptor antagonist , L 365 , 260 . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
METHODS : CCK AR and CCK BR mRNA expression and cellular distribution in the rat lung were detected by highly sensitive method of in situ reverse transcription polymerase chain reaction ( RT PCR ) and conventional in situ hybridization . ^^^ RESULTS : CCK AR and CCK BR gene positive signals were observed in bronchial epithelial cells , alveolar epithelial cells , pulmonary macrophages and vascular endothelial cells of the rats ' lung by in situ RT PCR . ^^^ The hybridization signals of CCK AR were relatively faint . ^^^ By in situ hybridization , however , only the signals of CCK BR but not CCK AR were detected in the lung , and the positive staining was only found in vascular endothelial cells and macrophages . ^^^ CONCLUSION : CCK AR and CCK BR gene were present in pulmonary vascular endothelial cells , macrophages , bronchial epithelial cells and alveolar epithelial cells , which play an important role in mediating the regulatory actions of CCK 8 on these cells . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
After the meal pattern experiments , CCK ( 0 . 5 , 1 , 2 , 4 , 8 , and 16 microg / kg ip ) was administered to examine the role of the interstitial cells and vagal IMA mechanoreceptors in relaying peripheral signals of satiety activated by CCK A receptors , whereas the specificity of the response was assessed with the antagonist devazepide ( 300 microg / kg ip ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptor activates RhoA through G alpha 12 / 13 in NIH3T3 cells . ^^^ In the present study , using NIH3T3 cells stably transfected with CCK A receptors as a model cell , we demonstrate that CCK can induce actin stress fibers through a G 13 and RhoA dependent mechanism . ^^^ These results show that in NIH3T3 cells bearing CCK A receptors , CCK activates Rho primarily through G 13 , leading to rearrangement of the actin cytoskeleton . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Enterostatin inhibition of dietary fat intake is dependent on CCK A receptors . ^^^ The series of in vivo and in vitro experiments included studies of 1 ) the feeding effect of peripheral enterostatin on Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lacking CCK A receptors , 2 ) the effect of CCK 8S on the intake of a two choice high fat ( HF ) / low fat ( LF ) diet , 3 ) the effects of peripheral or central injection of the CCK A receptor antagonist lorglumide on the feeding inhibition induced by either central or peripheral enterostatin , and 4 ) the ability of enterostatin to displace CCK binding in a 3T3 cell line expressing CCK A receptor gene and in rat brain sections . ^^^ Enterostatin did not bind on CCK A receptors because neither enterostatin nor its analogs VPDPR and beta casomorphin displaced [ 3H ] L 364 , 718 from CCK A receptors expressed in 3T3 cells or the binding of 125I CCK 8S from rat brain sections . ^^^ The data suggest that both the peripheral and central responses to enterostatin are mediated through or dependent on peripheral and central CCK A receptors . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pancreatic regeneration after ethionine induced acute pancreatitis in rats lacking pancreatic CCK A receptor gene expression . ^^^ We used Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , a model lacking pancreatic CCK A receptor gene expression . ^^^ METHODS : Ethionine induced pancreatitis was induced in the 7 week old male OLETF rats and in a control group that does not lack the pancreatic CCK A receptor , Long Evans Tokushima Otsuka ( LETO ) rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK agonists have been shown to modify baseline and stimulant induced DA release in the brain via CCK A mediated mechanisms . ^^^ However , the role of endogenous CCK in regulating brain DA via CCK A receptors has not been fully elucidated . ^^^ Recently , a strain of rats ( Otsuka Long Evans Tokushima Fatty ( OLETF ) ) , lacking the CCK A receptor due to a genetic mutation , was discovered , providing a potentially useful tool to study the DA regulatory role of CCK A receptors . ^^^ In order to further clarify the role of CCK A receptors in the regulation of central DA transmission , extracellular DA levels in the nucleus accumbens ( NAC ) and the caudate putamen ( CP ) of OLETF rats , and their non mutant counterparts , Long Evans Tokushimo Otsuka rats , was assessed by microdialysis at baseline and in response to cocaine ( 15 mg / kg ) and amphetamine ( 0 . 5 mg / kg ) administration . ^^^ These findings suggest that CCK A receptors play an important role in the regulation of central DA transmission , and support the notion that the OLETF rat is a useful model to study this regulation . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Response to acute food deprivation in OLETF rats lacking CCK A receptors . ^^^ Together , these data suggested that OLETF rats lacking CCK A receptors are not only capable of increasing their food intake in response to food deprivation , but also exhibit differential sensitivity to the effects of deprivation during both the food deprivation and refeeding periods . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Activation of the high affinity state of the CCK A receptor with the synthetic peptide JMV 180 confirmed the physiologic relevance of the response . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Intermolecular interactions were determined between a synthetic peptide corresponding to the third extracellular loop and several residues from the adjoining sixth and seventh transmembrane domains of the human cholecystokinin 1 receptor , CCK ( 1 ) R ( 329 357 ) , and the synthetic agonists Ace Trp Lys [ NH ( epsilon ) CONH o ( MePh ) ] Asp MePhe NH ( 2 ) ( GI 5269 ) and the C 1 N isopropyl N ( 4 methoxyphenyl ) acetamide derivative of 3 ( 1H Indazol 3ylmethyl ) 3 methyl 5 pyridin 3 yl 1 , 5 benzodiazepine ( GI 0122 ) , using high resolution nuclear magnetic resonance spectroscopy and computer simulations . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCK A receptor antagonist abolished the beta 51 63 induced suppression of food intake . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Many lines of evidence indicate that cholecystokinin ( CCK ) and its receptors , named CCK 1 R and CCK 2 R , are expressed in the hypothalamo pituitary adrenal ( HPA ) axis , the function of which they acutely stimulate . ^^^ Semiquantitative reverse transcription polymerase chain reaction showed that CCK treatment lowered the expression of CCK 1 R and CCK 2 R mRNAs in the pituitary , but not adrenal gland . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A cyclic CCK 8 analogue selective for the cholecystokinin type A receptor : design , synthesis , NMR structure and binding measurements . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The recent discovery that subsets of rat taste receptor cells ( TRCs ) express the peptide cholecystokinin ( CCK ) and that subsets of TRCs respond to CCK with altered potassium currents or elevated intracellular calcium via CCK A receptor has lead to the hypothesis that CCK may play a novel signaling role within the taste bud , perhaps modifying tastant responses by co transmission with a classic transmitter . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Confocal immunofluorescence studies showed that the CCK A receptor and leptin were colocalized in the endoplasm . ^^^ This was reproduced by the high affinity CCK A receptor agonist , CCK OPE . ^^^ These results indicate that canine chief cells synthesize and secrete leptin in response to CCK via the high affinity state of the CCK A receptor . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK mediates its effects through interaction with specific receptors subdivided in two subtypes CCK A ( present in the periphery and in few selected brain nuclei ) and CCK B ( the predominant receptor subtype in the brain ) . ^^^ Data showing that CCK A receptors mediate mnemonic while CCK B receptors mediate amnestic effects are also presented . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Bolus intravenous administration of CCK ( 10 microg / kg ) significantly increased pancreatic and islet blood flow in control Long Evans Tokushima Otsuka ( LETO ) rats , but not in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lacking CCK A receptors . ^^^ Our results demonstrated that exogenous CCK is a potent vasodilator of exocrine as well as islet vasculature via CCK A receptors , and that such action is mediated by a NO dependent mechanism rather than by vagal mechanisms . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK A receptor antagonist ( L 364 , 718 ) or CCK B receptor antagonist ( L 365 , 260 ) was injected intraperitoneally 15 min before leptin or CCK treatments . ^^^ CCK 8s induced reduction in the score and WWI was prevented by CCK A , but not by CCK B receptor antagonist , whereas neither antagonist altered the inhibitory effect of leptin on colitis induced injury . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
As Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lack CCK A receptor because of a genetic abnormality , we examined whether learning and memory were impaired in these animals using both Morris water maze ( MWM ) and step through type passive avoidance ( PA ) learning test . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Lack of cholecystokinin A receptor enhanced gallstone formation : a study in CCK A receptor gene knockout mice . ^^^ We generated cholecystokinin ( CCK ) A receptor ( R ) deficient ( / ) mice and found that CCK did not produce gallbladder contraction in CCK AR ( / ) mice . ^^^ The purpose of this study was to identify the role of CCK AR on gallstone formation . ^^^ Age matched CCK AR gene ( + / + ) and ( / ) progenies were used . ^^^ Sludge and gallstone formation were significantly higher in CCK AR ( / ) mice than in CCK AR ( + / + ) mice at 12 and 24 months of age , although these were not different between 12 and 24 months of age . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In order to confirm this observation more directly in vivo , the EA mediated analgesic effects are compared between Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , the natural knockout rats with the homozygously disrupted CCK A receptor gene , with Long Evans Tokushima Otsuka ( LETO ) rats . ^^^ Our results suggest that the analgesic effect of acupuncture is closely related with the amount of CCK A receptor expression . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
MK 329 ( 0 . 4 mg / kg , 4 ) , the CCK A receptor antagonist , L 365 , 260 ( 0 . 4 mg / kg , 4 ) , the CCK B receptor antagonist and atropine ( 0 . 2 mg / kg , 4 ) , the M receptor antagonist , did not affect the OT effect on gallbladder motility . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK modulates dopamine release in the nucleus accumbens via the CCK A receptor ( R ) . ^^^ We recently determined the transcriptional start site of the human CCK AR gene , and detected two sequence changes ( 81A / G and 128G / T ) in the promoter region . ^^^ The aims of the present study were to determine the prevalence of the 81A / G and 128G / T polymorphism of the CCK AR gene between alcoholics and normal control subjects and the occurrences of the polymorphisms in subtypes of alcoholics . ^^^ RESULTS : The allelic frequency of 81G in the CCK AR gene polymorphism ( 81A / G ) was significantly higher in alcoholics than in control subjects . ^^^ CONCLUSIONS : The CCK AR gene 81A / G polymorphism , especially in the 81G allele , may be associated with intractable alcoholism . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Our data clearly identified CCK A and CCK B receptor mRNAs in the rat retina and demonstrated that they are functional , stimulating tyrosine phosphorylation pathways . ^^^ Our results provide novel biochemical information to further understand the physiological role of CCK A and B receptors in rat retina . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Prior intraperitoneal treatment with lorglumide ( CR 1409 ) , a selective CCK A receptor antagonist , abolished the inhibitory effect of ethanol on the gastric emptying . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Inhibitory effect of the lectin wheat germ agglutinin on the binding of 125I CCK 8s to the CCK A and B receptors of AR42J cells . ^^^ A binding assay was used with 125I CCK 8s and dexamethasone stimulated AR42J cells , bearing CCK A as well as CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Three dimensional modeling showed that the CCK A receptor ( CCK AR ) antagonist devazepide penetrated into the transmembrane ( TM ) domains , whereas CCK was placed on the surface of the CCK AR . ^^^ Four types of rat CCK AR cDNAs were transfected into CHO K 1 and COS 7 cells : normal CCK AR cDNA transfected cells ( wild type , WT ) ; K 120 substituted with 5 ; K130V ; and R352V . ^^^ Three chimeras including the CCK AR / 3ibeta2 adrenergic receptor ( beta2AR ) , 3Nibeta2AR , and 3Cibeta2AR were constructed . ^^^ WT and CCK AR / 3Cibeta2AR increased [ Ca ( 2+ ) ] ( 1 ) in response to CCK ; 3Nibeta2AR was vice versa . ^^^ Thus , Lys 120 outside the TM 2 and Arg 352 outside the TM 6 of the CCK AR are amino acids interacting with Tyr [ SO ( 3 ) H ] 27 and Asp 32 of the CCK peptide for binding . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CCK and the Ca ( 2+ ) ionophore enhanced the Src related PTK activity , whereas the high affinity CCK A receptor agonists , fibroblast growth factor ( FGF ) , and the protein kinase C ( PKC ) activator had no or little effect . ^^^ Thus , Src cascades appear to be coupled to the low affinity CCK A receptor and utilize G ( q ) PLC pathways for their activation , independent of PKC and CaMK cascades . ^^^ The low affinity CCK A receptor regulates ROCI via mediation of Src related PTK and activates Src pathways to cause [ Ca ( 2+ ) ] ( o ) dependent pancreatic exocytosis . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
By contrast to its central fever inducing effect , in rodents exposed to cold CCK 8 elicits a dose dependent hypothermia on peripheral injection probably acting on CCK A receptors . ^^^ The possible role of CCK ergic mediation in endotoxin ( LPS ) fever has revealed that while CCK B receptors seem to be involved in the development of fever , the role of CCK A receptors could be more complex . ^^^ In particular , while rats lacking functional CCK A receptors show an exaggerated fever response , this phenomenon may be associated with a trait different from the absence of this receptor set . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We have previously shown that while CCKA receptor antagonists generally do not affect locomotor behaviors , systemic administration of a CCKA receptor antagonist attenuates amphetamine ( AMPH ) induced locomotion in animals previously treated chronically with AMPH , suggesting that chronic stimulant pretreatment may sensitize CCK systems . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Mediation of mother infant interactions by the brain gut peptide cholecystokinin ( CCK ) was examined by observing behavior of Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which lack functional CCKA receptors because of a genetic abnormality . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
This increased contractility was associated with up regulation of CCK A receptor mRNA levels in antral muscle . ^^^ Our data suggest that modulation of gastric emptying after adaptation to a low protein diet involves up regulation of both CCK A receptors and CCK induced contraction of antral smooth muscle . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The participation of the vagal and sympathetic pathways and involvement of CCK A receptors were considered . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A non invasive method for measurement of gastric emptying in mice : effects of altering fat content and CCK A receptor blockade . ^^^ Gastric emptying of cooked whole egg was also determined following administration of either vehicle or CCK A receptor antagonist , devazepide . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In matched Chinese PD subjects with and without hallucinations , the presence of the 45 C / T locus in the cholecystokinin ( CCK ) gene , particularly when combined with the CCK receptor , CCKAR ( cholecystokinin A receptor ) , C polymorphism , was associated with increased hallucination risk . ^^^ Genomic DNA was analyzed for CCK , CCKAR , and CCKBR ( cholecystokinin B receptor ) polymorphisms by polymerase chain reaction . ^^^ Of 5 cases with both CCK T and CCKAR C alleles , 4 were hallucinators . ^^^ CONCLUSIONS : Our study supports a previous association of hallucinations in PD subjects with the CCK T allele and the combined CCK T and CCKAR C allele , suggesting that the CCK system may influence the development of hallucinations in PD subjects . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
At 96 h after the administration of picrotoxin into the basolateral nucleus , we have observed an increase in the expression of genes associated with 18 different monoamine ( ie adrenergic alpha 1 , alpha 2 and beta 2 , serotonergic 5HT5b and 5HT6 , dopamine D 4 and muscarinic m 1 , m 2 and m 3 ) and peptide ( CCK A and B , angiotensin 1A , mu and kappa opiate , FSH , TSH , LH , GNRH , and neuropeptide Y ) G protein coupled receptors ( GPCRs ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The circadian rhythm of the body core temperature ( T ( c ) ) and the effects of changes in ambient temperatures on the homeostasis of T ( c ) in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which are naturally occurring cholecystokinin ( CCK ) A receptor ( CCK AR ) gene knockout ( / ) rats , were examined . ^^^ To confirm the role of CCK AR in the regulation of body temperature , the values of T ( c ) in the CCK AR ( / ) mice were compared with those in CCK B receptor ( CCK BR ) ( / ) , CCK AR ( / ) BR ( / ) , and wild type mice . ^^^ Mice without CCK AR showed larger hysteresis than mice with CCK AR . ^^^ From these results , we conclude that the lack of CCK AR causes homeostasis of T ( c ) in rats and mice to deteriorate . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Thus , the inhibitory effect of peptone on P 18 was apparently not mediated by endogenous CCK acting at CCKA receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
A separate group of nodose neurones that possessed high affinity CCK type A ( CCK A ) receptors also responded to luminal infusion of 5 HT . ^^^ From these results we concluded that the vagal nodose ganglion contains neurones that may possess only high or low affinity CCK A receptors or 5 HT 3 receptors . ^^^ Some neurones that express high affinity CCK A receptors also express 5 HT 3 receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin induced satiety is mediated through interdependent cooperation of CCK A and 5 HT 3 receptors . ^^^ Likewise , 5 HT ' s anorectic response has been linked to recruitment of peripheral CCK A receptors . ^^^ Evidence to date , however , does not elucidate whether there is a concomitant interaction between CCK A and 5 HT 3 receptors or whether each receptor functions independently in the negative feedback control of food intake elicited by CCK . ^^^ In the present study , we used selective receptor antagonists to investigate the roles of CCK A and 5 HT 3 receptors in CCK induced satiation . ^^^ Pretreatment with lorglumide ( 1 . 0 mg / kg ip ) , a selective CCK A receptor antagonist , reversed CCK induced inhibition of sucrose intake . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
However , conclusive evidence that human pancreatic acini lack functional CCK A receptors has been presented . ^^^ Although most knowledge of vagal CCK A receptors comes from research on rodents , physiologic studies suggest that this information is applicable to humans . ^^^ In contrast to its effect on satiety , which is mediated by low affinity vagal CCK A receptors , CCK acts through high affinity CCK A receptors to evoke pancreatic secretion , suggesting that different affinity states of the vagal CCK receptors mediate different digestive functions . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) , one of the first discovered gastrointestinal hormones , which stimulates pancreatic enzyme secretion and induces gallbladder contraction , is one of the most abundant neurotransmitter peptides in the brain and is implicated in satiety via CCK A receptors . ^^^ To examine the mechanism of this enhanced suppression , we measured the mRNA levels of CCK , CCK A and CCK B receptors in the cerebral cortex and the hypothalamus of young and old male rats . ^^^ The mRNA level of CCK A receptors in the hypothalamus decreased with age , whereas the mRNA levels of CCK B receptors in the hypothalamus and cerebral cortex did not . ^^^ Moreover , the effects of aging on the gene expressions of CCK A and CCK B receptors were different . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The gene expressions of cholecystokinin ( CCK ) in the proximal small intestinal mucosa and CCK A receptor in the pancreas were examined in male and female young ( 4 8 months old ) and old ( 26 29 months old ) rats . ^^^ In males , but not in females , the mRNA levels of CCK in the intestine and those of the CCK A receptor in the pancreas were significantly lower in old than young rats . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In rat , gastrin and its CCKBR seem responsible for foetal pancreas growth while after birth , CCK was shown to be the most potent trophic factor via occupation of its CCKAR . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pretreatment with the selective CCK A receptor antagonist lorglumide ( 0 . 3 3 microM ) attenuated the CCK8s induced inward current in a concentration dependent manner , with a maximum inhibition of 69 + / 12 % obtained with 3 microM lorglumide . ^^^ Immunohistochemical experiments showed that CCK A receptors were localized on the membrane of 34 , 65 , and 60 % of fundus , corpus , and antrum / pylorus projecting DMV neurons , respectively . ^^^ Our data indicate that CCK A receptors are present on a subpopulation of gastric projecting neurons and that their activation leads to excitation of the DMV membrane . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) plays a major role in the regulation of pancreatic enzyme secretion based on its binding to the CCK A receptor ( CCK AR ) . ^^^ While CCK AR is known to be expressed in rat islet B cells , the localization of CCK AR in rat pancreatic A and D cells remains poorly understood . ^^^ The aim of this study was to identify the localization of CCK AR in rat pancreatic islets by means of double immunofluorescence straining with antibodies against CCK AR , glucagon , insulin and somatostatin and with in situ hybridization to detect its transcript . ^^^ CCK AR like immunoreactive cells were found to overlap both with glucagon like immunoreactive cells and insulin like immunoreactive cells but not with somatostatin like immunoreactive cells . ^^^ An in situ hybridization study using a cRNA probe for CCK AR revealed that CCK AR mRNA was expressed in the center and periphery of the pancreatic islets . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The Cholecystokinin 1 receptor ( CCK1R ) mediates actions of CCK in areas of the central nervous system and of the gut . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Presence of CCK A , B receptors and effect of gastrin and cholecystokinin on growth of pancreatobiliary cancer cell lines . ^^^ In RT PCR , the presence of CCK A receptor and CCK B / gastrin receptor mRNA was detected in all biliary and pancreatic cancer cell lines . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The cholecystokinin A receptor ( CCK A receptor ; CCKAR ) and duodenal cholecystokinin 8 ( CCK ) revealed the associations of dioxin treatment with hormonal changes . ^^^ The intensity of CCKAR expression increased in nonvacuolated acinar cells ; a decrease in the size of CCK positive epithelial cells occurred in duodenum . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Experiments were performed under control conditions , and after pretreatment by gavage feeding with YF 476 , using either a single , low dose of 0 . 3 micromol kg , which would block the CCK B receptors , or a 1000 times higher dose ( 300 micromol kg ) , which would also block the CCK A receptors . ^^^ Supra physiological doses of CCK 33 to the general circulation appeared to affect the pancreatic enzyme secretion via CCK A receptors located elsewhere than in the pancreatic and duodenal tissue . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
AIMS : Cholecystokinin ( CCK ) modulates dopamine release in the nucleus accumbens through the CCK A receptor ( CCK AR ) . ^^^ Based on the evidence of interaction between CCK and dopamine , we had found previously that the CCK AR gene 81A / G polymorphism was associated with alcohol dependence . ^^^ Since the precise mechanism underlying this association has not been elucidated , the role of CCK AR in ethanol ingestion was examined using CCK AR gene deficient ( / ) mice and compared with those of CCK BR ( / ) and wild type mice . ^^^ RESULTS : CCK AR ( / ) mice consumed more ethanol than CCK BR ( / ) and wild type mice , and showed no aversion to high concentrations of ethanol solution . ^^^ D2R expression in the nucleus accumbens was significantly lower in the CCK BR ( / ) mice and was significantly higher in CCK AR ( / ) mice than in wild type mice . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
We investigated the interaction between ghrelin and CCK functioning in short term regulation of feeding in Otsuka Long Evans Tokushima fatty ( OLETF ) rats , which have a disrupted CCK type A receptor ( CCK AR ) , and their lean littermates , Long Evans Tokushima Otsuka ( LETO ) rats . ^^^ Using immunohistochemistry , we also demonstrated the colocalization of GH secretagogue receptor ( GHS R ) , the cellular receptor for ghrelin , with CCK AR in vagal afferent neurons . ^^^ The efficiency of ghrelin and CCK signal transduction may depend on the balance of their respective plasma concentration and / or on interactions between GHS R and CCK AR . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Furthermore , CCK ' s enhancement of distension induced Fos in Cap rats was reversed by the selective CCK A receptor antagonist lorglumide . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
These novel CCK ligands have shown to act as mixed CCK A / CCK B ligands in a [ 125 ] 1 CCK 8 receptor binding assay . ^^^ The best pyrazoline 5e of this series displayed an IC 50 of 20 and 25 nmol / L for the CCK A , and CCK B receptor , respectively . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) and the CCKA receptor gene polymorphism , and smoking behavior . ^^^ We analyzed genetic variants of the promoter region of the cholecystokinin ( CCK ; which modulates the release of dopamine ) gene , and intron 1 and exon 5 of the CCKA receptor gene , and performed association analyses of nicotine dependence using an allele specific amplification ( ASA ) method and PCR RFLP methods . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Molecular cloning , expression and pharmacological characterization of the canine cholecystokinin 1 receptor . 1 The full length , canine cholecystokinin 1 ( CCK 1 ) receptor was cloned from gallbladder tissue using RT PCR with a combination of primers designed to interact with conserved regions of the human and rat CCK 1 receptor , which also shared homology with the canine genomic sequence . 2 Analysis of the sequence of the canine CCK 1 receptor revealed a 1287 base pair product , which encoded a 429 amino acid protein . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
No amplified fragments of orexin 2 , NT 2 , and CCK A receptor cDNA were generated with GT 1 7 RNA , indicating that the GT 1 7 cells did not express mRNA of them . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Injection of the CCK A receptor antagonist 2 NAP abolished both the responses to CCK 8S and to gastric distension . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pretreatment with the CCK A receptor antagonist , lorglumide ( 1 microM ) , antagonized the effects of CCK 8s , whereas perfusion with the CCK B preferring agonist CCK 8 nonsulfated ( CCK ns , 1 microM ) did not affect the frequency of sEPSCs . ^^^ Our results suggest that the excitatory effects of CCK 8s on terminals impinging on a subpopulation of cNTS neurons are mediated by CCK A receptors ; these responsive neurons , however , do not have morphological or neurochemical characteristics that automatically distinguish them from nonresponsive neurons . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The CCKA receptor antagonist lorglumide inhibited CCK 8S induced activation of orexin neurons , whereas the CCKB receptor agonists CCK 4 ( a tetrapeptide form of cholecystokinin ) and nonsulfated CCK 8 had little effect . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Effects of cholecystokinin ( CCK ) 8 on hypothalamic oxytocin secreting neurons in rats lacking CCK A receptor . ^^^ We examined the effects of intravenous ( 4 ) administration of CCK 8 on the neuronal activity of hypothalamic OXT secreting neurons and plasma OXT level in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats that have a congenital defect in the expression of the CCK A receptor gene . ^^^ These results suggest that peripheral administration of CCK 8 may selectively activate the hypothalamic OXT secreting neurons and brainstem neurons through CCK A receptor in rats . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Reverse transcription of meningioma derived RNA into cDNA followed by amplification by the polymerase chain reaction using specific primers for CCK peptide and its CCK A and / B receptor revealed 100 % presence of CCK peptide and CCK B receptors mRNA whereas CCK A receptor was expressed in 66 % of the meningiomas . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The biological functions attributed to CCK are mediated by two receptor subtypes , termed CCKA and CCKB , located predominantly in the gastrointestinal ( GI ) tract and in the brain , respectively . ^^^ This paper focuses on the data available on the effect of CCKA receptor antagonist administration in humans , and shows how , in addition to allowing a more exact definition of the role of CCK in the regulation of some GI functions , these drugs may also possess therapeutic potential in GI disorders . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The expression of ghrelin , IAPP , and PYY and the CCK A receptor genes were examined in both gastrin and gastrin CCK double knockout ( KO ) mice using immunocytochemistry and quantitative RT PCR . ^^^ Fundic ghrelin cells expressed the CCK A receptor , and ghrelin expression increased after CCK infusion . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin , or CCK , is a 33 amino acid peptide , originally considered a gut hormone , that acts via two subtypes of receptors , named CCK 1 R and CCK 2 R . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
To examine the role of cholecystokinin 1 receptor ( CCK 1 ) in the activation of brainstem and myenteric neurons by CCK , we compared the ability of exogenous CCK 8 to induce Fos like immunoreactivity ( Fos LI ) in these neurons in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , lacking CCK 1 receptors , and Long Evans Tokushima Otsuka ( LETO ) controls . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Selective CCK A but not CCK B receptor antagonists inhibit HT 29 cell proliferation : synergism with pharmacological levels of melatonin . ^^^ We used HT 29 human colon cancer cells , expressing CCK receptors , to test the antiproliferative effects of several antagonists of CCK A and / or CCK B and their possible synergism with melatonin . ^^^ The following drugs were tested : gastrin ( CCK B agonist ) ; CCK 8s ( CCK A agonist ) ; proglumide ( CCK A plus CCK B antagonist ) ; lorglumide ( CCK A antagonist ) ; PD 135 , 158 ( CCK B antagonist and weak CCK A agonist ) ; devazepide or L 364 , 718 ( CCK A antagonist ) ; L 365 , 260 ( CCK B antagonist ) , and melatonin . ^^^ These results suggest that melatonin and CCK A antagonists are useful for controlling human colon cancer cell growth in culture and in combined therapy significantly increases their efficiency . . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
CONCLUSIONS AND CLINICAL RELEVANCE : Analysis of the results of this study reveals that sulfated CCK 8 activates myenteric and hindbrain neurons of rats primarily through CCK 1 R . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) interacts with two types of G protein coupled receptors in the brain : CCK A and CCK B receptors . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The difference in mRNA expressions of hypothalamic CCK and CCK A and B receptors between responder and non responder rats to high frequency electroacupuncture analgesia . ^^^ The mRNA expressions of CCK , and CCK A and B receptor were determined by real time RT PCR . ^^^ CCK mRNA levels were not significantly different in the two groups , whereas both CCK A and B receptors were significantly more expressed in non responders . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Those increases were abolished by the CCK A receptor blocker ( lorglumide ) , but not by the CCK B receptor blocker ( itriglumide ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
The aims of the present study were to determine the time point when the administration of the CCK A receptor antagonist loxiglumide had its maximal suppressive effect on the proliferation of pancreatic acinar cells and to investigate the effects of loxiglumide on the cell cycle time of pancreatic acinar cells during transient acinar cell proliferation induced by endogenous or exogenous CCK . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
Pentagastrin induced protein synthesis in the parotid gland of the anaesthetized rat , and its dependence on CCK A and B receptors and nitric oxide generation . ^^^ Both the CCK A receptor antagonist lorglumide ( 48 mg kg ( 1 ) , i . v . ) and the CCK B receptor antagonist itriglumide ( 5 . 5 mg kg ( 1 ) , i . v . ) , given separately , prevented the expected increase in pentagastrin and , in addition , reduced the glandular protein synthesis by 16 and 12 % , respectively , below the level of saline treated rats . ^^^ In rats treated with saline only , the glandular protein synthesis was reduced by 22 % by the CCK A receptor antagonist and by 17 % by the CCK B receptor antagonist ; combined , the two antagonists caused no further reduction ( 20 % ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
In addition , intravenous administration of CCK has been observed to reproduce the symptoms in FD and this effect can be blocked both by atropine and loxiglumide ( CCK A antagonist ) . ^^^
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P06307 and P32238 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NA
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Many lines of evidence indicate that cholecystokinin ( CCK ) and its receptors , named CCK 1 R and CCK 2 R , are expressed in the hypothalamo pituitary adrenal ( HPA ) axis , the function of which they acutely stimulate . ^^^ Semiquantitative reverse transcription polymerase chain reaction showed that CCK treatment lowered the expression of CCK 1 R and CCK 2 R mRNAs in the pituitary , but not adrenal gland . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin , or CCK , is a 33 amino acid peptide , originally considered a gut hormone , that acts via two subtypes of receptors , named CCK 1 R and CCK 2 R . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CONCLUSIONS AND CLINICAL RELEVANCE : Analysis of the results of this study reveals that sulfated CCK 8 activates myenteric and hindbrain neurons of rats primarily through CCK 1 R . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Although the wide distribution , myriad number of functions , and reported pharmacological heterogeneity of CCK receptors would suggest a large number of receptor subtypes , the application of modern molecular biological techniques has identified two CCK receptors , CCK A receptor ( CCK AR ) and CCK B receptor ( CCK BR ) , that mediate the actions of CCK and gastrin ; gastrin receptors have been found to be identical to CCK BR . ^^^ CCK AR , found predominantly in the GI system and select areas of the CNS , have high affinity for CCK and the nonpeptide antagonist L 364 , 718 , whereas CCK BR , found predominantly in the CNS and select areas of the GI system , have high affinity for CCK and gastrin and the nonpeptide antagonist L 365 , 260 . ^^^ Both CCK AR and CCK BR are highly conserved between species , although there is some tissue specific variation in expression . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In a previous study , we developed a new antagonist radioligand , 125I Bolton Hunter labeled JMV 179 , for the CCK A receptor ( CCK AR ) , to analyze CCK antagonist binding sites in pancreatic plasma membranes . ^^^ The binding of 125I ASA JMV 179 to plasma membranes was inhibited by JMV 179 ( IC 50 , 6 + / 2 nM ) , by ( Thr 28 , Ahx 31 ) CCK 25 33 ( IC 50 , 1 . 2 + / 0 . 5 nM ) , and by the nonpeptide CCK AR antagonist L 364 , 718 ( IC 50 , 2 + / 1 nM ) . ^^^ Photoaffinity labeling using pancreatic membranes or acini demonstrated that 125I ASA JMV 179 detected a new 47 50 kDa protein in addition to the 85 100 kDa CCK AR . ^^^ In competition assays using nonsolubilized or solubilized membranes , this protein displayed binding features of the CCK AR and was retained on immobilized wheat germ agglutinin , as was the CCK AR . ^^^ Protease digestions of both the CCK AR and the 47 50 kDa protein yielded identical labeled fragments , demonstrating a structural relationship between the two proteins . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We used the type A cholecystokinin receptor ( CCK AR ) antagonist devazepide to assess the importance of CCK in mediating the anorexia produced by 2 h duodenal infusions of glucose ( 9 . 2 , 11 . 0 , and 18 . 3 mmol . kg 1 . h 1 ) and the glucose dimer maltose ( 4 . 5 , 6 . 7 , and 8 . 5 mmol . kg 1 . h 1 ) at the start of the dark period in nonfasted rats with free access to food . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine the structural basis of CCK A receptor ( CCK AR ) functionally coupled to Gs , a series of chimeric mutants were constructed by replacing exons of human CCK B receptor ( CCK BR ) , from the second to the fifth ( last ) exon , with human CCK AR counterparts . ^^^ However , only the wild type CCK AR and chimeric mutants containing the second exon of CCK AR were able to mediate significantly greater increases in intracellular cAMP content and adenylyl cyclase activity compared with wild type CCK BR . ^^^ A CCK BR mutant was further constructed by replacing five amino acids , Gly Leu Ser Arg ( Arg ) Leu , in the first intracellular loop with the corresponding five CCK AR specific amino acids , Ile Arg Asn Lys ( Arg ) Met . ^^^ These data suggest that the first intracellular loop of CCK AR is essential for coupling to Gs and activation of adenylyl cyclase signal transduction cascade . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Thus far , two CCK receptors have been molecularly identified to mediate the actions of CCK and gastrin , CCK A and CCK B receptors ( CCK AR and CCK BR , respectively ) . ^^^ The regulation of CCK AR and CCK BR affinity by guanine nucleotides and the receptor activation of G protein dependent stimulation of phospholipase C and adenylyl cyclase suggested that they were guanine nucleotide binding protein coupled receptors [ G protein coupled receptors ( GPCRs ) ] ; however , the eventual cloning of their cDNAs revealed their heptahelical structure and confirmed their membership in the GPCR superfamily . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Single or double substitutions of the four nonconserved amino acids in the first intracellular loop of the CCK BR were made with their CCK AR counterparts to determine which residues are critical in Gs coupling . ^^^ Single substitution of Ser 82 to Asn , produced maximal cAMP responses comparable with the chimeric CCK BR containing the entire first intracellular loop of the CCK AR . ^^^ Finally , CCK AR reverse mutants were studied to compare them with their corresponding CCK BR mutants that showed increased cAMP responses . ^^^ Substitution of CCK AR residue Arg 68 to Leu resulted in a complete loss of cAMP response , whereas Asn 69 to Ser or Met 72 to Leu showed markedly diminished cAMP responses . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We report here a study of polymorphisms in the CCK pre pro hormone gene ( CCK ) , CCK AR , and CCK BR in DSM 4 panic patients ( n = 99 ) vs controls matched for gender and ethnicity . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The cholecystokinin A receptor ( CCK AR ) is a G protein coupled receptor that mediates important central and peripheral cholecystokinin actions . ^^^ Residues of the CCK AR binding site that interact with the C terminal part of CCK that is endowed with biological activity are still unknown . ^^^ Here we report on the identification of Arg 336 and Asn 333 of CCK AR , which interact with the Asp 8 carboxylate and the C terminal amide of CCK 9 , respectively . ^^^ Identification of the two amino acids was achieved by dynamics based docking of CCK in a refined three dimensional model of CCK AR using , as constraints , previous results that demonstrated that Trp 39 / Gln 40 and Met 195 / Arg 197 interact with the N terminus and the sulfated tyrosine of CCK , respectively . ^^^ This study also allowed us to demonstrate that ( 1 ) the identified interactions are crucial for stabilizing the high affinity phospholipase C coupled state of the CCK AR . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Our aim was to identify the amino acid of the cholecystokinin A receptor ( CCK AR ) binding site in an interaction with the sulfate of CCK , which is crucial for CCK binding and activity . ^^^ A three dimensional model of the [ CCK AR CCK ] complex was built . ^^^ Wild type and mutated CCK AR were transiently expressed in COS 7 cells for pharmacological and functional analysis . ^^^ The mutant was approximately 1 , 470 and 3 , 200 fold less potent than the wild type CCK AR to activate G proteins and to induce inositol phosphate production , respectively . ^^^ These data , together with those showing that the mutated receptor failed to discriminate nonsulfated and sulfated CCK while it retained other pharmacological features of the CCK AR , strongly support an interaction between Arg 197 of the CCK AR binding site and the sulfate of CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Amylase release in vivo and in vitro and bicarbonate secretion in vivo were not stimulated by CCK 8 in CCK AR ( / ) mice , whereas the responses to other stimulants were substantial in ( / ) mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Daily energy intake and expenditure were significantly greater in CCK BR ( / ) and CCK AR ( / ) BR ( / ) mice than CCK AR ( / ) and wild type [ CCK AR ( + / + ) BR ( + / + ) ] mice . ^^^ Relative liver and kidney weights ( g / kg body ) were significantly greater in CCK AR ( / ) BR ( / ) mice than in wild type mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We examined the anxiety related behavior of CCK AR , CCK BR , and CCK ARBR gene knockout ( / ) mice in the elevated plus maze . ^^^ CCK AR ( / ) mice showed a significantly higher frequency of open arm entries than wild type and CCK BR ( / ) mice , whereas the percentage open arm entry values in CCK AR ( / ) mice did not differ from those in wild type mice . ^^^ Thus , this increased frequency in open arm entries for CCK AR ( / ) mice was interpreted to be due to an increase in locomotor activity , rather than to a reduction in anxiety . ^^^ By contrast , CCK BR ( / ) mice showed significantly lower percentage open arm entry values and spent significantly less time in the open arms than wild type and CCK AR ( / ) mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Numerous techniques have been used to elucidate the structural basis for interaction of cholecystokinin ( CCK ) related peptides with their hormone binding receptor , the CCK A receptor ( CCK AR ) , including structure activity relationship studies , site directed mutagenesis , photoaffinity labeling , and solution NMR analysis of both CCK peptide ligands and peptide fragments derived from the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
METHODS : CCK AR and CCK BR mRNA expression and cellular distribution in the rat lung were detected by highly sensitive method of in situ reverse transcription polymerase chain reaction ( RT PCR ) and conventional in situ hybridization . ^^^ RESULTS : CCK AR and CCK BR gene positive signals were observed in bronchial epithelial cells , alveolar epithelial cells , pulmonary macrophages and vascular endothelial cells of the rats ' lung by in situ RT PCR . ^^^ The hybridization signals of CCK AR were relatively faint . ^^^ By in situ hybridization , however , only the signals of CCK BR but not CCK AR were detected in the lung , and the positive staining was only found in vascular endothelial cells and macrophages . ^^^ CONCLUSION : CCK AR and CCK BR gene were present in pulmonary vascular endothelial cells , macrophages , bronchial epithelial cells and alveolar epithelial cells , which play an important role in mediating the regulatory actions of CCK 8 on these cells . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We generated cholecystokinin ( CCK ) A receptor ( R ) deficient ( / ) mice and found that CCK did not produce gallbladder contraction in CCK AR ( / ) mice . ^^^ The purpose of this study was to identify the role of CCK AR on gallstone formation . ^^^ Age matched CCK AR gene ( + / + ) and ( / ) progenies were used . ^^^ Sludge and gallstone formation were significantly higher in CCK AR ( / ) mice than in CCK AR ( + / + ) mice at 12 and 24 months of age , although these were not different between 12 and 24 months of age . ^^^ The plasma cholesterol levels , daily food intake , and body weight were not significantly different between CCK AR ( + / + ) and ( / ) mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We recently determined the transcriptional start site of the human CCK AR gene , and detected two sequence changes ( 81A / G and 128G / T ) in the promoter region . ^^^ The aims of the present study were to determine the prevalence of the 81A / G and 128G / T polymorphism of the CCK AR gene between alcoholics and normal control subjects and the occurrences of the polymorphisms in subtypes of alcoholics . ^^^ RESULTS : The allelic frequency of 81G in the CCK AR gene polymorphism ( 81A / G ) was significantly higher in alcoholics than in control subjects . ^^^ CONCLUSIONS : The CCK AR gene 81A / G polymorphism , especially in the 81G allele , may be associated with intractable alcoholism . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Three dimensional modeling showed that the CCK A receptor ( CCK AR ) antagonist devazepide penetrated into the transmembrane ( TM ) domains , whereas CCK was placed on the surface of the CCK AR . ^^^ Four types of rat CCK AR cDNAs were transfected into CHO K 1 and COS 7 cells : normal CCK AR cDNA transfected cells ( wild type , WT ) ; K 120 substituted with 5 ; K130V ; and R352V . ^^^ Three chimeras including the CCK AR / 3ibeta2 adrenergic receptor ( beta2AR ) , 3Nibeta2AR , and 3Cibeta2AR were constructed . ^^^ WT and CCK AR / 3Cibeta2AR increased [ Ca ( 2+ ) ] ( 1 ) in response to CCK ; 3Nibeta2AR was vice versa . ^^^ Thus , Lys 120 outside the TM 2 and Arg 352 outside the TM 6 of the CCK AR are amino acids interacting with Tyr [ SO ( 3 ) H ] 27 and Asp 32 of the CCK peptide for binding . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The circadian rhythm of the body core temperature ( T ( c ) ) and the effects of changes in ambient temperatures on the homeostasis of T ( c ) in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which are naturally occurring cholecystokinin ( CCK ) A receptor ( CCK AR ) gene knockout ( / ) rats , were examined . ^^^ To confirm the role of CCK AR in the regulation of body temperature , the values of T ( c ) in the CCK AR ( / ) mice were compared with those in CCK B receptor ( CCK BR ) ( / ) , CCK AR ( / ) BR ( / ) , and wild type mice . ^^^ Mice without CCK AR showed larger hysteresis than mice with CCK AR . ^^^ From these results , we conclude that the lack of CCK AR causes homeostasis of T ( c ) in rats and mice to deteriorate . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) plays a major role in the regulation of pancreatic enzyme secretion based on its binding to the CCK A receptor ( CCK AR ) . ^^^ While CCK AR is known to be expressed in rat islet B cells , the localization of CCK AR in rat pancreatic A and D cells remains poorly understood . ^^^ The aim of this study was to identify the localization of CCK AR in rat pancreatic islets by means of double immunofluorescence straining with antibodies against CCK AR , glucagon , insulin and somatostatin and with in situ hybridization to detect its transcript . ^^^ CCK AR like immunoreactive cells were found to overlap both with glucagon like immunoreactive cells and insulin like immunoreactive cells but not with somatostatin like immunoreactive cells . ^^^ An in situ hybridization study using a cRNA probe for CCK AR revealed that CCK AR mRNA was expressed in the center and periphery of the pancreatic islets . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
AIMS : Cholecystokinin ( CCK ) modulates dopamine release in the nucleus accumbens through the CCK A receptor ( CCK AR ) . ^^^ Based on the evidence of interaction between CCK and dopamine , we had found previously that the CCK AR gene 81A / G polymorphism was associated with alcohol dependence . ^^^ Since the precise mechanism underlying this association has not been elucidated , the role of CCK AR in ethanol ingestion was examined using CCK AR gene deficient ( / ) mice and compared with those of CCK BR ( / ) and wild type mice . ^^^ RESULTS : CCK AR ( / ) mice consumed more ethanol than CCK BR ( / ) and wild type mice , and showed no aversion to high concentrations of ethanol solution . ^^^ D2R expression in the nucleus accumbens was significantly lower in the CCK BR ( / ) mice and was significantly higher in CCK AR ( / ) mice than in wild type mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We investigated the interaction between ghrelin and CCK functioning in short term regulation of feeding in Otsuka Long Evans Tokushima fatty ( OLETF ) rats , which have a disrupted CCK type A receptor ( CCK AR ) , and their lean littermates , Long Evans Tokushima Otsuka ( LETO ) rats . ^^^ Using immunohistochemistry , we also demonstrated the colocalization of GH secretagogue receptor ( GHS R ) , the cellular receptor for ghrelin , with CCK AR in vagal afferent neurons . ^^^ The efficiency of ghrelin and CCK signal transduction may depend on the balance of their respective plasma concentration and / or on interactions between GHS R and CCK AR . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To examine the hormonal mediators , the effects of a somatostatin monoclonal antibody and a CCK A receptor antagonist ( L 364718 ) on acid induced inhibition of gastric acid secretion were studied in transplanted rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We evaluated the effects of a potent cholecystokinin ( CCK ) B / gastrin receptor antagonist , L 365 , 260 ( 3R ( + ) N ( 2 , 3 dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepin 3 yl ) N ' ( 3 methylphenyl ) urea ) ; a selective CCK A receptor antagonist , devazepide ( L 364 , 718 ) ; and cimetidine on gastric acid secretion induced by pentagastrin , histamine and bethanechol in anesthetized rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The anorectic activity of 21 was blocked by the specific CCK A receptor antagonist MK 329 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In Experiment 3 , the responsibility of endogenous cholecystokinin ( CCK ) for the difference in food intake between the two diets was investigated for 6 h by using a CCK A receptor antagonist , Devazepide ( DVZ , 1 mg / kg b . wt . ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Intraventricular administration of the selective CCK A receptor agonist A 71623 at 1 and 10 nmol / kg suppressed 30 min meal size 69 + / 22 % and 75 + / 7 % , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist , devazepide , blocks the anorectic action of CCK but not peripheral serotonin in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Analysis of the ability of gastrin 17 1 to inhibit 125I gastrin 1 binding demonstrated that gastrin bound to a single class of receptors with a Kd of 0 . 21 + / 0 . 04 nM and a binding capacity of 184 + / 29 fmol / mg protein . 125I Gastrin 1 binding was inhibited by the specific CCK B receptor antagonist L 365 , 260 approximately 40 times more effectively than by the specific CCK A receptor antagonist L 364 , 718 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The results probably indicate that CCK A receptor stimulation inhibits TSH secretion at the level of the anterior pituitary gland . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
All of the analogues that showed high affinity ( less than 10 nM ) for the CCK A receptor also were full agonists in amylase release and most were full or nearly full agonists in the phosphoinositide ( PI ) turnover assay , the most notable exception being the delta Z Phe 33 analogue , which showed 69 % of the maximal response in the PI assay . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A 71623 , a selective CCK A receptor agonist , suppresses food intake in the mouse , dog , and monkey . ^^^ Our results support other evidence suggesting that the anorectic actions of exogenous application of CCK 8 in these species are mediated via stimulation of the CCK A receptor subtype . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The amino acid sequence deduced from the cloned cDNA showed 85 . 7 % and 49 . 0 % identity to canine parietal cell gastrin receptor and rat pancreatic CCK A receptor , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide , a potent CCK A receptor antagonist , and L 365 , 260 , a selective CCK B receptor antagonist , have been introduced as pharmacologic tools for differentiating the physiologic roles of CCK A and CCK B receptor subtypes . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Thus , devazepide , a selective CCK A receptor antagonist , produced a dose related inhibition of the CCK 8 stimulated rise in circulating beta endorphin concentrations . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present study used the substance loxiglumide , which acts as a specific antagonist at the CCK A receptor , to evaluate this hypothesis . ^^^ Therefore , effects mediated by the CCK A receptor do not play a major physiological role in the regulation of the interdigestive and postprandial motility of the left colon . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Stimulation of peripheral and central CCK A receptors by the selective CCK A receptor agonist A 71623 suppressed intakes of a liquid diet in both deprived and sated rats . ^^^ Although these results stress the relative importance of the CCK A receptor in the effects of exogenous CCK 8 administration on feeding , stimulation of the CCK B receptor may still be involved in the control of feeding following the endogenous release of CCK . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The inhibitory potency of MK 329 , a selective CCK A receptor antagonist , was similar against either CCK 8 ( 10 nM ) or gastrin 1 ( 10 microM ) , except that a minor portion ( approximately 30 40 % ) of gastrin 1 induced pepsinogen release was insensitive to MK 329 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Subcutaneously administered selective CCK A receptor antagonist , L 364 , 718 ( 1 mg / kg ) , reversed the inhibitory effect of centrally as well as peripherally administered CCK 8 , but the selective CCK B receptor antagonist , L 365 , 260 ( 1 mg / kg ) , did not . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Thus peripherally administered CCK induces vasopressin release by CCK A receptor activation , in agreement with its inhibitory effect on food intake in this species . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In contrast , in the mouse CCK JMV 180 potently suppressed intakes on its own , and this effect was blocked by pretreatment with the selective CCK A receptor antagonist , A 70104 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The specific CCK A receptor antagonist , MK 329 ( formerly L 364 , 718 ; 1 . 0 nM ) , reversibly blocked the facilitatory effect of CCK 8 on ganglionic transmission . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The cholecystokinin ( CCK ) receptor involved in contraction of guinea pig ileal longitudinal muscle to cholecystokinin is poorly understood ; some studies have suggested that contraction was mediated via a CCK A receptor whereas other studies have implicated CCK B receptors in ileal contraction to CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
G 17I induced amylase secretion was unaffected by 100 nM of the selective peripheral CCK A receptor antagonist L 364 , 718 , suggesting that amylase hypersecretion followed non selective CCK receptor activation , a function normally assumed by selective CCK A receptors in rat pancreatic acini . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This paper reviews experiments in which devazepide ( a selective CCK A receptor antagonist ) and L 365 , 260 ( a selective CCK B gastrin receptor antagonist ) have been used . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The parent compound of this series ( lorglumide ) is the first nonpeptidic , potent and selective antagonist of the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Efforts to include the weak CCK antagonist benzotript into this construct utilizing a similar approach have resulted in a novel series of benzotript based hybrid antagonists N alpha ( 3 ' quinolylcarbonyl ) ( R ) tryptophan di n pentylamide ( 9 , A 67396 ) , N alpha ( 4 ' , 8 ' dihydroxy 2 ' quinolylcarbonyl ) ( R ) tryptophan di n pentylamide ( 23 , A 70276 ) , and N alpha ( 3 ' quinolylcarbonyl ) ( R ) 5 ' hydroxytryptophan di n pentylamide ( 36 , A 71134 ) which possess respectively binding affinities of 23 , 21 , and 11 nM for the pancreatic CCK A receptor and which inhibit CCK 8 induced amylase secretion . ^^^ Compound 9 possesses a selectivity of greater than 500 fold for the pancreatic CCK A receptor over the CCK B receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This increase in sensitivity to quinpirole was blocked by pretreatment with the nonselective CCK receptor antagonist proglumide and the preferential CCK A receptor antagonist CR 1409 but not by the preferential CCK B receptor antagonist L 365 , 260 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The high selectivity of the tissue for sulfated CCK 8 suggests that the secretory effect of CCK 8 on guinea pig ileal electrolyte transport is mediated by a CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
At the end of 40 min , food was removed and rats were injected subcutaneously ( SC ) with devazepide ( DVZ ; 1 ng / kg 1 mg / kg ) , an antagonist selective for the CCK A receptor , or its vehicle , 0 . 5 % carboxymethylcellulose ( CMC ) . ^^^ These results confirm and extend previous reports that CCK A receptor blockade increases food intake after an oral preload . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present report reviews recent evidence obtained in studies using devazepide ( a selective CCK A receptor antagonist ) and L 365 , 260 ( a selective CCK B / gastrin receptor antagonist ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective CCK B receptor antagonists CI 988 ( PD 134308 ) and L 365 , 260 produced anxiolytic like effects , whereas MK 329 , a CCK A receptor antagonist , was respectively less potent by factors of 313 and 200 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective cholecystokinin ( CCK ) B receptor agonist and antagonist , BC 264 and L 365260 , respectively , and the CCK A receptor antagonist , L 364718 , were used to investigate the possible involvement of different classes of CCK receptors in the control of food intake induced by exogenous CCK octapeptide ( CCK 8 ) in the cat with gastric fistula . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
L 364 , 718 , an antagonist selective for the CCK A receptor , blocked completely the action of centrally administered CCK , whereas L 365 , 260 , a selective CCK B receptor antagonist , had no effect on the ability of centrally administered CCK to inhibit feeding . ^^^ Intraventricularly administered CCK thus appears to reduce feeding in the rat through a mechanism involving a CCK A receptor subtype in the periphery . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In particular , compounds 2c , 2g , and 2h possess a high affinity for the CCK A receptor subtype coupled with a low affinity for the CCK B subtype . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effects of the CCK A receptor antagonist CR 1409 on the activity of rat midbrain dopamine neurons . ^^^ Repeated treatment with 5 mg / kg ( IP ) increased the number of spontaneously active DA cells in the A 10 ( ventral tegmental area ) but not the A 9 ( substantia nigra zona compacta ) region , which suggests that these DA populations are differentially affected by prolonged CCK A receptor blockade . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These findings suggest that ceruletide specifically suppresses the barrel rotation evoked by SMS 201 995 in a long lasting manner possibly acting through CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The mammillary bodies and supramammillary nuclei also contained CCK A receptor sites . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Herein we describe the properties of A 71378 [ desamino Try ( SO3H ) Nle Gly Trp Nle ( N methyl ) Asp Phe NH 2 ] , a highly selective CCK A receptor ligand . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Synthesis and biological activity of new cholecystokinin ( CCK ) analogs with a special CCK A receptor antagonistic effect ] . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
All compounds with IC 50 ' s less than 100 microM proved to have greater affinity for the CCK A receptor , with the most potent analogue , 6e , having an IC 50 of 0 . 16 microM . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine the role of CCK A receptors in the cholecystokinin ( CCK ) induced suppression of locomotor activity in the rat , the ability of the selective CCK A receptor antagonist L 364 , 718 to block these responses was investigated . ^^^ It is concluded that L 364 , 718 is a potent antagonist of the actions of CCK 8 and caerulein on locomotor activity , suggesting that the effects of these peptides are mediated by a CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Intracerebral , but not i . p . , injection of a low dose of a CCK antagonist , reversed the effect of peripheral CCK 8 on food intake as did i . p . injection of peripheral CCK A receptor antagonists . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These data indicate that in striking contrast to CCK receptors in rat spinal cord , those in the primate cord are of the CCK A receptor subclass . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In addition , the effect of continuous subcutaneous infusion of the CCK A receptor antagonist devazepide was studied . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The inhibitory effect of 10 micrograms / kg ( s . c . ) CCK 8S was prevented by loxiglumide , a mixed type of CCK A and B receptor antagonist , at 1 mg / kg ( intraperitoneal ) and 40 micrograms / rat ( intracerebroventricular , i . c . v . ) ; L 364 , 718 , a CCK A receptor antagonist , at 125 and 250 ng / rat ( i . c . v . ) ; and L 365 , 260 , a CCK B receptor antagonist at 250 ng / rat ( i . c . v . ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the isolated pancreatic acini of rats , KSG 504 caused a parallel rightward shift of the concentration response curve for CCK 8 stimulated amylase release with no change in its maximal response , indicating a competitive antagonism of the drug for the CCK A receptor ( Schild plot analysis ; slope = 0 . 927 , pA 2 = 6 . 9 ) . ^^^ These results demonstrate that KSG 504 is a competitive and selective CCK A receptor antagonist that is effective in vivo after oral administration . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Our results indicate that CCK receptors present in chicken ileum behave similarly but not identically to the CCK A receptor described in mammals . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In order to investigate a possible direct agonist effect of the CCK B / gastrin receptor antagonist , we studied amylase release from isolated rat pancreatic acini in response to PD 136450 and sulfated CCK 8 alone and in combination with the specific CCK A receptor antagonist MK 329 . ^^^ The specific CCK A receptor antagonist MK 329 dose dependently inhibited CCK 8 and PD 136450 induced amylase release . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK B / gastrin receptor antagonist L 365 , 260 abolished the stimulating effect of cionin on both histamine release and acid secretion , whereas the CCK A receptor antagonist L 364 , 718 only had a faint effect . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Additionally , we utilized 32P labeled cDNA probes of the CCK A receptor and CCK B ( gastrin ) receptor coding regions in order to examine the expression of CCK receptor subtypes in normal rat pancreas at the mRNA level . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor mRNA was not expressed in the fetal pancreas of either strain or in the adult pancreas of OLETF rats , but was expressed in the adult pancreas of LETO rats . ^^^ These results suggest that OLETF rats are a new model of a congenital defect of the CCK A receptor gene and should be useful for determining CCK receptor function . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We examined whether the short term administration of KSG 504 ( KSG ) , a synthetic CCK A receptor antagonist , inhibited the regeneration of pancreatic acinar cells after ethionine induced acute pancreatitis in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Lack of satiety effect of cholecystokinin ( CCK ) in a new rat model not expressing the CCK A receptor gene . ^^^ CCK A receptor mRNA was detected in the hypothalamus of LETO rats but not OLETF rats . ^^^ These results show that in OLETF rats the absence of CCK A receptor gene expression in the hypothalamus results in hyperphagia because of lack of satiety . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Therefore , we characterized CCK binding properties and CCK A receptor mRNA expression in pancreatic carcinomas and dysplastic pancreata from the Tg ( Ela 1 , SV40E+Ela 1 , neo ) Bri 19 strain of ELSV transgenic mice . ^^^ RT PCR and Southern blot analysis confirmed the 125I BH CCK 8 binding studies by demonstrating CCK A receptor mRNA expression in the ELSV transgenic pancreatic carcinomas and dysplastic pancreas , as well as in normal nontransgenic mouse pancreas . ^^^ In conclusion , pancreatic carcinomas and dysplastic pancreas from ELSV transgenic mice and normal nontransgenic mouse pancreas all bind 125I BH CCK 8 and express mRNA for the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In a double blind , placebo controlled study , we investigated the effect of the specific CCK A receptor antagonist loxiglumide on food intake ( carbohydrate rich meal ) and on subjective hunger feelings scored with visual analogue scales and food selection lists in seven healthy obese women and in seven healthy lean women . ^^^ In conclusion , in the present study during infusing the CCK A receptor antagonist loxiglumide we found no increase in preprandial satiety nor in food intake of a carbohydrate rich meal nor in postprandial satiety in lean and obese women . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Both somatostatin and CCK A receptor antagonists inhibit stimulation of the gallbladder by CCK . ^^^ The aim of this study was to compare the effect of somatostatin and the CCK A receptor antagonist loxiglumide ( CR 1505 ) on gallbladder volume at baseline and after feeding . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK 8 infused intravenously ( 0 . 1 1 microgram . kg 1 . h 1 ) dose dependently increased the occurrence of relaxations while it was reduced by the CCK A receptor antagonist devazepide but not the CCK B antagonist L 365260 , both administered intravenously in a dose range of 0 . 1 100 micrograms / kg . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK is also responsible , via the CCK A receptor , for the pancreatic hyperplasia observed following the feeding of protease inhibitors or pancreaticobiliary diversion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The fact that devazepide is 1000 times more potent as a CCK A receptor antagonist than L 365 , 260 , whereas the two compounds are nearly equipotent at the CCK B receptor subtype , suggests that CCK B rather than CCK A receptors are involved in these effects . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The affinity of YM 022 for gastrin / CCK B receptor was more than 2 orders of magnitude higher than that for rat pancreatic CCK A receptor and various other receptors , such as benzodiazepine . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Guinea pig gallbladder and pancreas possess identical CCK A receptor subtypes : receptor cloning and expression . ^^^ Pharmacological and functional studies in pancreas and gallbladder demonstrate a CCK A receptor subtype in both tissues . ^^^ However , some pharmacological studies and affinity cross linking studies of CCK receptors on pancreatic acini and gallbladder suggest that these two tissues possess two different subtypes of the CCK A receptor . ^^^ We cloned these receptors in guinea pig using a cDNA clone of the CCK A receptor from rat pancreas . ^^^ The guinea pig gallbladder CCK A receptor was cloned by hybridization screening of a gallbladder cDNA library using a cDNA probe from the rat CCK A receptor coding region . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cloning and expression of the rabbit gastric CCK A receptor . ^^^ Using polymerase chain reaction with primers from the known sequence of the rat pancreatic CCK A receptor cDNA , we prepared a 600 bp product from rat and rabbit stomach cDNA . ^^^ From Southern analysis these represented a fragment of a gastric CCK A receptor . ^^^ PCR was then used to amplify a rabbit lambda ZAP 2 gastric epithelial cDNA library with the same primers , and the product was identified by sequencing as representing a CCK A receptor fragment . ^^^ Hence from sequence and second messenger responses , the clone represents the CCK A receptor presumably responsible for pepsinogen secretion by gastric chief cells and somatostatin release from gastric D cells . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Metabolism of cholecystokinin ( CCK ) and the effect of L 364 , 718 , a specific CCK A receptor antagonist , on the metabolism of CCK were examined in dogs . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To further evaluate the role of cholecystokinin ( CCK ) in regulating acid output in humans , dose response curves were constructed to CCK 8 or G 17 ( 6 . 4 800 pmol kg 1 per h ) with and without a specific CCK A receptor antagonist ( loxiglumide ) . ^^^ These data suggest that CCK 8 directly stimulates acid secretion by binding to a CCK B / gastrin receptor on parietal cells , but at the same time inhibits acid responses by stimulating gastric somatostatin release to a CCK A receptor mediated pathway . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This study examined the effect of the CCK A receptor antagonist loxiglumide ( lox ) on gastrin or CCK induced gastric acid secretion and meal stimulated plasma gastrin levels in a placebo controlled study . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The human peptic cell muscarinic cholinergic receptor is not of the M 1 subtype , and the CCK 8 response is predominantly mediated by a CCK A receptor subtype . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present study compared the patterns of c fos protein like immunoreactivity ( FLI ) induced in rat brain by CCK and the indirect 5HT agonist dexfenfluramine ( DFEN ) , as well as the ability for devazepide , a CCK A receptor antagonist , to antagonize both anorexia and FLI induced by these agents . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In order to determine receptor domains which are important in conferring specificity for L 365260 and L 364718 we constructed by overlap PCR a rat gastrin / CCK B receptor chimaera which contained the seventh transmembrane domain of the rat CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CONCLUSIONS : The stimulation observed after the addition of CCK was the result of activation of the CCK A receptor subtype . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Consistent with this observation was our finding that the CCK A receptor selective antagonist L 364 , 718 dose dependently ( 10 ( 11 ) 10 ( 7 ) M ) inhibited CCK mediated somatostatin release but at the same doses did not alter the effect of gastrin . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Loxiglumide , ( CR 1505 ) , a newly synthesized nonpeptide CCK A receptor antagonist , D . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
N alpha Methylation at the position corresponding to Asp 32 ( CCK 33 numbering ) was consistent with high affinity , efficacy , and selectivity for the CCK A receptor . ^^^ The observation of parallel structure binding affinity profiles with respect to sites of N methylation in the C terminal regions of tetrapeptide vs heptapeptide CCK analogues suggests that the two series interact similarly with the CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Expression of the CCK A receptor gene in the pancreas and pancreatic exocrine function was examined in diabetic model rats ( OLETF ) at 5 wks of age . ^^^ Little or no CCK A receptor was detected in the pancreas of OLETF rats . ^^^ These results suggest that OLETF rats are a new experimental model for congenital deficiency of CCK A receptor in the pancreas . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This effect of CCK 8 could be reversed by Devazepide , a CCK A receptor antagonist dose dependently at 50 ng and 200 ng , and by L 365 , 260 , a CCK B receptor antagonist at 5 ng and 8 ng administered to the same site . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
After L 364 , 718 , a CCK A receptor antagonist , or ritanserin , 5 HT 2 receptor antagonist , the duration of the ileal postprandial motor pattern was reduced by 60 % . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The protective effects of systemic ceruletide were blocked , partially but significantly , by the preadministration of L 364 , 718 ( 3S ( ) N [ 2 , 3 dihydro 1 methyl 2 oxo S phenyl 1H 1 , 4 benzodiazepine 3 yl ] 1H indole 2 carboxamide , 1 10 mg / kg i . p . ) , a selective CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
However , even after 9 months of effective blockade of the CCK A receptor , mice had normal body weight and an almost normal pancreas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These analogues , which lack an acidic residue at the penultimate position , demonstrated surprisingly high CCK A receptor affinity and selectivity . ^^^ The effect of N methylation pattern on CCK A receptor affinity showed consistent trends for analogues in which n = 1 , 2 , or 3 , with the di N methylated analogues having the highest affinity in each case . ^^^ Two conformationally constrained analogues also demonstrated high CCK A receptor affinity and selectivity , as well as nearly maximal agonist activity . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Previous structure activity studies on a series of CCK A selective tetrapeptide agonists , typified by A 71623 ( Boc Trp Lys ( CONH Ph o Me ) Asp ( N Me ) Phe NH 2 ) , have shown that replacement of the Lys ( N epsilon carbamoyl ) substituent with N epsilon acyl substituents resulted in partial agonists with moderate to high affinities for the CCK A receptor and that replacement of the C terminal dipeptide with either ( N Me ) Asp Phe or ( N Me ) Asp ( N Me ) Phe was highly favorable to in vitro and in vivo CCK activity . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective CCK A receptor antagonist MK 329 reversed the inhibitory effect of the centrally as well as peripherally administered CCK 8 , or of Suc ( Thr 28 , Leu 29 , MePhe 33 ) CCK 7 , whereas the selective CCK B receptor antagonist L 365260 did not . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Distinct requirements for activation at CCK A and CCK B / gastrin receptors : studies with a C terminal hydrazide analogue of cholecystokinin tetrapeptide ( 30 33 ) . ^^^ Using 125I Bolton Hunter cholecystokinin octapeptide ( 26 33 ) ( 125I Bolton Hunter CCK 8 ) as the radioligand , A 57696 was found to be selective for cortical CCK B receptors ( IC 50 = 25 nM ) , compared with pancreatic CCK A receptors ( IC 50 = 15 microM ) . ^^^ The Kd of A 57696 at gall bladder CCK A receptors was 19 microM . ^^^ Stimulatory actions of CCK 8 and A 57696 were reversed by the CCK B selective ( R ) L 365 , 260 ( 100 nM ) , whereas at the same concentration , the CCK A selective ( S ) L 365 , 260 was ineffective . ^^^ A 57696 represents a new class of CCK A peptide antagonist at guinea pig pancreas a new class of CCK A peptide antagonist at guinea pig pancreas and gall bladder . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK 8 effects on motivational and emotional states of rats involve CCKA receptors of the postero median part of the nucleus accumbens . ^^^ These results support the neuroanatomical heterogeneity in the distribution of CCK and its binding sites in the NAS , but raise the question of the presence of CCKA receptors not detected in binding studies and of the behavioral effects mediated by CCKB receptor stimulation in this structure . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptors have high affinity for sulphated CCK 8 and for MK 329 but low affinity for desulphated CCK 8 and CCK 4 whilst CCK B sites bind MK 329 with low affinity and discriminate poorly between sulphated and desulphated CCK 8 . ^^^ CCK A receptors are found predominantly in peripheral tissues but they also exist in discrete regions of the primate CNS , including the spinal cord . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
However , it has not been established that endogenous CCK causes satiety or whether the response is mediated by peripheral type ( CCK A ) or brain type ( CCK B ) receptors . ^^^ The development of potent and selective antagonists for CCK A ( MK 329 ) and CCK B ( L 365 , 260 ) receptors now allows these issues to be addressed . ^^^ The CCK A antagonist MK 329 and the CCK B antagonist L 365 , 260 increased food intake in partially satiated rats and postponed the onset of satiety ; however , L 365 , 260 was 100 times more potent than MK 329 in increasing feeding and preventing satiety . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
It is suggested that the variable effects of MK 329 on morphine induced and opioid mediated social conflict analgesia may reflect differential , dose dependent effects at CCK B and CCK A sites respectively , a proposal consistent with the 500 fold potency difference observed between the two models . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptors in the rat interpeduncular nucleus : evidence for a presynaptic location . ^^^ Using autoradiography , ' peripheral type ' or cholecystokinin A ( CCK A ) receptor binding was measured in the interpeduncular nucleus ( IPN ) of rats which had received electrolytic lesions of the habenular nucleus . ^^^ These data suggest that CCK A receptors in rat IPN are localized on presynaptic terminals within the nucleus . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The exact locus of this interaction , or whether it involves ' peripheral type ' ( CCK A ) or ' central type ' ( CCK B ) receptors is not known . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effect of CCK 8 on aspartate levels was significantly inhibited by the CCKB antagonist , L 365 , 260 ( 20 mg kg 1 , s . c . ) , but not by the CCKA antagonist , L 364 , 718 ( 20 mg kg 1 , s . c . ) . ^^^ While the effect of CCK 8 on aspartate is selectively mediated via CCKB receptor subtype , the effect of CCK 8 on glutamate appears to be mediated via both CCKA and CCKB receptor subtypes . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The protective effects of CCK 8 were almost completely abolished by the blockage of CCK A receptors with loxiglumide , whereas the protective effect of pentagastrin was completely abolished by L 365 , 260 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Tests were undertaken with and without elimination of endogenous CCK by loxiglumide , a selective CCK A receptors antagonist , before and after eradication of H pylori with triple therapy ( omeprazole , amoxicyllin , bismuth ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These effects were induced by 5 nM CCK 8 but not BC 264 and they were blocked by the CCKA antagonist , L 364 , 718 , but not by the CCKB antagonist , L 365 , 260 . 3 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
It has been reported that certain N alpha carboxyacyl analogues of CCK 8 and of CCK 7 with a substituted Gly in position 3 or 4 of the peptide possess higher potencies at stimulating pancreatic enzyme secretion than at stimulating gallbladder contraction , suggesting that these analogues are able to differentiate subtypes of CCKA receptors . ^^^ These data demonstrate that the CCKA receptors in the pancreas and on gallbladder smooth muscle possess similar affinities for the various N alpha carboxyacyl analogues of CCK 7 and CCK 8 with a substituted Gly and provide further evidence that the CCKA receptors in gallbladder and pancreas can not be distinguished pharmacologically . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Because the dipeptoid compounds can occupy all available pancreatic CCKA receptors , these compounds must induce a configuration of the receptor different from either CCK 8 or the previously characterized partial agonist CCK JMV 180 , thereby inducing a distinct signaling pattern . ^^^ Because the dipeptoid compounds do not fully mimic CCK actions , it is likely that they interact with only some of the critical binding sites within the CCKA receptor normally occupied by CCK8 . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective CCK A antagonist L 364 , 718 ( Devazepide ) antagonized both types of contraction with a pKB of 10 . 10 and 9 . 95 , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
However , it remains unclear whether these growth effects are mediated specifically by CCK A receptors , CCK B receptors , or both . ^^^ METHODS : Rats were subcutaneously injected with either ( 1 ) CCK 8 , a nonselective CCK agonist ( 2 . 50 micrograms / kg body wt ) ; ( 2 ) A 71623 , a selective CCK A agonist , tert butyl oxycarbonyl Trp Lys ( epsilon N 2 methylphenylaminocarbonyl ) Asp ( N methyl ) Phe NH 2 ( 1 . 84 micrograms / kg body wt ) ; ( 3 ) SNF 8815 ; a selective CCK B agonist , [ ( 2R , 3S ) beta MePhe 28 , N MeNle 31 ] CCK 26 33 ( 2 . 40 micrograms / kg body wt ) ; or ( 4 ) saline ( control ) for 21 days . ^^^ Likewise , selective CCK A agonist significantly increased pancreatic weight , protein , RNA , and DNA contents , protein DNA ratio , RNA DNA ratio , pancreatic area per nucleus , and number of mitoses per 10 , 000 acinar cells . ^^^ CONCLUSION : These findings indicate that pancreatic growth is mediated specifically by CCK A receptors in the rat in vivo . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK antagonists reveal that CCK 8 and JMV 180 interact with different sites on the rat pancreatic acinar cell CCKA receptor . ^^^ The ability of CCKA antagonists to inhibit full and partial CCK agonists of the rat pancreatic acinar cell CCKA receptor has been studied . ^^^ Concurrent superfusion of either L 364 , 718 ( 0 . 1 microM ) or lorglumide ( 10 microM ) , chemically distinct , specific , potent antagonists of the CCKA receptor , resulted in a rapid inhibition of the [ Ca2+ ] 1 signal initiated by all concentrations of CCK 8 . ^^^ A model is proposed to reconcile this data , based on the assumption that JMV 180 and CCK 8 interact with discrete sites on the CCKA receptor , which are differentially affected by the binding of antagonists . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) is a gut hormone that regulates pancreatic endocrine functions via CCKA receptors . ^^^ The data indicate that some of the synthetic tetrapeptides exhibit a high affinity for the CCK receptor of the endocrine pancreas and that they are highly selective for this ( peripheral ) CCKA receptor subtype . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We showed on AR 4 2J cells that : a minority of CCKA R ( Kd = 0 . 7 nM ) , a classical CCKB R ( Kd = 0 . 93 nM ) and a new high affinity gastrin binding site ( Kd = 2 . 1 pM ) coexisted ; CCK through CCKA R and CCKB R , was more potent to stimulate amylase secretion ( EC 50 = 34 pM ) and Ca2+ mobilization ( EC 50 = 30 pM ) than to occupy its receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that CCK JMV 180 distinguishes between the CCKA receptors associated with pancreatic exocrine secretion in the acini and those involved in contraction of the isolated gallbladder smooth muscle in rabbits . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The protective effects of CCK were dose dependent and almost completely reversed by pretreatment with the specific CCKA receptor antagonist , loxiglumide , while the CCKB receptor antagonist , L 365 , 260 , was not effective . ^^^ We conclude that CCK exerts protective activity against ethanol induced damage and that this effect is mediated through specific CCKA receptors and hyperemia involving NO . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pancreatic growth and secretion were not inhibited by CCKA receptor blockade , which suggests that the effects of CCK mediated by the CCKA receptor are not essential for growth or development of the pancreatic amylase secretory response in the neonatal guinea pig . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The cyclic analogue 1a has Ki values of 4 . 5 and > 5000 nM at delta and mu opioid receptors , respectively ; and IC 50 values of 1 . 6 and > 10 , 000 nM for CCK A and CCK B receptors , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Therefore , we studied the effect of prolonged suppression of gallbladder emptying with a cholecystokinin ( CCK A ) receptor antagonist on bile formation in Richardson ground squirrels fed a trace versus a 1 % cholesterol diet . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The results confirm that the rainbow trout gallbladder CCK receptor does not distinguish sulfated CCK from sulfated gastrin as do modern CCKA receptors , but does distinguish sulfated from nonsulfated forms of both . ^^^ Finally , studies with antagonists known to be specific for either CCK or gastrin receptors in mammalian systems indicate that this ancient receptor behaves more like a mammalian CCKB receptor than as a CCKA receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To relate specific effects on growth and transformation to activation of specific affinity states of the CCKA receptor stably expressed in CHO cells we compared responses to the CCK analogues JMV 180 and CCK 8 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Identification of a region of the N terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK . ^^^ These results identify for the first time a part of the N terminal , close to the membrane , of the human CCKA receptor that is essential for the high affinity interaction with CCK . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We suggest that ( a ) pancreatic adaptation to high dietary protein is not mediated via CCK A receptors and ( b ) the stimulation of pancreatic protein secretion by a meal or by exogenous CCK 8 is mediated partly by CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that both peptides induced the synthesis of the secretory enzyme after occupancy of CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Since L 364 , 718 is known to be a powerful selective antagonist to the peripheral CCK A receptors , these data suggest that the effects produced by exogenous CCK are due to peripheral receptors that project to the NTS . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of the partial muscarinic agonist pilocarpine on physiological responses were investigated in rat pancreatic acinar cells and compared with carbachol , a full muscarinic agonist , together with previous results using JMV 180 , a partial agonist of CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These studies were undertaken to investigate if CCK A and CCK B receptors were perhaps mediating the mitogenic effects of gastrin on Swiss 3T3 cells . ^^^ Receptor antagonists that inhibit the biological effects and binding of peptides to the CCK A ( L 364 , 718 ( L 18 ) ) and CCK B ( L 365 , 260 ( L 60 ) ) receptors were ineffective toward inhibiting the binding and proliferative effects of gastrin on Swiss 3T3 cells . ^^^ Radiolabeled L 18 and L 60 demonstrated no binding to the cells , indicating that CCK A and CCK B receptors may be absent on Swiss 3T3 cells . ^^^ Possible mRNA expression of CCK A and CCK B receptor subtypes by gastrin responsive rodent intestinal and fibroblast cell lines ( Swiss 3T3 , IEC 6 , CA ) was measured by the methods of Northern blot analysis and reverse transcriptase polymerase chain reaction . mRNA from rat pancreas , AR42J cells , and rat antrum served as positive controls . ( ABSTRACT TRUNCATED AT 400 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Identification of CCK A receptors on chief cells with use of a novel , highly selective ligand . ^^^ Functional studies suggest that guinea pig chief cells have both cholecystokinin A ( CCK A ) and CCK B receptors ( CCK A R and CCK B R , respectively ) . ^^^ However , all efforts to directly characterize the specific CCK A R using binding have been unsuccessful . ^^^ Recent studies describe specific CCK A R agonists such as A 71378 ( [ desamino Nle 28 , 31 ( N methyl ) Asp 32 ] CCK heptapeptide ] . ^^^ In the present study , [ D Tyr Gly ] A 71378 was synthesized , which has > 300 fold selectivity for CCK A R and can be iodinated . [ D Tyr Gly ] A 71378 was equipotent to A 71378 in stimulating pepsinogen release from purified guinea pig chief cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK JMV 180 has been demonstrated to act as a functional agonist at high affinity pancreatic CCKA receptors but as a functional antagonist at CCKA low affinity receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The duration of MMC disruption and the increase in colonic spike burst frequency after spermidine administration ( 20 mumol ) were significantly reduced by CCK A and CCK B antagonists . ^^^ These results indicate that exogenous polyamines disrupt intestinal MMCs and stimulate colonic motility through a release of CCK acting at CCK A and CCK B receptors and suggest that endogenous polyamines are involved in the postprandial control of intestinal motility . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that peripherally administered CCK 8S has stimulatory effects on the dopaminergic system in the PNAc , and raise the possibility that the effect appears to be mediated via CCKA receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
None of the three ureido acetamides , at concentrations up to 1 microM , significantly blocked CCK 8 evoked contractions of the guinea pig ileum in vitro , a CCKA receptor bioassay . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The behavioral responses induced by BDNL were not significantly blocked by L 365 , 260 , but were suppressed by CI 988 , another selective CCK B antagonist , and by high doses of L 364 , 718 , a selective CCK A antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Use of the compound JMV 180 indicated CCK was acting through the low affinity state of the CCKA receptor to reduce CT phosphate levels . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
RESULTS : Exogenous CCK significantly reduced food intake in gastrectomized rats ; this was blocked by administration of a CCK A but not a CCK B receptor antagonist . ^^^ Chronic treatment with a CCK A or CCK B receptor antagonist after total gastrectomy in rats significantly increased postoperative food intake and body weight . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These findings support the view that exogenous CCK reduces food intake in pigs by acting , primarily , on CCKA receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This response is probably mediated through CCK A receptors because CCK 8S , but not CCK 8US , enhanced MA induced responses . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that 1 ) Both muscularly and neurally located CCK receptors are present on the longitudinal layer of chicken ceca whereas only muscular receptors are present on the circular muscle . 2 ) 5HT2 receptors seem to be involved in the neurally mediated CCK 8s response observed in the longitudinal layer . 3 ) The different potency of CCK 8s , CCK 8ns and CCK 4 to induce contractile effects and of the CCK A and CCK B antagonists to block such effects suggests the existence of two different CCK receptors on the circular layer . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Furthermore , the conditioned stimulus ( the odor ) causes behavioral change either by sensitizing a system that includes the CCKA receptor , by causing the release of endogenous CCK , or by changing some non CCK system that enhances the processing of CCKA receptor mediated information . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCKA receptor antagonist devazepide has previously been shown to inhibit vasopressin release induced in pigs by intravenous ( i . v . ) CCK . 3 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Previous i . c . v . injection of devazepide , a CCKA receptor antagonist , ( 10 micrograms kg 1 ) antagonized the inhibitory effects of both CCK 8s and igmesine injected i . c . v . on dopamine induced colonic hyperkinesia . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We transfected COS cells with cDNA for rat cholecystokinin A ( CCK A ) and different CCK B receptors and measured binding of 125I CCK 8 , [ 3H ] L 364 , 718 and [ 3H ] L 365 , 260 to characterize the different affinity states for each type of CCK receptor . ^^^ Rat CCK A and CCK B receptors , canine CCK B receptors and canine mutant CCK B ( M CCK B ) receptors in which the leucine in position 355 was replaced by valine each existed in three different affinity states for CCK 8 , high affinity , low affinity , and very low affinity . ^^^ In rat CCK A and probably CCK B receptors , most were in the very low affinity state , whereas with canine CCK B and M CCK B receptors , most were in the low affinity state . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide , a preferential CCKA antagonist , only at a high dose ( 100 micrograms / kg ) tended to increase the action of CCK 8 in the plus maze . ^^^ This peculiar interaction between CCK 8 and CCK antagonists could be explained in the light of the opposite role of CCKA and CCKB receptors in the regulation of motor activity in mice . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Microiontophoretic administration of sulfated CCK octapeptide ( CCK 8S , agonist for CCK A and CCK B receptors ) and the selective CCK B receptor agonists , CCK 4 and unsulfated CCK 8 , inhibited the firing rates of a subpopulation of SNr neurons . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
L 364718 , a CCKB receptor antagonist , had an inhibitory effect against CCK 8 when applied i . c . v . , while L 365260 , a CCKB receptor antagonist , had no influence , suggesting the apparent dominant control of CCKA receptors in the central nervous system on gastric acid secretion . ^^^ The potentiation of the acid secretory response to CCK 8 by the CCKA antagonist was completely blocked by vagotomy or atropine , as well as hexamethonium . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Optimization of this series led to the identification of an azabicyclononane amidine , L 740 , 093 [ N [ ( 3R ) 5 ( 3 azabicyclo [ 3 . 2 . 2 ] nonan 3 yl ) 2 , 3 dihydro 1 methyl 2 oxo 1H 1 , 4 benzodiazepin 3 yl ] N ' ( 3 methylphenyl ) urea ] , that bound with high affinity of CCK B receptors from guinea pig cerebral cortex ( IC 50 of 0 . 1 nM ) and had a CCK B / CCK A receptor selectivity of 16 , 000 . ^^^ In comparison , L 365 , 260 had 85 fold lower affinity ( 8 . 5 nM ) and was only 87 fold selective for CCK B over CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To examine the possible contribution of endogenous CCK mechanisms to individual differences in responsivity to AMP treatment , male Wistar rats were divided into low and high AMP responders based on a median split of their locomotor response to AMP and the effects of the selective CCK antagonists L 365 260 ( CCKB ; 0 . 01 , 0 . 1 , 0 . 5 mg / kg ; n = 16 ) and devazepide ( CCKA ; 0 . 001 , 0 . 01 , 0 . 1 mg / kg ; n = 23 ) were determined . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The recent discovery and development of CCK receptor antagonists having selective affinity for either CCKA or CCKB receptors has led to a better understanding of the functional role of CCK and its binding sites in the brain and periphery . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These facilitatory effects were reversed not only by prior administration of the delta selective antagonist naltrindole ( 0 . 5 mg / kg s . c . ) , but also unexpectedly by the selective cholecystokinin CCK A antagonist MK 329 ( 20 micrograms / kg i . p . ) . ^^^ In addition , the CCK analog [ Boc Tyr ( SO3H ) Nle Gly Trp Nle Asp Phe NH 2 ] ( a mixed CCK A / CCK B agonist ) increased the jump latency and this effect was blocked by MK 329 ( 20 micrograms / kg i . p . ) and by naloxone , but not by the selective CCK B antagonist L 365 , 260 ( 5 mg / kg i . p . ) . ^^^ Taken together , these findings suggest that the potentiating effects of delta agonists on mu mediated analgesia are due to an increase in the release of endogenous CCK interacting with CCK A and CCK B receptors and resulting in positive and negative regulation of the endogenous opioid system . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These changes appear to be mediated by cholecystokinin ( CCK ) because the increases were blocked by infusion of the CCKA receptor antagonist , MK 329 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK B antagonist L 365 , 260 ( 10 pmol 1 nmol ) failed to block the gastric vagal afferent response to gastric loads or 100 pmol CCK , while the CCK A antagonist devazepide ( 100 pmol 100 nmol ) competitively and dose dependently attenuated the response to CCK but not to gastric loads . ^^^ These data suggest that 1 ) the vagal afferent response to CCK is mediated through CCK ' s interactions with vagal , rather than pyloric , CCK A receptors , and 2 ) the vagal afferent responses to CCK and to gastric loads are mediated by dissociable , possibly independent , transduction mechanisms . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Gastrin , CCK , and their analogues also inhibit cross linking , and the spectrum of analogue affinities correlates better with the values previously reported for binding to the gastrin / CCK C receptor than with the values reported for binding to either the CCK A or the gastrin / CCK B receptor . ^^^ Cross linking is also inhibited by proglumide and benzotript , but no inhibition is seen with either the CCK A receptor selective antagonist L 364 , 718 or the gastrin / CCK B receptor selective antagonist L 365 , 260 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Gastrin stimulates growth of human colon cancer cells via a receptor other than CCK A or CCK B . ^^^ Two receptors for cholecystokinin ( CCK ) have been isolated which also bind gastrin : CCK A type and CCK B type , both are coupled to phospholipase C ( PLC ) activation . ^^^ The trophic effect was not blocked by receptor antagonists for CCK A ( L 364 , 718 ) or CCK B ( L 365 , 260 ) . ^^^ The gastrin receptor pharmacology on LoVo cells and the lack of appropriate transcripts suggest that gastrin stimulated growth of these cells by a receptor other than CCK A or CCK B type and there likely exists another receptor for gastrin . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of benzodiazepines on cholecystokinin ( CCK ) responses produced following activation of CCKB receptors by pentagastrin in the ventromedial hypothalamus ( VMH ) or CCKA receptors by CCK 8S in the dorsal raphe of the rat brain in vitro have been investigated . 2 . ^^^ In the rat dorsal raphe , where activation of CCKA receptors leads to neuronal depolarization , flurazepam also produced a weak block of the CCK response . 4 . ^^^ At central CCKA receptors , flurazepam blocked CCK 8S responses but the inhibition was not competitive , with a reduction in the peak CCK 8S obtainable in the presence of flurazepam . ^^^ These results suggest that flurazepam acts at a site other than the CCKA receptor itself to block CCK responses in the dorsal raphe . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Observed biological activities of substituted phenyl urea / thiourea tetrapeptides as agonists with the cholecystokinin alimentary canal ( CCK A ) receptor , and ( R ) 4 benzamido 5 oxopentanoic acid derivatives with both peripheral ( CCK A ) and the central ( CCK B ) ( brain ) receptors have been shown to be correlated with various physicochemical , e . g . pi , sigma , and structural , e . g . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We showed in this study that , on guinea pig brain membranes known to possess CCKB and CCKA receptors , [ 125I ] BH [ Leu 15 ] gastrin ( 5 17 ) binds to a single class of high affinity binding sites in a saturable and specific manner . [ 125I ] BH [ Leu 15 ] gastrin ( 5 17 ) interacts with guinea pig brain membranes with a maximal binding capacity that is about three fold lower than that of [ 125I ] BHCCK 8 ( CCK 8 , the C terminal octapeptide of cholecystokinin ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide ( L 364 , 718 ) , a selective antagonist of CCKA receptors , effectively blocked the action of CCK 8 ( s ) , but not that of CCK 4 ( 30 33 ) or SNF 9007 ( phase 1 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
With the availability of selective gastrin / CCKB ( L 365 , 260 ) and CCKA ( L 364 , 718 ) receptor antagonists the present study was designed to investigate the role of gastrin and cholecystokinin ( CCK ) receptors in meal stimulated gastric acid secretion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Concentration response curves to CCK 8S were shifted to the right by low concentrations of the CCKA receptor antagonist , Devazepide , but not by the CCKB receptor antagonist , L 365 , 260 , data which indicate that receptors were of the CCKA subtype . ^^^ An excess of CCK 8S inhibited binding as did Devazepide , but not L 365 , 260 , confirming that binding sites were CCKA subtype receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Binding of cholecystokinin 8 ( CCK 8 ) peptide derivatives to CCKA and CCKB receptors . ^^^ The structural requirements for the selective binding of cholecystokinin 8 ( CCK 8 ) related peptides to peripheral ( CCKA ) receptors are not sufficiently understood . ^^^ The pentapeptide derivative of CCK 8 , succinyl Tyr ( SO3H ) Met Gly Trp Met phenethylamide , was found to bind selectively with high affinity to the CCKA receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pharmacological experiments using CCK or NPY analogs suggest that both subtypes of CCK ( CCK A and CCK B ) and NPY ( Y 1 and Y 2 ) receptor binding sites are expressed by discrete populations of neurons in the nodose ganglion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effect of a novel CCKA receptor antagonist ( 2 NAP ) on the reduction in food intake produced by CCK in pigs . ^^^ The effect of a novel CCKA receptor antagonist 2 naphthalene sulphonyl L aspartyl 2 ( phenethyl ) amide , sodium salt ( 2 NAP ) on the reduction of food intake induced by exogenous CCK , administered centrally or peripherally , has been examined in pigs . 2 NAP is hydrophilic and should not readily cross the blood brain barrier . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCKB pharmacological profile as shown in competition studies by using several CCK related compounds and nonpeptide CCK antagonists discriminating between CCKA and CCKB sites . ^^^ Since rise in [ Ca2+ ] 1 noted by stimulation of C 6 cells with CCK 8S could be blocked by the CCKB receptor antagonist L 365 , 260 ( 100 nM ) but not by the CCKA receptor antagonist L 364 , 718 ( 100 nM ) , CCK induced calcium signal is triggered by activation of CCKB receptors in C 6 cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The antinociceptive activity of SNF 9007 was not a result of the activation of CCK receptors , as treatment with either CCK A or CCK B receptor antagonist was ineffective in blocking SNF 9007 antinociception . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK interaction with the gallbladder smooth muscle CCKA receptor was studied in further detail . ^^^ CCK and the CCKA gallbladder muscularis receptor are main regulators of postprandial gallbladder emptying . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Blocking CCK A receptors accelerates gastric emptying of liquid meals and abolishes the gastrocolonic reflex . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A review of the literature encompassing numerous pharmacological , physiological , and biochemical studies indicates the presence of at least four CCK receptor types , CCKA , CCKB , gastrin , and CG 4 receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A new CCK A antagonist , KSG 504 , administered intraduodenally , inhibits pancreatic secretion in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The results of the present study indicate that activation of both CCKB and CCKA receptors may prevent the development of tolerance to morphine , and the sulfate group in the CCK 8 molecule may be essential for the tolerance inhibition . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Sulfation of the tyrosine residue in CCK 8 is known to be important for its activity at CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
FPL 14294 [ 4 ( sulfoxy ) phenylacetyl ( MePhe 6 ) CCK 6 ] is a CCK analog with enhanced metabolic stability that was comparable to CCK 8 in potency to contract isolated gallbladder and in affinity at the CCK A and CCK B receptor . ^^^ Anorectic activity was inhibited by pretreatment with a CCK A antagonist ( MK 329 ) but not by a CCK B antagonist ( L 365 , 260 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Blocking of CCK A receptors by MK 329 did not significantly change the effect of GRP , whereas prevention of secretin release by removal of the small intestine caused a 13 fold reduction in the GRP induced pancreatic bicarbonate secretion and completely abolished the effect on hepatic bicarbonate secretion but did not change the effect on pancreatic protein secretion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Administration of the selective CCKA receptor antagonist MK 329 , but not the CCKB receptor antagonist L 365 , 260 , prior to CCK injection , prevented oxytocin release as measured by radioimmunoassay and oxytocin neuronal activation as measured by electrophysiology and by the lack of induction of c fos mRNA . 3 . ^^^ We conclude that CCK acts on CCKA receptors , either in the area postrema or on peripheral endings of the vagus nerve , to cause the release of hypothalamic oxytocin and ACTH . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Saturation and competitive binding studies were carried out using sulphated CCK 8 and two selective CCK receptor antagonists : MK 329 , to define type A ( CCKA ) binding sites ; and , L 365 , 260 , to define type B ( CCKB ) binding sites . ^^^ However , both MK 329 ( IC 50 = 18 nM ) and L 365 , 260 ( IC 50 = 45 nM ) competed for vagal 125I CCK binding indicating the presence of CCKA and CCKB binding sites . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Furthermore , the selective CCKA antagonist CAM 1481 inhibited the increase in [ Ca2+ ] 1 induced by CCK 8 ( half maximal inhibitory concentration = 3 nM ) in GLC 19 but not in H 510 cells . ^^^ Thus , the effects of CCK 8 are mediated through CCKA receptors in GLC 19 cells and via CCKB / gastrin receptors in H 510 cells . ^^^ Our results show , for the first time , that CCKA receptors can mediate Ca2+ mobilization and growth in SCLC cells and that SCLC cells express two distinct functional CCK receptor subtypes . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These effects were blocked by the CCK A antagonist MK 329 ( 0 . 02 mg / kg ) , supporting the involvement of CCK A receptors in CCK induced analgesia . ^^^ The results suggest that activation of CCK A receptors by BDNL leads to antinociceptive responses indirectly mediated by stimulation of mu opioid receptors by endogenous enkephalins . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCKA receptor mediates classical CCK like effects on the gut . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Derived by reasoned modification of the CCK A selective 3 carboxamido 1 , 4 benzodiazepine , MK 329 , this paper chronicles the development of potent , orally effective compounds in which selectivity for the CCK B receptor subtype was achieved . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
KSG 504 , a new synthetic cholecystokinin ( CCK ) receptor antagonist derived from proglumide , has superior selectivity and affinity to CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The use of selective CCK antagonists has allowed to establish that the gastric motor effect of the peptide is direct and mediated through the stimulation of CCK A receptors . ^^^ As a consequence , CCK A antagonism results in acceleration of emptying rate under certain experimental and clinical conditions . ^^^ This peculiar pharmacologic effect of CCK A antagonists , which could be useful in the treatment of functional dyspepsia ( idiopathic or diabetic ) , gastroparesis and gastro esophageal reflux disease ( where patients often display a delayed emptying rate of solid food ) needs to be further investigated , in order to fully explore their potential as gastrokinetic drugs . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In addition , icv administration of CCKA but not CCKB receptor antagonist prevents meal and CCK 8 induced colonic hyperkinesia in dogs . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK A ) and gastrin ( CCK B ) receptors have been demonstrated in the azaserine induced rat pancreatic carcinoma DSL 6 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Recent studies have suggested that this growth promoting effect of CCK was initiated through the occupation of the CCKA receptor . ^^^ As an answer to the first question , rats were infused with CCK JMV 180 , a CCKA high affinity agonist , at doses of 50 , 100 , 150 , and 300 micrograms . kg 1 . h 1 , or Cae ( 0 . 25 micrograms . kg 1 . h 1 ) for 4 days . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
No binding was detected with the CCK A antagonist [ 3H ] L 364 , 718 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Energy calculations were performed for CCK 8 ( Asp 26 Tyr ( SO 3 ) 27 Met 28 Gly29 Trp 30 Met31 Asp 32 Phe33 NH 2 , 1 ) and [ desaminoTyr ( SO 3 ) 27 , Nle 28 , 31 ] CCK 7 ( 2 ) , which are nonselective ligands of CCK receptors , and for the CCK A selective analog [ desaminoTyr ( SO 3 ) 27 , Nle 28 , 31 , N Me Asp 32 ] CCK 7 ( 3 ) and the CCK B selective analog [ desaminoTyr ( SO 3 ) 27 , Nle 28 , N Me Leu 31 ] CCK 7 ( 4 ) . ^^^ The proposed models are consistent with the results of biological testing for CCK related peptides including cyclic analogs and CCK A selective tetrapeptides . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective non peptide CCKB receptor antagonist L 365 , 260 was more potent than the selective CCKA receptor antagonist MK 329 in inhibiting the [ Ca2+ ] 1 mobilization elicited by 10 nM CCK 8 with IC 50 values of 20 + / 8 nM and 400 + / 100 nM , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Injection of the CCK A antagonist L 364 , 718 30 min before CCK 8 injection eliminated c fos expression in these regions . ^^^ These findings support the hypothesis that CCK 8 induced c fos expression is mediated by CCK A receptors . ^^^ Meal induced c fos expression was not blocked by the CCK A antagonist L 364 , 718 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The cholecystokinin ( CCK ) family of peptides and receptors are present throughout the brain and gastrointestinal tract and can be pharmacologically subdivided into two subtypes : CCKA and CCKB . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Intra accumbens infusion of CCK ( 10 ng ) , or s . c . administration of the CCKA receptor antagonist devazepide had no effect upon response rates . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present study was performed to determine whether these effects are mediated by way of CCK A receptors , CCK B receptors , or both . ^^^ Both CCK octapeptide and the selective CCK A agonist tert butyloxycarbonyl Trp Lys ( epsilon N 2 methylphenylaminocarbonyl ) Asp ( N methyl ) Phe NH 2 stimulated pancreatic growth and the development of acidophilic atypical acinar cell foci and nodules . ^^^ Furthermore , the effect produced by the selective CCK A agonist tert butyloxycarbonyl Trp Lys ( epsilon N 2 methylphenylaminocarbonyl ) Asp ( N methyl ) Phe NH 2 was greater than that produced by CCK octapeptide . ^^^ These findings suggest that the growth of putative preneoplastic lesions ( acidophilic atypical acinar cell foci and nodules ) in the rat pancreas during the early stages of azaserine induced pancreatic carcinogenesis is mediated specifically by way of CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The role of cholecystokinin ( CCK ) as a central and peripheral satiety factor was studied using the CCK B ( L 365 , 260 ) and CCK A ( MK 329 ) receptor antagonists in esophageal fistula dogs . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide powerfully blocked responses to CCK 8S with an affinity ( pKB = 9 . 54 ) that was in agreement with reported functional data obtained in pancreatic amylase secretion studies , a system exhibiting CCKA receptor activity . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Neither an inactive analog ( LY 206890 ) nor a CCK A selective analog ( LY 219057 ) affected the number of spontaneously active A 10 DA cells . ^^^ The diphenylpyrazolidinone CCK B antagonists , but neither the inactive nor the CCK A selective analog , also decreased the number of spontaneously active A 9 DA cells ; however , none of these compounds produced catalepsy in awake animals . ^^^ These results indicate that the firing of A 9 and A 10 DA neurons is suppressed specifically by antagonism of CCK B , but not CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Operant feeding was recorded in 18 h deprived pigs after peripheral ( 4 ) or central ( ICV ) administration of saline , the CCK A agonist A 71378 , the CCK B agonist pentagastrin , or pentagastrin vehicle . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Extracellular single unit recording techniques were used to study the effects of the cholecystokinin A ( CCK A ) antagonist , L 364 , 718 , and the CCK B antagonist , PD 134308 , on DA neuronal activity in chloral hydrate anesthetized rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In this study we used JMV 180 to evaluate the potential participation of these two CCK A sites in the satiety effect of CCK 8 in rats and mice . ^^^ Both CCK 8 and JMV 180 induced suppression of food intake were attenuated by the CCK A antagonist MK 329 ( 24 . 8 nmol / kg ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective CCKA receptor antagonist L 364 , 718 potently inhibited CCK 8S induced slow depolarizations ( IC 50 2 . 9 pM ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A antagonist completely blocked LH secretion in response to CCK , whereas the CCK B antagonist had no effect . ^^^ To assess whether endogenous CCK , released in response to food intake , stimulates LH secretion , six monkeys were fasted for 1 day and then provided with a normal meal of monkey chow ( i . e . a refeed meal ) the following day , with either no antagonist , CCK A antagonist , or CCK B antagonist administered 30 min before the meal . ^^^ The refeed meal led to a comparable stimulation of LH secretion regardless of whether monkeys received no antagonist ( 3 . 7 + / 0 . 44 LH pulses / 9 h ) , CCK A antagonist ( 3 . 33 + / 0 . 56 LH pulses / 9 h ) , or CCK B antagonist ( 4 . 0 + / 0 . 78 LH pulses / 9 h ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK stimulated acid secretion was not blocked by L 365 , 260 , a CCKB / gastrin receptor antagonist , and was significantly increased by devazepide , a CCKA receptor antagonist , given alone or together with L 365 , 260 . ^^^ We conclude : 1 ) pentagastrin stimulates acid secretion through a gastrin type receptor , but CCK may not , and 2 ) pentagastrin and CCK can stimulate acid secretion despite simultaneous blockade of CCKB / gastrin and CCKA receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
COS cells transfected with this cDNA clone bound CCK 8 and L 364 , 718 with high affinities appropriate for the CCKA receptor , and exhibited a transient increase in intracellular calcium in response to CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This study provides evidence that CCK exerts an inhibitory effect on gastric acid secretion and plasma gastrin release as well as a stimulatory influence on the release of PP and somatostatin via CCK A receptors but does not influence directly insulin or glucagon secretion in man . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present results suggest that the activation of CCKA and CCKB receptors by endogenous CCK , could play an opposite role in the control of behavioral responses induced by endogenous enkephalins . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The compounds tested were selective CCK B antagonists [ CI 988 ( 0 . 01 1 mg / kg SC ) , L 365 , 260 ( 0 . 004 2 mg / kg IP ) and LY 262 , 691 ( 0 . 001 1 mg / kg SC ) ] , CCK B agonists [ CCK 4 ( 0 . 01 1 mg / kg SC ) and BC 264 ( 0 . 004 1 mg / kg IP ) ] and CCK A antagonists [ devazepide ( 0 . 001 1 mg / kg SC ) and lorglumide ( 0 . 01 1 mg / kg SC ) ] . ^^^ None of these drugs induced the expected behavioural effects , i . e . an anxiolytic like release of the behavioural suppression with CCK B and , possibly , CCK A antagonists and / or a further reduction of lever pressing with CCK B agonists , indicative of an anxiogenic like potential . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin applied iontophoretically as the sulfated octapeptide ( CCK 8S ) or as highly selective CCKA and CCKB agonists induced excitatory as well as inhibitory effects on dorsal lateral geniculate unit activity . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine what subtype ( s ) of CCK receptors are involved in antagonizing the antinociception induced by these opioids , effect of lorglumide sodium salt ( a CCKA receptor antagonist ) or PD 135 , 158 N methyl D glucamine salt ( a CCKB receptor antagonist ) on opioid induced inhibition of the tail flick response was examined . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A series of new spiroglumide amido acid derivatives was synthesized and evaluated for their ability to inhibit the binding of cholecystokinin ( CCK ) to guinea pig brain cortex ( CCKB receptors ) and peripheral rat pancreatic acini ( CCKA receptors ) , as well as to inhibit in vitro the gastrin induced Ca2+ increase in rabbit gastric parietal cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The demonstration that systemic administration of the CCKA receptor antagonist , devazepide , increases food intake in rats has provided the strongest support for the hypothesis that endogenous peripherally released cholecystokinin ( CCK ) acts as a satiety factor . ^^^ The present study was therefore undertaken to confirm the hypothesis that endogenous peripheral CCK is a satiety factor by investigating the effects of a novel CCKA receptor antagonist , 2 NAP , which is unlikely to cross the blood brain barrier , on food intake in rats . 2 . 2 NAP ( 1 16 mg kg 1 , i . p . ) had no significant effects on the intake of a test meal in rats . 3 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In vitro binding studies showed that some derivatives exhibited potent affinity for gastrin CCK B receptor and high selectivity over peripheral CCK ( CCK A ) receptor . ^^^ Structure activity relationship studies of this series suggested that 1 [ ( R ) 2 , 3 dihydro 1 ( 2 , 3 dihydro 1 ( 2 methylphenacyl ) 2 oxo 5 phe nyl 1H 1 , 4 benzodiazepin 3 yl ] 3 ( 3 methylphenyl ) urea ( 35b , YM 022 ) was the optimal compound with IC 50 values of 0 . 17 , 0 . 11 and 150 nM for gastrin , CCK B and CCK A receptors , respectively , and an ED 50 value of 9 . 5 nmol / kg ( i . v . ) in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The sulphated octapeptide C terminal fragment of cholecystokinin ( CCK 8S ) is present in high concentration in the mammalian brain , where it acts via two types of receptor denoted CCKA and CCKB . ^^^ Using in vivo extracellular unitary recordings of CA 3 pyramidal hippocampal neurons , we compared the effect of SNF 8702 , a potent selective CCKB receptor agonist , to that of CCK 8S , and assessed the effects of selective CCKA and CCKB antagonists . ^^^ Both CCK 8S and SNF 8702 induced activations were suppressed by the microiontophoretic application of the CCKB antagonist CI 988 , but not by that of the CCKA antagonist SR 27897 . ^^^ CCK 8S induced activation was not significantly modified by the intravenous administration of the CCKA antagonists devazepide and SR 27897 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
MATERIALS AND METHODS : Male NMRI mice weighing 12 15 g were assigned to six groups ( 10 mice / group ) which were treated with different combinations of 0 . 9 % NaCl , omeprazole , a CCK A antagonist , a CCK B antagonist , loxiglumide , and L 365 , 260 for 10 days each according to different protocols . ^^^ RESULTS : Omeprazole caused a marked , 10 fold increase in serum gastrin which was not affected by the gastrin antagonist , but markedly reduced by the CCK A antagonist . ^^^ In contrast , the CCK A antagonist significantly decreased pancreatic weight and protein content . ^^^ The inhibitory effect of loxiglumide on omeprazole induced increase in serum gastrin might be explained by recent findings which showed that CCK A antagonists can stimulate gastric acid secretion probably due to a reduction of the inhibitory effect of basal CCK on the D cell and its somatostatin release . ^^^ Probably such a slight stimulation of gastric acid secretion caused by the CCK A antagonist might reduce the gastrin increase caused by omeprazole ' s abolishment of acid secretion . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We then used the type A cholecystokinin ( CCK A ) receptor antagonist devazepide to assess the importance of CCK in mediating the anorexia produced by oleic acid . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Peptoid CCK receptor antagonists : pharmacological evaluation of CCKA , CCKB and mixed CCKA / B receptor antagonists . ^^^ In radioligand binding assays , the dipeptoid PD 135666 ( ( benzenebutanoic acid , beta [ [ 3 ( 1H indol 3 yl ) 2 methyl 1 oxo 2 [ [ ( tricyclo [ 3 . 3 . 1 . 1 ( 3 , 7 ) ] dec 2 yloxy ) carbonyl ] amino ] propyl ] amino ] , [ R ( + * , S * ) ] ) selectively inhibited [ 125I ] Bolton Hunter CCK 8 binding to CCKB receptors in mouse cerebral cortex ( CCKB IC 50 = 0 . 1 nM ) but was weaker as an inhibitor of CCKA receptor binding in the rat pancreas ( IC 50 = 26 nM ) . ^^^ These data suggest that the anxiolytic effects of CCK receptor antagonists parallel their affinity for the CCKB rather than the CCKA receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aim of this study was to assess the role of cholecystokinin ( CCK ) A receptors in these changes using a CCK A antagonist loxiglumide . ^^^ CONCLUSIONS : CCK A receptors are involved in the induction of meal like fullness and nausea associated with intraduodenal lipid and gastric distention . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
For example , CCK appears to exert its anti opioid actions mainly through the activation of CCK B receptors , whereas its opioid like effects seem to result from the stimulation of CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK B antagonists suppressed CCK 4 induced calcium mobilization more potently than CCK A antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Additional experiments indicated that , as with feeding , CCK 8S inhibits water intake by an action at peripheral CCKA receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Both CCK A and CCK B receptor subtypes were visualized in the nucleus of the solitary tract and the area postrema of normal rats , but levels of binding to both of these subtypes were unaffected by the experimental treatments . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
TP 680 showed approximately 2 and 22 times greater selectivity for peripheral CCKA receptors relative to brain CCK ( CCKB ) receptors than MK 329 and loxiglumide , respectively , when IC 50 values for inhibition of [ 125I ] CCK 8 binding in isolated acini and cerebral cortex were compared . 3 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Several roles of CCKA and CCKB receptor subtypes in CCK 8 induced and LiCl induced taste aversion conditioning . ^^^ Because CCK 8 has affinity for both CCKA and CCKB receptor subtypes , we wanted to determine the subtype involved in CCK 8 induced TAC . ^^^ Pretreatment with the selective CCKA antagonist MK 329 ( L 364 , 718 or devazepide ) , at doses of 0 . 1 , 1 . 0 , or 10 . 0 mumol / kg , markedly antagonized ( > 70 % ) CCK 8 induced TAC . ^^^ Considering the existing data on the induction of TAC by various CCK analogues , we consider an action of CCK 8 on peripheral CCKA , but not CCKB , receptors necessary for the induction of TAC . ^^^ Our results of partial antagonism of CCK 8 and LiCl induced TAC by L 365 , 260 , CI 988 , or MK 329 suggest , but do not prove , that both CCKA and CCKB mechanisms may be operative during TAC . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK ( 1 nM 1 microM ) caused concentration dependent depolarisations when superfused over the nodose ganglion at 37 degrees C as measured by a silicone grease gap technique , and both CCKA antagonists caused significant rightward shifts in the concentration response curve to CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCKB antagonist PD 135158 reduced the CCK effects in 10 of 14 cells ; the CCKA antagonist KL 1001 reduced the CCK effects in 17 of 36 cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) is co localized with dopamine ( DA ) in portions of the mesolimbic system , where it may facilitate the function of DA through the CCKA receptor subtype . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To test whether the mechanism involved is dependent upon action at type A or type B CCK receptors , we examined the ability of CCKA ( devazepide ) and CCKB ( L 365 , 260 ) receptor antagonists to attenuate the suppression of sham feeding by intraintestinal oleic acid , maltotriose , or L phenylalanine . ^^^ Suppression by oleic acid or maltotriose was dose dependently attenuated by intraperitoneal administration of the CCKA receptor antagonist , as was suppression by exogenous CCK . ^^^ These results suggest that suppression of sham feeding by intestinally infused oleic acid and maltotriose is mediated by endogenous CCK acting at CCKA receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In conclusion , it is considerable that postprandial CCK induced gallbladder contractions are controlled through CCK A receptors both on the vagal nerve in stimulating endogenous release of acetylcholine and on the gallbladder directly to stimulate muscle contraction in the dog . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
L 364 , 718 ( a CCK A antagonist ) showed a relative selectivity and a high affinity for those receptors located in central tissues , whereas L 365 , 260 ( a CCK B antagonist ) is almost inactive in all studied tissues . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These compounds displayed micromolar affinities for CCK A rather than CCK B receptor and the results have been discussed on the basis of a molecular modelling study . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCKB receptor preferring agonists gastrin 17 1 , desulfated CCK 8 and CCK 4 had only small stimulatory effects ( < 12 % of maximal CCK 8 effect , EC 50 ' s in the low nanomolar range ) and did not inhibit the CCK 8 response , suggesting that they were acting at CCKB but not , as partial agonists , at CCKA receptors . ^^^ These results suggest that CCK effects on [ Ca2+ ] 1 of porcine chief cells are mainly ( > 80 % ) mediated via CCKA receptors , which differ from guinea pig and rabbit chief cell receptors by a higher distinction capacity between selective CCKA and CCKB , receptor agonists ( A 71378 versus A 72962 ) and antagonists ( L364 . 718 versus L365 . 260 ) and by the apparent lack of activation by desulfated CCK 8 and gastrin 17 1 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The 2 gastrointestinal peptides cholecystokinin ( CCK ) and gastrin , which act through CCK A receptors ( having high affinity for CCK ) or CCK B / gastrin receptors ( having high affinity for CCK and gastrin ) , are considered to be important tumor growth factors . ^^^ We have evaluated CCK A and CCK B / gastrin receptors in 34 human thyroid cancers using in vitro receptor autoradiography with 2 different radioligands . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
It is possible that this effect of EB is due to upregulation of CCKA receptors in the terminals of vagal afferent fibers because these receptors have been implicated in the mediation of the satiating effect of intraperitoneally injected CCK 8 . ^^^ As additional measures of EB ' s effects on CCK receptors , we also characterized EB ' s effects on CCK . 8 binding in the area postrema ( AP ) , a brain region rich in CCKA receptors , the ventromedial hypothalamus ( VMH ) , a region rich in CCKB receptors , and in the pancreas , a gland rich in CCKA receptors . ^^^ Furthermore , competition experiments with 500 nM of the selective CCKA receptor antagonist devazepide or the selective CCKB antagonist L 365 , 260 demonstrated that EB failed to affect CCK receptor subtype number in the medial and lateral divisions of the NTS . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine the role of GABAergic neurotransmission in cholecystokinin octapeptide ( CCK 8 ) induced contraction of the guinea pig ileal longitudinal muscle myenteric plexus preparation , CCKA or CCKB receptors were protected by L 364 , 718 and L 365 , 260 , respectively . ^^^ CCKA receptor protection alone decreased contractile responses to CCK 8 , and additional protection of GABAA receptors resulted in restoration of the contractile responses at high concentrations of CCK 8 . ^^^ The results suggest that the CCKA and CCKB receptors that mediate the contractile action of CCK differ with regard to GABAergic neurotransmission . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
AIMS : The effect of two recently developed CCK receptor antagonists , namely dexloxiglumide and spiroglumide , on gastric emptying and secretion as well as their selectivity towards CCKA and CCKB receptors in vivo was studied in the rat . ^^^ RESULTS : The putative CCKA antagonist , dexloxiglumide , administered by intravenous route , was able to inhibit CCK 8 induced delay of gastric emptying in a dose dependent fashion , with an ID 50 ( 95 % CL ) of 1 . 14 ( 0 . 84 1 . 53 ) mg / kg . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Moreover , both CCKA and CCKB receptor mechanisms have been implicated in CCK ' s effects on feeding . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results demonstrate that endogenous and exogenous CCK delays gastric emptying of liquids through stimulation of CCKA receptors and suggest that adaptation of the gastric motor response to CCK does not occur . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In contrast , L 364 , 718 , a CCK A antagonist in mammals , shows this effect only at very high dose levels . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine whether this behavior was intrinsic to a single receptor protein we studied the binding affinity of CHO cells stably transfected with a cloned rat CCKA receptor . 125I CCK binding to intact cells at 37 degrees C revealed two affinity states for CCK of Kd values 20 pM and 2 . 4 nM . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
By mapping the distribution of cholecystokinin ( CCK ) receptor types onto an established phylogenetic hypothesis of vertebrate relationships , we tested two hypothesis about the evolution of CCK receptors : ( 1 ) A single CCK receptor type , CCK 10 , is the ancestral receptor , while CCK A and CCK B receptors represent derived receptor types ; ( 2 ) the evolution of two separate CCK receptors is functionally related to the evolution of endothermy . ^^^ Additional competitive inhibition studies showed that the mako CCK 10 receptor has very low affinities for the following nonpeptide agonist and antagonists : A 71623 , L 364 , 718 , A 57696 , A65186 . 72 , Cam 1481 , and SR 27897B ( specific for some mammalian CCK A receptors ) and L 365 , 260 and CI 988 ( specific for some mammalian CCK B receptors ) , confirming the pharmacological differences between the CCK 10 receptor and the CCK A and B receptors . ^^^ CCK A and CCK B , are not part of the suite of characters necessary for evolution of endothermy in fishes . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Suppression of SKF 38393 induced grooming and vacuous chewing movements by CCK 8S was blocked by the selective CCKA receptor antagonist MK 329 ( also known as devazepide or L 364 , 718 ) ( 0 . 1 , 0 . 3 mg / kg i . p . ) but unaffected by the CCKB receptor antagonist L 365 , 260 ( 0 . 1 , 0 . 3 mg / kg i . p . ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The specific CCK A and secretin receptors expressed in normal pancreata were markedly reduced in pancreatic preneoplastic lesions and absent in adenocarcinomas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that CCK 8 activates at least two different channels , a Ca ( 2+ ) dependent Cl channel and a non selective cation channel in oocytes expressing the CCKA receptor , while the CCKB receptor elicits only a Ca ( 2+ ) dependent Cl channel . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCKA binding profile as shown in competition studies by using different CCK related compounds and non peptide CCK antagonists discriminating between CCKA and CCKB sites . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The preparation of the dehydropeptides ( 1 , R = Me ; 2 , R = H ) and the cyclopropylpeptides ( 3 , R = Me ; 4 , R = H ) possessing good binding affinities for the CCK A and CCK B receptors is described . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The overlapping distribution of opioid and cholecystokinin ( CCK ) peptides and their receptors ( mu and delta opioid receptors ; CCK A and CCK B receptors ) in the central nervous system have led to a large number of studies aimed at clarifying the functional relationships between these two neuropeptides . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A variety of experimental evidence suggests that exogenously applied CCK , acting at the CCKA receptor , potentiates the function of DA in the NAC . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The response to 100 pmol CCK was completely abolished by devazepide ( 0 . 5 mg kg 1 ) and by chronic subdiaphragmatic vagotomy performed 10 14 days prior to experimentation , indicating that CCK sensitivity was via CCKA receptors and exclusively mediated via vagal afferents rather than splanchnic or enteric afferents . 4 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These data therefore do not support the postulate that CCK acting via CCKA or CCKB receptors modulates release of GABA under the present experimental conditions . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Competition binding by agonists and antagonists of CCKA and CCKB / gastrin receptors demonstrated the presence of two distinct binding components , sites presenting a high affinity for [ Thr , Nle ] CCK 9 , gastrin , PD 135158 , L 365 , 260 and a low affinity for MK 329 , SR 27897 , and sites presenting a high affinity for [ Thr , Nle ] CCK 9 , MK 329 , SR 27897 and a low affinity for gastrin , PD 135158 , L 365 , 260 . 5 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A meal disrupts migrating motor complexes ( MMC ) in the rat intestine through stimulation of peripheral cholecystokinin ( CCK ) B and central CCK A receptors . ^^^ This initiates a reflex including stimulation of central CCK A receptors . ^^^ Exogenous CCK also stimulates peripheral CCK A receptors not located in capsaicin sensitive vagal afferent fibers . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Direct contractile effect of cholecystokinin octapeptide on caecal circular smooth muscle cells of guinea pig via both CCK A and CCK B / gastrin receptors . ^^^ This study strongly suggested the presence of both CCK A and CCK B / gastrin receptors in caecal circular smooth muscle cells of guinea pig , and that the contractile effect of CCK 8 on these cells was mediated via both of these receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
BACKGROUND & AIMS : Gastrin and cholecystokinin ( CCK ) are gut brain peptides , with multiple functions in the gastrointestinal tract mediated through CCK B gastrin and CCK A receptors . ^^^ The aim of this study was to investigate the distribution and pharmacological characteristics of CCK A and CCK B receptors in the human upper gastrointestinal tract and compare them with those in the rat and dog . ^^^ CCK A receptors were found in the basal region of the antral and fundic mucosa . ^^^ CCK A receptors were also located in the muscularis propria of antrum , fundus , and gallbladder , whereas CCK B gastrin receptors were only detected in gastric fundic circular muscle . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptors were expressed rarely in tumors except in gastroenteropancreatic tumors ( 38 % ) , meningiomas ( 30 % ) , and some neuroblastomas ( 19 % ) . ^^^ The identified CCK A and CCK B receptors were specific and of high affinity in the subnanomolar range . ^^^ The rank order of potency of various CCK analogues was : sulfated CCK 8 = L 364 , 718 > > nonsulfated CCK 8 = L 365 , 260 > or = gastrin for CCK A receptors and sulfated CCK 8 > gastrin = nonsulfated CCK 8 > L 365 , 260 > L 364 , 718 for CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present study examined roles of endogenous cholecystokinin ( CCK ) and CCK A receptors in the regulation of pancreatic exocrine secretion and gastroduodenal motility in conscious sheep during interdigestive period . ^^^ These results suggest that endogenous CCK contributes to the regulation of interdigestive pancreatic exocrine secretion , omasal contractions and duodenal MMC in the ovine gastrointestinal tract via CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
During the diluting period , inhibition of GB contractions by a CCKA receptor antagonist , atropine or hexamethonium , resulted in concentration of GB bile , whereas during the concentrating period , CCK 8 shifted the concentration process back to dilution . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the second set of experiments , the effect of cholecystokinin ( CCK ) CCKA and CCKB receptor antagonists , devazepide and L 365260 , on citalopram induced decrease of exploratory behaviour in the elevated plus maze was studied . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Unstimulated CCK receptors remained on the surface of both recombinant stable rat CCK A receptor bearing Chinese hamster ovary cell line ( CHO CCKR ) cells and native rat pancreatic acinar cells and did not constitutively internalize . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCKA receptor on pancreatic acini has a greater affinity for sulfated CCK than for gastrin , while the gastrin / CCKB receptor in gastric mucosa and brain has similar affinities for both gastrin and CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Systemic pretreatment with the CCKB antagonist , L 365 , 260 , but not with the CCKA antagonist , L 364 , 718 , significantly antagonised the effect of CCK 8S on cortical dynorphin B and aspartate release . ^^^ Thus , the present results indicate that cortical CCK release exerts a stimulatory modulation on cortical dynorphin B and aspartate release via the CCKB receptor subtype , and on glutamate release via both CCKA and CCKB receptor subtypes . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Because in the initial report of naloxone ' s potentiation of CCK a relatively high , nonphysiologic dose of CCK ( i . e . , 13 micrograms / kg ) was used as the training drug , in the current analysis subjects were trained to discriminate 5 . 6 micrograms / kg CCK from its vehicle and the assessments and comparisons of the effects of naloxone and naltrindole were based on this dose . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A series of 2 aralkyl 4H pyridothiadiazine 1 , 1 dioxides and 3 aralkylamino 2 aryl 2H pyrido [ 4 , 3 e ] 1 , 2 , 4 thiadiazine 1 , 1 dioxides structurally related to quinazolinone CCK receptor antagonists were synthesized and evaluated as CCK A and CCK B receptor ligands . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
IQM 95 , 333 displaced [ 3H ] CCK 8S binding to CCKA receptors from rat pancreas with a high potency in the nanomolar range . ^^^ Like devazepide , IQM 95 , 333 was a more potent antagonist of CCK 8S than of CCK 4 induced contraction of the longitudinal muscle from guinea pig ileum , suggesting selective antagonism at CCKA receptors . 4 . ^^^ IQM 95 , 333 and devazepide were also potent inhibitors of CCK 8S stimulated amylase release from isolated pancreatic acini , a CCKA receptor mediated effect . ^^^ Low doses ( 50 100 micrograms kg 1 , i . p . ) of IQM 95 , 333 and devazepide , without any intrinsic effect on food intake or locomotion , blocked the hypophagia and the hypolocomotion induced by systemic administration of CCK 8S , two effects associated with stimulation of peripheral CCKA receptors . 6 . ^^^ In conclusion , IQM 95 , 333 is a potent and selective CCKA receptor antagonist both in vitro and in vivo with an anxiolytic like activity in two different animal models , which can only be attributed to blockade of this CCK receptor subtype . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Acetylcholine and CCK agonists ( the CCKA receptor agonists A 71378 and A 71623 ; the CCKB receptor agonist Suc CCK 4 ) were iontophoretically administered alone and in combination . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of cholecystokinin ( CCK ) CCKA receptor antagonist devazepide ( 10 micrograms / kg and 1 . 0 mg / kg ) , CCKB receptor antagonist L 365260 ( 1 . 0 mg / kg ) , and CCKB receptor agonist CCK tetrapeptide ( CCK 4 , 75 micrograms / kg ) , and their concomitant administration with antidepressants desipramine ( 10 mg / kg ) and citalopram ( 10 mg / kg ) on rat exploratory behaviour were studied in the recently developed exploration box test . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
There are two CCK receptors ; both CCK A and CCK B receptors are stimulated by CCK 8 SE . ^^^ The relative importance of the CCK A and CCK B receptors in the somnogenic and hypothermic effects of CCK 8 SE is not well understood . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin depolarizes guinea pig sphincter of Oddi neurons by activating CCK A receptors . ^^^ CCK induced depolarization was significantly reduced by a CCK A , but not a CCK B , receptor antagonist . ^^^ It is concluded that CCK can act on CCK A receptors to depolarize SO neurons . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A and CCK B antagonists , devazepide and L 365260 ( 100 micrograms / kg , i . p . ) , respectively , inhibited the postprandial colonic motor response while only L 365260 reduced the CCK induced stimulation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results indicate that CCK A type receptors rather than CCK B receptors may be involved in CCK induced insulin secretion in sheep . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To test the possible role of cholecystokinin ( CCK ) in the decrease of social exploration induced by intraperitoneal ( IP ) injection of lipopolysaccharide ( LPS , 100 microg / kg ) , mice were pretreated with IP or intracerebroventricular ( ICV ) injection of the CCKA receptor antagonist L 364 , 718 ( 3 mg / kg and 10 microg / kg , respectively ) and the CCKB receptor antagonist L 365 , 260 ( 1 mg / kg and 10 microg / kg , respectively ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
All subjects were studied twice , in a randomized , double blind study , during intravenous infusion of either loxiglumide ( CCK A antagonist ) or saline . ^^^ Endogenous CCK or CCK A receptors therefore play a role in the fat induced reduction of intragastric pressure and might also modulate gastric perception after lipid . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We investigated cell proliferation modulated by cholecystokinin ( CCK ) and somatostatin analogue RC 160 in CHO cells bearing endogenous CCKA receptors and stably transfected by human subtype sst 5 somatostatin receptor . ^^^ These effects are positively regulated by CCK and negatively influenced by RC 160 , interacting through CCKA and sst 5 receptors , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A antagonist loxiglumide at 20 mg / kg , a dose which abolished the action of all caerulein doses on food intake , failed to alter the food intake either in obese or in lean rats when given without an agonist . ^^^ However , the failure of the CCK A antagonist to increase food intake questions whether any of the effects of exogenous CCK are of physiological relevance . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK 8S induced Ca increases were blocked by the CCKB receptor antagonist PD 135158 ( 100 nM ) but not by the CCKA antagonist lorglumide ( 100 nM ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
When tested by radioreceptor assay , a synthetic replicate of alligator gastrin 49 exhibited a gastrin like pattern of biological activity on mammalian CCK A and CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
METHODS : Thirty day old male rats were pairfed for 10 days with lactalbumin as a control diet or lactalbumin plus PHA or purified soybean trypsin inhibitor ( STI ) as a positive control ( 42 mg / rat / day ) with or without 20 micrograms of the cholecystokinin A ( CCK A ) antagonist MK 329 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These behavioural effects , prevented by the prior i . p . administration of the CCK B antagonist L 365 , 260 but not by the CCK A antagonist L 364 , 718 , were shown to depend on dopaminergic systems , since they were blocked by D 1 ( SCH 23390 , 25 microg / kg i . p . ) or D 2 ( sulpiride , 50 or 100 mg / kg i . p . ) antagonists . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
METHODS : The effect of the CCK A antagonist loxiglumide ( LOX ) on GE and motility was studied using magnetic resonance imaging in six healthy volunteers after ingestion of 500 ml Intralipid 10 % ( 550 kcal ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
At birth lambs received an injection of the CCK A antagonist devazepide ( 0 . 01 or 0 . 1 mg / kg ) , the CCK B antagonist PD 135158 ( 0 . 01 or 0 . 1 mg / kg ) , or saline for the controls ( 1 ml / kg ) . ^^^ The use of a CCK A antagonist , but not a CCK B antagonist , was concluded to prevent the formation of a preferential relationship between the lamb and its mother , most probably by impairing neonatal learning . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The increase in hepatic vagal activity produced by CCK 8 was significantly reduced by i . v . administration of 200 micrograms / kg of the CCKA receptor antagonist devazepide . ^^^ These outcomes demonstrate that activation of CCKA receptors by CCK 8 increases hepatic vagal afferent activity and support the view that the duodenal satiety action of CCK is mediated by the hepatic branch . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) regulates somatostatin secretion through both the CCK A and CCK B / gastrin receptors in sheep . 1 . ^^^ The objectives of the present study were to compare the in vivo potencies of the sulphated ( s ) and non sulphated ( ns ) forms of gastrin heptadecapeptide ( G 17 ) and CCK octapeptide ( CCK 8 ) on SOM secretion , and to determine the nature of the receptors involved by repeating the studies in the presence of the CCK A and CCK B / gastrin receptor antagonists L 364 , 718 and L 365 , 260 , respectively . ^^^ Both the CCK A and CCK B / gastrin receptor antagonists suppressed CCK 8s stimulated SOM output . ^^^ Despite sharing a common biologically active carboxy terminus , CCK stimulates SOM secretion by both the CCK A and CCK B / gastrin receptors , while gastrin acts via the CCK B / gastrin receptor alone . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCKA and CCKB receptor subtypes both mediate the effects of CCK 8 on myenteric neurons in the guinea pig ileum . ^^^ In 5 of these neurons , application of the CCKA antagonist L 364 , 718 ( 100 500 nM ) antagonized the action of CCK 8 and the CCKB antagonist L 365 , 260 ( 500 nM ) had no effect . ^^^ The results demonstrate that the excitatory effects of CCK 8 are mediated by both CCKA and CCKB receptor subtypes . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
All the compounds were evaluated in vitro towards both CCK B and CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pretreatment with either the CCKA receptor antagonist devazepide or the CCK ( B ) receptor antagonist L 365 , 260 significantly attenuated this effect over a range of doses ( 20 , 100 , 500 microg / kg i . p . ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of loxiglumide ( CAS 107097 80 3 , CR 1505 ) , a novel cholecystokinin A ( CCK A ) receptor antagonist , on pancreatic exocrine secretion stimulated by exogenously administered CCK 8 were examined in conscious dogs with chronic pancreatic fistula . ^^^ These results demonstrated that the selective CCK A antagonist loxiglumide inhibited the increase of pancreatic exocrine secretion stimulated by CCK 8 based on selective blockade of receptor binding of CCK in dogs . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of loxiglumide ( CAS 107097 80 3 , CR 1505 ) , a novel cholecystokinin A ( CCK A ) receptor antagonist , on pancreatic exocrine secretion stimulated by meal were examined in conscious dogs with chronic pancreatic fistula . ^^^ These results show that the selective CCK A antagonist loxiglumide may inhibit the increase of pancreatic exocrine secretion based on selective blockade of receptor binding of CCK endogenously induced by meal in dogs . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Loxiglumide ( ( + / ) 4 ( 3 , 4 dichlorobenzamido ) N ( 3 methoxypropyl ) N pentylglutaramic acid , CAS 107097 80 3 , CR 1505 ) is a cholecystokinin A ( CCK A ) receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Otsuka Long Evans Tokushima Fatty ( OLETF ) rats develop obesity , hyperglycemia , and non insulin dependent diabetes mellitus and do not express cholecystokinin A ( CCK A ) receptors , the receptor subtype mediating the satiety actions of CCK . ^^^ Together , these data are consistent with the interpretation that the lack of CCK A receptors in OLETF rats results in a satiety deficit leading to increases in meal size , overall hyperphagia , and obesity . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCKB binding profile as shown in competition studies by using different CCK related compounds and non peptide CCK antagonists discriminating between CCKA and CCKB sites . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The compounds were selective for CCK B receptors as they did not bind with high affinity to CCK A receptors expressed in human tumors ( meningiomas or gastroenteropancreatic tumors ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The objectives of the present study were to determine the separate effects of CCK and gastrin on fundic and antral SOM secretion and to assess the type of receptor involved , using CCK A ( L 364 , 718 ) and CCK B / gastrin ( L 365 , 260 ) receptor antagonists . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results indicate that CCKA receptors within the SPD arterial bed mediate the satiating action of CCK , consistent with local action of duodenal CCK . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Selective N methylation of a racemic precursor with [ 11C ] iodomethane and subsequent optical resolution of the racemate with HPLC afforded optically pure [ 11C ] L 365 , 260 and [ 11C ] L 365 , 346 , which are selective for CCK B ( central type ) receptors and CCK A ( peripheral type ) receptors , respectively . ^^^ These preliminary results suggest that the nonpeptide CCK antagonist [ 11C ] L 365 , 346 may be useful for probing pancreatic CCK A receptors by PET . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A series of phenoxyacetanilide derivatives was synthesized and their antagonist activities for human gastrin / cholecystokinin ( CCK ) B and CCK A receptors were evaluated . ^^^ Among the compounds synthesized , 2 [ 3 [ 3 [ N [ 2 ( N methyl N phenylcarbamoylmethoxy ) phenyl ] N ( N meth yl N phenylcarbamoylmethyl ) carbamoylmethyl ] ureido ] phenyl ] acetic acid ( 20i , DA 3934 ) exhibited high affinity for gastrin / CCK B receptors and high selectivity over CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A critical appraisal of this research indicates that while it is clearly demonstratable that exogenous peripheral CCK can alter food intake by acting on CCKA receptors , the mechanism involved may be more closely related to the induction if aversion and nausea , rather than satiety . ^^^ Moreover , CCKA receptor antagonist which do not cross the blood brain barrier fail to increase meal size , as would be expected if peripheral CCK was an effective satiety factor . ^^^ These studies show that CCK administered intracerebroventicularly , or by micoinjection into discrete brain regions , also inhibits feeding via a CCKA receptor mechanism . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present study sought to determine the roles of CCK A and CCK B receptor activation in the PAG in modulating defensive rage behavior . ^^^ Administration of the CCK A antagonist , PD 140548 ( 34 nmol / 0 . 25 microliter ) , into the PAG failed to alter response latencies for defensive rage behavior . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These stimulations were fully prevented by the presence of 10 pM YM 022 , a G / CCK B receptor antagonist , but unaffected by L 364 , 718 , a CCK A receptor antagonist . ^^^ CCK A and G / CCK B receptors mRNA were detected in the cells . ^^^ The evidence for secreted gastrin and CCK A and B receptors mRNA may further suggest the existence of an autocrine loop involving a stimulatory gastrin / CCK B receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The stimulation of CCK A or CCK B receptors is implicated in the physical and psychological responses of CCK to stress . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Binding studies showed the overexpression of two classes of CCK A receptors of low and high affinity when compared to the normal pancreas which was less sensitive to CCK 8 . ^^^ CONCLUSIONS : CCK 8 exerts a biphasic growth response on the acinar pancreatic carcinoma , mediated by two classes of CCK A receptors overexpressed in the tumour . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that there are discrete , noninteractive populations of jejunal afferents that possess either 5 HT 3 or CCK A receptors but not both . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Two types of CCK receptors have been identified : ( 1 ) CCK A receptors are mainly located in the periphery , but are also found in some areas of the CNS ; and ( 2 ) CCK B receptors are widely distributed in the brain . ^^^ It is shown that anxiety like symptoms can only be induced by a selectively acting CCK B agonist , whereas mixed CCK A and B agonists and selective CCK A agonists fail to change behavior in anxiety tests . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Moreover , the affinity of the different compounds towards the cholecystokinin CCK A and CCK B receptors was evaluated . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We detected the expression of mRNA encoding CCK A and CCK B receptors in eight human pancreatic tumour cell lines using reverse transcription polymerase chain reaction ( RT PCR ) , but not by RNase protection assays . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We therefore investigated , by in situ hybridization , whether CCK A or CCK B receptor mRNA could be detected in normal rat pancreatic islets and in the rat insulinoma cell line , RINm5F . ^^^ The CCK A , but not the CCK B , receptor transcript was detected in both islets and RINm5F cells . ^^^ Islet CCK A receptors were mostly confined to the center of the islets corresponding to the distribution of the B cells . ^^^ We conclude that the CCK A , but not the CCK B , receptor subtype is expressed in both normal rat islets and in the rat insulinoma derived cell line RINmS5F . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
High gastrin and cholecystokinin ( CCK ) gene expression in human neuronal , renal , and myogenic stem cell tumors : comparison with CCK A and CCK B receptor contents . ^^^ In addition , CCK A and CCK B receptors were evaluated in the same group of tumors with receptor autoradiography . ^^^ CCK A and CCK B receptors were not frequently found in these tumors , except for leiomyosarcomas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The response to CCK was mediated via the CCKA receptor as shown by the antagonistic action of devazepide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
However , the results obtained with CCK or CCKA receptor antagonists in different species ( rats , mice ) and different models of acute pancreatitis ( cerulein pancreatitis , hemorrhagic pancreatitis induced by choline deficient , ethionine supplemented diet , arginine induced pancreatitis , sodium taurocholate induced pancreatitis ) produced variable results . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A , CCK B , neurotensin , somatostatin and VIP receptors were localized by in vitro receptor autoradiography with iodinated radioligands on histological sections of surgical samples of 27 gastric and 25 colonic adenocarcinomas . ^^^ CCK A , CCK B and neurotensin 1 receptors were found in a minority of both tumor types . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
High affinity CCK receptors are divided in two main subtypes : the CCK A ( A for ( A for `` alimentary ' ' ) and the CCK B ( B for `` brain ' ' ) receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The responses to both CCK and CAH were abolished by the CCKA antagonist devazepide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK 8 interacts with nanomolar affinities with two different receptors designated CCK A and CCK B . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Exogenous CCK and gastrin stimulate pancreatic exocrine secretion via CCK A but also via CCK B / gastrin receptors in the calf . ^^^ Specific CCK A and CCK B / G receptor antagonists ( SR 27897 and PD 135158 , respectively ) were used to identify the CCK receptor subtype involved in exogenous CCK and gastrin induced exocrine pancreatic responses . ^^^ Although CCK A receptors are not predominantly expressed , they seem to play a major role in the response of pancreatic exocrine secretion to CCK . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the jejunum , CCK 8 induces an inhibitory response that is mediated by both CCK A and B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Studies with CCK receptor binding , hybridization with radiolabeled complementary DNA ( cDNA ) probes , or reverse transcription polymerase chain reaction have shown that CCK A receptors also are present in rat pancreatic putative preneoplastic lesions and cancer tissue , rat pancreatic cancer cell lines , pancreatic carcinomas in transgenic mice , hamster pancreatic cancer , and human pancreatic cancer cell lines and tumors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
OBJECTIVE : To characterise the cholecystokinin ( CCK ) receptor subtypes in medullary thyroid cancer by measuring the expression of CCK A and CCK B / gastrin receptor mRNA . ^^^ MAIN OUTCOME MEASURE : Presence of CCK A and CCK B / gastrin receptors . ^^^ CCK B / gastrin receptors but not CCK A receptors were detected by RT PCR in all six biopsy specimens . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Sulfated CCK derivatives performed significantly better but also displayed a comparably high uptake in normal CCK A receptor expressing tissues . ^^^ This effect was probably due to their similar affinity for both CCK A and CCK B receptors . ^^^ Nonsulfated gastrin derivatives may be preferable because of their CCK B receptor selectivity , hence lower accretion in normal CCK A receptor expressing organs . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Resected tissue specimens of pancreatic adenocarcinomas were therefore studied by both reverse transcriptase polymerase chain reaction ( RT PCR ) and in situ hybridization for the presence of CCK A receptors . ^^^ Ninety percent of studied tumors demonstrated CCK A expression by RT PCR , and this expression was localized to neoplastic cells by in situ hybridization . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Since CCK B / G subtype receptor is predominant over the CCK A subtype in the human pancreas , we hypothesized that it could be expressed by islet cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Decreased responsiveness to dietary fat in Otsuka Long Evans Tokushima fatty rats lacking CCK A receptors . ^^^ Adult Otsuka Long Evans Tokushima fatty ( OLETF ) rats lack functional cholecystokinin A ( CCK A ) receptors , are diabetic , hyperphagic , and obese , and have patterns of ingestion consistent with a satiety deficit secondary to CCK insensitivity . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide and L 365 , 260 were used to block CCKA and CCK ( B ) receptors and ondansetron and tropisetron to block 5 HT 3 and 5 HT 4 receptors , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A and B and neurotensin receptors were not detected in HCC . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Sulfated CCK derivatives performed significantly better but additionally displayed a high uptake in normal , CCK A receptor expressing tissues ( such as the liver / gallbladder , pancreas , and bowel ) . ^^^ Nonsulfated gastrin derivatives may be preferable because of their CCK B receptor selectivity , and hence , lower accretion in normal CCK A receptor expressing organs . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Therefore , in this article we ( 1 ) review evidence for CCK ' s participation in control of meal size , ( 2 ) document involvement of CCK A receptors located on vagal sensory neurons in control of food intake by exogenous and endogenous CCK , ( 3 ) point out apparent discrepancies in the experimental record , which auger for non endocrine sources of CCK and non vagal sites of CCK action , and ( 4 ) summarize recent observations , suggesting mechanisms by which CCK could participate in the control of daily food intake and body weight regulation . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To assess the role of endogenous cholecystokinin in the control of gastric emptying of peptone solutions and Intralipid suspensions , we examined the ability of a dose range of the CCK A antagonist , devazepide to accelerate the gastric emptying of various caloric concentrations of peptone and Intralipid in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the present study we investigated the presence of CCK A and CCK B , as well as somatostatin 2 ( SSTR 2 ) receptors by RT PCR , and studied the actions of EGF , CCK and octreotide on DNA synthesis in the human pancreatic adenocarcinoma cell line Capan 2 . ^^^ By means of RT PCR analysis we were able to demonstrate SSTR 2 expression , but not CCK A or CCK B receptor mRNA in Capan 2 cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A scattered distribution of CCK A and B receptor immunopositive varicose fibers were visualized throughout the N . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) and gastrin exert their effects through two receptors , the CCK A and CCK B receptors . ^^^ Prenatal expression of both CCK A and CCK B receptors in various tissues was analyzed by RT PCR . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In conclusion , CCK 8 blocked ascending contraction elicited by electrical field stimulation of duodenal mucosa by means of simultaneous activation of CCK A and CCK B receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Interaction between CCK and a preload on reduction of food intake is mediated by CCK A receptors in humans . ^^^ We therefore tested the hypothesis that alimentary CCK ( CCK A ) receptors mediate the interaction of CCK with an appetizer on food intake in humans . ^^^ CCK octapeptide ( CCK 8 , 0 . 75 microgram infused over 10 min ) or saline ( placebo ) with concomitant infusions of saline ( placebo ) or loxiglumide , a specific CCK A antagonist , was infused into 16 healthy men with use of a double blind , four period design . ^^^ These effects are mediated by CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In vitro we found that 1 ) 55 / 70 gastric vagal afferents ( GVAs ) were polymodal , responding to CCK 8 and mechanical stimuli , 13 were mechanoreceptive , and 2 were CCK responsive ; 2 ) sequential or randomized intra arterial injections of CCK 8 ( 0 . 1 200 pmol ) dose dependently increased firing rate and reached the peak rate at 100 pmol ; 3 ) the action was suppressed by CCK A ( Devazepide ) but not by CCK B ( L 365 , 260 ) receptor antagonist ; 4 ) neither antagonist blocked the mechanosensitivity of GVA fibers . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
At least two different G coupled high affinity receptors have been identified : the CCK A and the CCK B receptors . ^^^ This article reviews the main biological role of CCK , the therapeutic potential of CCK A and CCK B receptor agonists and antagonists and the common compounds from the different families of ligands . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Using a multi fistulated model , plasma PYY levels were compared in 6 dogs after 60 mM oleate was perfused into the proximal one half of the small intestine following i . v . administration of saline or devazepide , a CCK A antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pancreatic secretory response to feeding in the calf : CCK A receptors , but not CCK B / gastrin receptors are involved . ^^^ The present study was aimed at determining both the role of external stimuli in the outset of the prefeeding phase and the implication of pancreatic CCK A and CCK B / gastrin receptors in the mediation of pancreatic response to feeding . ^^^ The first objective was studied by suppressing external stimuli associated with food intake ( unexpected meal ) and the second by infusing highly specific and potent antagonists of CCK A ( SR 27897 ) and CCK B / gastrin ( PD 135158 ) receptors during the prandial period . ^^^ The expectancy of a meal seemed to elicit an increased pancreatic response right before a meal and CCK A receptors may mediate this information via neural pathways . ^^^ The implication of CCK and CCK A receptors in mediating the postfeeding pancreatic response was also demonstrated . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lacked CCK A receptors ( CCKAR ) because of a genetic abnormality . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The relative affinity of CCK to its receptor has been characterized in various biological and pharmacological studies and it is now well established that CCK has a higher affinity to the CCKA than to the CCKB receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In rodents exposed to cold a dose dependent hypothermia has been observed on peripheral injection of CCK probably acting on CCKA receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Full length cDNA clones encoding the human CCK A and CCK B / gastrin receptor are expressed in peripheral blood mononuclear cells from healthy volunteers without haematopoietic malignancy . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Acid inhibition by intestinal nutrients mediated by CCK A receptors but not plasma CCK . ^^^ We examined the role of CCK A receptors in acid inhibition by intestinal nutrients . ^^^ The CCK A antagonist MK 329 ( 1 mg / kg 4 ) reversed acid inhibition caused by CLD , lipid , and dextrose . ^^^ Lipid and carbohydrate inhibit acid secretion by activating CCK A receptors but not by altering plasma CCK concentrations . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the present study we investigated the influence of WGA and UEA 1 on CCK 8 induced alpha amylase secretion of the rat pancreatic tumor cell line AR42J , which expresses both CCK A and CCK B receptors . ^^^ The simultaneous application of the lectins with CCK antagonists L 364 , 718 or L 365 , 260 led to a reduction of secretion , but the assignment to CCK A or CCK B receptors was not possible . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To investigate the roles of endogenous NT and CCK , we administered [ ( 3 ) H ] TC into the rat duodenum or lower jejunum and tested the effect of the NT antagonist SR 48692 ( 2 nmol 10 kg ( 1 ) 10 min ( 1 ) ) or CCK A antagonist lorglumide ( 100 nmol 10 kg ( 1 ) 10 min ( 1 ) ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Those present in peripheral system have been termed as CCK A receptors and those present in central nervous system as CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Moreover , the cells responded to CCK agonists after adenoviral mediated gene transfer of CCK A or CCK B receptors . ^^^ Quantitative RT PCR indicated that the message levels for CCK A receptors were approximately 30 fold lower than those of CCK B receptors , which were approximately 10 fold lower than those of m 3 Ach receptors . ^^^ In situ hybridization indicated the presence of m 3 Ach receptor and insulin mRNA but not CCK A or CCK B receptor mRNAs in adult human pancreas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The consensus structure between CCK 15 and CCK 8 shows a good superposition of the side chains of residues 12 14 with crucial moieties of two non peptidic CCK A antagonists . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To test the validity of this hypothesis , we determined gastric acid secretion in the CCK 1 ( CCK A ) receptor deficient Otsuka Long Evans Tokushima fatty ( OLETF ) rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The amount of mRNA expression of CCK A and CCK B receptors was determined by reverse transcription polymerase chain reaction . ^^^ The results show that CCK A receptors are significantly more expressed in non responders than responders , whereas CCK B receptor expression is similar in both groups . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Rats lacking DMN CCK A receptors are obese and have increased expression of NPY in the DMN , supporting earlier data that CCK may act at the DMN to suppress food intake . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We previously reported genetic variations in the promoter and coding regions of the CCKA receptor ( CCKAR ) , CCKBR , and CCK genes and a possible association between polymorphisms of the CCKAR gene and alcoholism . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Our aim was determine the relationship between cholecystokinin ( CCK ) A receptor blockade , glucose levels , insulin secretion and gastric emptying in humans , and to assess the effect of CCK A blockade on pancreatic polypeptide secretion . ^^^ In a second experiment , a continuous intravenous infusion of loxiglumide ( 7 . 5 mg kg h ( 1 ) ) was started 60 min before and continued until 120 min after test meal ingestion to block the CCK A receptors . ^^^ Blockade of peripheral CCK A receptors accelerates gastric emptying of liquids with an increase in postprandial insulin levels . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Anxiogenic effects were observed in the elevated plus maze in rats when pure CCKB receptor agonists ( CCK 4 and CCK 8 non sulfated ) or CCK 8S , a CCKB / CCKA agonist , were injected into the lateral ventricle . ^^^ In contrast , CCK 33 , a CCKA agonist or CCK ( 1 21 ) and CCK ( 26 29 ) were ineffective . ^^^ Furthermore , the anxiogenic effects of CCK 8S were prevented by blocking CCKB but not CCKA receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
RATIONALE : Converging evidence has demonstrated that cholecystokinin ( CCK ) inhibits mesolimbic brain dopamine ( DA ) function via activation of CCK A ( CCK 1 ) receptors . ^^^ Most research on the antipsychotic like drug effects of CCK has used CCK or CCK analogues that nonselectively activate both CCK A and CCK B ( CCK 2 ) receptors , which may produce opposite effects . ^^^ SR 146131 , a CCK A selective nonpeptide agonist , has recently been developed ( Sanofi Synthelabo ) . ^^^ CONCLUSIONS : The lack of an effect of SR 146131 on amphetamine induced disruption of PPI suggests that a selective nonpeptide CCK A agonist may not produce antipsychotic like effects on dopamine transmission . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pharmacological analysis suggests that this inhibition is mediated by CCK A receptors and involves PKC phosphorylation . ^^^ Pharmacology similarly demonstrated that these calcium elevations were mediated by CCK A receptors and were dependent on intracellular calcium stores . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that OT inhibits gastric emptying in male rats via a mechanism involving CCK stimulation and CCKA receptor activation . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Using specific antibodies against CCKA and CCKB receptors , somatostatin , glucagon and insulin , we were able to confirm by Western blot the presence of both CCK receptor protein subtypes in the calf pancreas as a 80 85 kDa CCKA receptor and 40 45 kDa CCKB receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
No difference was observed in the increase of food intake induced by CCK A and CCK B receptor antagonists in both control and post infected rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
BACKGROUND : Different routes of administration of CCK 33 and blockage of CCK A and muscarinic ( m 3 ) receptors are used in this study to evaluate the mechanisms by which cholecystokinin can stimulate the exocrine pancreas . ^^^ METHODS : The experiment was performed on eight anaesthetized pigs during control conditions and after administration of the CCK A and m 3 receptor antagonists , Tarazepide and 4 DAMP , respectively . ^^^ Pancreatic secretion evoked by peripheral CCK 33 in pharmacological doses was independent of m 3 receptors blockade but depended on CCK A receptors located elsewhere than in the duodenum / pancreas . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK peptides exert their action on two distinct receptor subtypes : CCK A ( Alimentary ) now called the CCK1R , mostly expressed peripherally ; and CCK B ( Brain ) , renamed the CCK2R , which is primarily present in the brain . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In contrast to gastrin , CCK also recognizes CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Blockade of CCK A receptors with intraperitoneal MK 329 ( 1 mg / kg ) did not reverse bombesin induced gastroprotection . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Evidence on the role of CCK in anxiety related and reward related behaviours in various animal models indicates that CCK B receptors in the basolateral amygdala are important mediators of anxiety related behaviours and that CCK A and CCK B receptors in the nucleus accumbens are important in mediating different aspects of reward related behaviour . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
After the meal pattern experiments , CCK ( 0 . 5 , 1 , 2 , 4 , 8 , and 16 microg / kg ip ) was administered to examine the role of the interstitial cells and vagal IMA mechanoreceptors in relaying peripheral signals of satiety activated by CCK A receptors , whereas the specificity of the response was assessed with the antagonist devazepide ( 300 microg / kg ip ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Response to acute food deprivation in OLETF rats lacking CCK A receptors . ^^^ Together , these data suggested that OLETF rats lacking CCK A receptors are not only capable of increasing their food intake in response to food deprivation , but also exhibit differential sensitivity to the effects of deprivation during both the food deprivation and refeeding periods . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK mediates its effects through interaction with specific receptors subdivided in two subtypes CCK A ( present in the periphery and in few selected brain nuclei ) and CCK B ( the predominant receptor subtype in the brain ) . ^^^ Data showing that CCK A receptors mediate mnemonic while CCK B receptors mediate amnestic effects are also presented . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Bolus intravenous administration of CCK ( 10 microg / kg ) significantly increased pancreatic and islet blood flow in control Long Evans Tokushima Otsuka ( LETO ) rats , but not in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lacking CCK A receptors . ^^^ Our results demonstrated that exogenous CCK is a potent vasodilator of exocrine as well as islet vasculature via CCK A receptors , and that such action is mediated by a NO dependent mechanism rather than by vagal mechanisms . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Our data clearly identified CCK A and CCK B receptor mRNAs in the rat retina and demonstrated that they are functional , stimulating tyrosine phosphorylation pathways . ^^^ Our results provide novel biochemical information to further understand the physiological role of CCK A and B receptors in rat retina . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Inhibitory effect of the lectin wheat germ agglutinin on the binding of 125I CCK 8s to the CCK A and B receptors of AR42J cells . ^^^ A binding assay was used with 125I CCK 8s and dexamethasone stimulated AR42J cells , bearing CCK A as well as CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
By contrast to its central fever inducing effect , in rodents exposed to cold CCK 8 elicits a dose dependent hypothermia on peripheral injection probably acting on CCK A receptors . ^^^ The possible role of CCK ergic mediation in endotoxin ( LPS ) fever has revealed that while CCK B receptors seem to be involved in the development of fever , the role of CCK A receptors could be more complex . ^^^ In particular , while rats lacking functional CCK A receptors show an exaggerated fever response , this phenomenon may be associated with a trait different from the absence of this receptor set . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We have previously shown that while CCKA receptor antagonists generally do not affect locomotor behaviors , systemic administration of a CCKA receptor antagonist attenuates amphetamine ( AMPH ) induced locomotion in animals previously treated chronically with AMPH , suggesting that chronic stimulant pretreatment may sensitize CCK systems . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Mediation of mother infant interactions by the brain gut peptide cholecystokinin ( CCK ) was examined by observing behavior of Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which lack functional CCKA receptors because of a genetic abnormality . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Thus , the inhibitory effect of peptone on P 18 was apparently not mediated by endogenous CCK acting at CCKA receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
At 96 h after the administration of picrotoxin into the basolateral nucleus , we have observed an increase in the expression of genes associated with 18 different monoamine ( ie adrenergic alpha 1 , alpha 2 and beta 2 , serotonergic 5HT5b and 5HT6 , dopamine D 4 and muscarinic m 1 , m 2 and m 3 ) and peptide ( CCK A and B , angiotensin 1A , mu and kappa opiate , FSH , TSH , LH , GNRH , and neuropeptide Y ) G protein coupled receptors ( GPCRs ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The participation of the vagal and sympathetic pathways and involvement of CCK A receptors were considered . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A separate group of nodose neurones that possessed high affinity CCK type A ( CCK A ) receptors also responded to luminal infusion of 5 HT . ^^^ From these results we concluded that the vagal nodose ganglion contains neurones that may possess only high or low affinity CCK A receptors or 5 HT 3 receptors . ^^^ Some neurones that express high affinity CCK A receptors also express 5 HT 3 receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
However , conclusive evidence that human pancreatic acini lack functional CCK A receptors has been presented . ^^^ Although most knowledge of vagal CCK A receptors comes from research on rodents , physiologic studies suggest that this information is applicable to humans . ^^^ In contrast to its effect on satiety , which is mediated by low affinity vagal CCK A receptors , CCK acts through high affinity CCK A receptors to evoke pancreatic secretion , suggesting that different affinity states of the vagal CCK receptors mediate different digestive functions . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) , one of the first discovered gastrointestinal hormones , which stimulates pancreatic enzyme secretion and induces gallbladder contraction , is one of the most abundant neurotransmitter peptides in the brain and is implicated in satiety via CCK A receptors . ^^^ To examine the mechanism of this enhanced suppression , we measured the mRNA levels of CCK , CCK A and CCK B receptors in the cerebral cortex and the hypothalamus of young and old male rats . ^^^ The mRNA level of CCK A receptors in the hypothalamus decreased with age , whereas the mRNA levels of CCK B receptors in the hypothalamus and cerebral cortex did not . ^^^ Moreover , the effects of aging on the gene expressions of CCK A and CCK B receptors were different . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Experiments were performed under control conditions , and after pretreatment by gavage feeding with YF 476 , using either a single , low dose of 0 . 3 micromol kg , which would block the CCK B receptors , or a 1000 times higher dose ( 300 micromol kg ) , which would also block the CCK A receptors . ^^^ Supra physiological doses of CCK 33 to the general circulation appeared to affect the pancreatic enzyme secretion via CCK A receptors located elsewhere than in the pancreatic and duodenal tissue . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) and the CCKA receptor gene polymorphism , and smoking behavior . ^^^ We analyzed genetic variants of the promoter region of the cholecystokinin ( CCK ; which modulates the release of dopamine ) gene , and intron 1 and exon 5 of the CCKA receptor gene , and performed association analyses of nicotine dependence using an allele specific amplification ( ASA ) method and PCR RFLP methods . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These novel CCK ligands have shown to act as mixed CCK A / CCK B ligands in a [ 125 ] 1 CCK 8 receptor binding assay . ^^^ The best pyrazoline 5e of this series displayed an IC 50 of 20 and 25 nmol / L for the CCK A , and CCK B receptor , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The biological functions attributed to CCK are mediated by two receptor subtypes , termed CCKA and CCKB , located predominantly in the gastrointestinal ( GI ) tract and in the brain , respectively . ^^^ This paper focuses on the data available on the effect of CCKA receptor antagonist administration in humans , and shows how , in addition to allowing a more exact definition of the role of CCK in the regulation of some GI functions , these drugs may also possess therapeutic potential in GI disorders . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCKA receptor antagonist lorglumide inhibited CCK 8S induced activation of orexin neurons , whereas the CCKB receptor agonists CCK 4 ( a tetrapeptide form of cholecystokinin ) and nonsulfated CCK 8 had little effect . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Selective CCK A but not CCK B receptor antagonists inhibit HT 29 cell proliferation : synergism with pharmacological levels of melatonin . ^^^ We used HT 29 human colon cancer cells , expressing CCK receptors , to test the antiproliferative effects of several antagonists of CCK A and / or CCK B and their possible synergism with melatonin . ^^^ The following drugs were tested : gastrin ( CCK B agonist ) ; CCK 8s ( CCK A agonist ) ; proglumide ( CCK A plus CCK B antagonist ) ; lorglumide ( CCK A antagonist ) ; PD 135 , 158 ( CCK B antagonist and weak CCK A agonist ) ; devazepide or L 364 , 718 ( CCK A antagonist ) ; L 365 , 260 ( CCK B antagonist ) , and melatonin . ^^^ These results suggest that melatonin and CCK A antagonists are useful for controlling human colon cancer cell growth in culture and in combined therapy significantly increases their efficiency . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cholecystokinin ( CCK ) interacts with two types of G protein coupled receptors in the brain : CCK A and CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The difference in mRNA expressions of hypothalamic CCK and CCK A and B receptors between responder and non responder rats to high frequency electroacupuncture analgesia . ^^^ The mRNA expressions of CCK , and CCK A and B receptor were determined by real time RT PCR . ^^^ CCK mRNA levels were not significantly different in the two groups , whereas both CCK A and B receptors were significantly more expressed in non responders . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In addition , intravenous administration of CCK has been observed to reproduce the symptoms in FD and this effect can be blocked both by atropine and loxiglumide ( CCK A antagonist ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Receptors for cholcystokinin ( CCK ) can be pharmacologically classified into at least two distinct subtypes , CCKAR and CCKBR . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The two known receptors mediating the actions of cholecystokinin ( CCK ) and gastrin , CCK type A ( CCKAR ) and CCK type B ( CCKBR ) receptors , are G protein coupled receptors having approximately 50 % amino acid homology . ^^^ Both the CCKAR and CCKBR have high affinity for sulfated CCK peptides , while only the CCKBR has high affinity for gastrin peptides . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Fusion of the C terminus of the CCKAR to the N terminus of the GFP did not alter receptor ligand binding affinity , signal transduction , or the pattern of receptor surface expression and receptor mediated cholecystokinin ( CCK ) internalization . ^^^ Newly obtained biologically active fluorescent derivatives of CCK were used for simultaneous observation of receptor and ligand trafficking in CHO , NIH / 3T3 , and HeLa cells stably expressing the fluorescent CCKAR and in transiently transfected COS 1 cells . ^^^ The CCKAR antagonists , L 364 , 718 and CCK 27 32 amide potently inhibited spontaneous internalization of the receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The cholecystokinin ( CCK ) receptor types A and B ( CCKAR and CCKBR ) are G protein coupled receptors with approximately 50 % amino acid identity ; both have high affinity for the sulfated CCK octapeptide ( CCK 8 ) , whereas only the CCKBR has high affinity for gastrin . ^^^ Alanine substitution of the equivalent amino acids in the CCKAR corresponding to each of the five amino acids in ECL 1 and ECL 2 affecting CCK 8 affinity for the CCKBR revealed only two mutations , L103A and F107A , that decreased CCK 8 affinity ( 68 and 2885 fold , respectively ) . ^^^ These data suggest that CCK 8 interacts at multiple contact points in the extracellular domains of CCK receptors and that the CCKAR and CCKBR have distinct binding sites despite their shared high affinity for CCK 8 . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A systemic administration of cholecystokinin ( CCK ) increases gastric vagal afferent activity via type A CCK receptors ( CCKAR ) . ^^^ In the present study , the response of gastric vagal afferent activity to an intravenous administration of CCK was investigated in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which lack CCKAR , and compared with its control strain , Long Evans Tokushima Otsuka ( LETO ) rats . ^^^ The responses were not influenced by the pretreatment with L 365 , 260 , a type B CCK receptor ( CCKBR ) antagonist , while they were significantly diminished by pretreatment with MK 329 , a CCKAR antagonist . ^^^ These results demonstrate that neither CCKAR nor CCKBR contributes to the response of the afferent activity of the gastric vagal nerve to a systemic administration of CCK in OLETF rats , suggesting an involvement of novel ( non A , non B ) CCK receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In order to identify the site ( s ) of action of CCK in the gastropyloric region , we performed immunohistochemistry using an antibody directed to the C terminal region of the cholecystokinin A receptor ( CCKAR ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Polymorphisms of the CCK , CCKAR and CCKBR genes : an association with alcoholism study . ^^^ We analyzed genetic variations in the promoter and coding regions of the CCK , CCKA receptor ( CCKAR ) and CCKB receptor ( CCKBR ) genes , and performed association analyses with alcoholism . ^^^ RESULTS : A total of 8 variants in the CCK gene , 11 variants in the CCKAR gene and 9 variants in the CCKBR gene were detected in the present study . ^^^ CONCLUSIONS : Our data suggest that polymorphisms of the CCK , CCKAR and CCKBR genes do not play a major role in alcohol withdrawal symptoms ( even though significant associations were found among polymorphisms at the 388 and 333 loci of the CCKAR gene and hallucinations , the rate was nonsignificant after Bonferroni correction ) . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Type A CCK receptor ( CCKAR ) antagonists differing in blood brain barrier permeability [ devazepide penetrates ; the dicyclohexylammonium salt of Nalpha 3 quinolinoyl d Glu N , N dipentylamide ( A 70104 ) does not ] were used to test the hypothesis that duodenal nutrient induced inhibition of gastric emptying is mediated by CCKARs located peripheral to the blood brain barrier . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Type A cholecystokinin receptor ( CCKAR ) antagonists differing in blood brain barrier permeability were used to test the hypothesis that duodenal delivery of protein , carbohydrate , and fat produces satiety in part by an essential CCK action at CCKARs located peripheral to the blood brain barrier . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We showed that STC 1 cells expressed CCKAR as well as its peptide ligand , CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Type A cholecystokinin receptor ( CCKAR ) antagonists differing in blood brain barrier permeability were used to test the hypothesis that satiety is mediated , in part , by CCK action at CCKARs located peripheral to the blood brain barrier . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In matched Chinese PD subjects with and without hallucinations , the presence of the 45 C / T locus in the cholecystokinin ( CCK ) gene , particularly when combined with the CCK receptor , CCKAR ( cholecystokinin A receptor ) , C polymorphism , was associated with increased hallucination risk . ^^^ Genomic DNA was analyzed for CCK , CCKAR , and CCKBR ( cholecystokinin B receptor ) polymorphisms by polymerase chain reaction . ^^^ Of 5 cases with both CCK T and CCKAR C alleles , 4 were hallucinators . ^^^ CONCLUSIONS : Our study supports a previous association of hallucinations in PD subjects with the CCK T allele and the combined CCK T and CCKAR C allele , suggesting that the CCK system may influence the development of hallucinations in PD subjects . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In rat , gastrin and its CCKBR seem responsible for foetal pancreas growth while after birth , CCK was shown to be the most potent trophic factor via occupation of its CCKAR . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.51576836
Although previous studies have concluded that the indole ring of Trp 30 is a critical pharmacophore for the interaction of CCK with both its A and B type receptors , we find 2 Nal 30 Ac CCK 7 ( 20 ) to be nearly equipotent to 2 in both CCK binding and as an anorectic agent sensitive to blockade by the Merck CCK A receptor antagonist MK 329 . 0.51576836^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.94201892
Further to these , ( 1S trans ) N [ alpha methyl N [ [ ( 2 methylcyclohexyl ) oxy ] carbonyl ] D tryptophyl ] L 3 ( phenylmethyl ) beta alanine ( 28h ) is a mixed CCK A / CCK B ligand with a CCK A binding affinity of IC 50 = 3 . 9 nM and a CCK B binding affinity of IC 50 = 4 . 2 , producing a CCK A / CCK B ratio of unity . 0.94201892^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.51863502
We conclude that CCK interacts with neural CCK A receptors to cause esophageal muscle contraction . 0.51863502^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The results show 1 ) that hyperCCKemia raised the histidine decarboxylase ( HDC ) activity of the ECL cells in PCS rats but not in control rats , and the CCK A receptor blockade failed to prevent the enzyme activation ; and 2 ) that PBD prevented the ECL cell hypoplasia and the decrease in HDC activity induced by antrectomy . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In general , these analogues maintained good potency and selectivity for the CCK A receptor ( guinea pig pancreas ) , as well as potent anorectic activity in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In addition , in ARIP cells , the CCK 8 induced increase in cytosolic calcium was abolished by pretreatment with the selective CCK B receptor antagonist L 365 , 260 but not by the CCK A receptor antagonist L 364 , 718 . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Since cDNA of both the CCK A receptor ( classical pancreatic CCK receptor ) coding region and the CCK B receptor coding region have recently been cloned and sequenced , we investigated the expression of messenger RNA of these receptors in DSL 6 pancreatic carcinoma . ^^^ Our results showed that the 32P labelled cDNA probe of the CCK A receptor coding region hybridized with an approximately 2 . 7 kb mRNA from both DSL 6 pancreatic carcinoma and normal rat pancreas . ^^^ However , the relative expression of the CCK A receptor mRNA in DSL 6 pancreatic carcinoma was approximately 8 fold of that in normal rat pancreas . ^^^ In summary , the CCK A receptor mRNA is overexpressed approximately 8 fold and the gastrin ( CCK B ) receptor mRNA is novelly expressed in DSL 6 pancreatic carcinoma as compared to normal rat pancreas . ^^^ The gene overexpression of the CCK A receptor and the novel gene expression of the gastrin ( CCK B ) receptor may be generated by alterations in gene regulation during carcinogenesis , and may play an important role in promoting tumor growth . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Competition experiments indicated that L 365 , 260 , a selective CCK B ( gastrin ) receptor antagonist , was the most potent displacer of 125I CCK 8 , and no significant displacement of binding was found with the selective CCK A receptor antagonist . ^^^ Growth of PANC 1 cells in culture was stimulated by CCK at a concentration consistent with the Kd , and CCK stimulated growth was inhibited by the CCK B receptor antagonist ( L 365 , 260 ) not the CCK A receptor antagonist ( L 364 , 718 ) . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Neither the CCK A receptor antagonist L 364 , 718 nor the CCK B receptor antagonist L 365 , 260 ( 10 ( 9 ) 10 ( 7 ) moles / kg ) antagonized CCK 8 actions . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pharmacological analysis using selective agonists and antagonists indicated the expression of the CCK A receptor at birth , whereas the CCK B receptor predominated at postnatal stages . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
MK 329 , a CCK A receptor selective antagonist , at a dose of 20 nmol / kg fully inhibited the action of 20 nmol / kg CCK 8 , while 100 nmol / kg of ( R ) L 365 , 260 , a CCK B selective antagonist , had no effect on the CCK 8 response . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Moreover , neither the response to gastrin 17 nor that to CCK 8s was affected by concomitant infusion of devazepide ( 200 micrograms / kg / h ) , a selective CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Exogenous CCK 8s and the CCK A receptor antagonist devazepide were infused continuously by means of osmotic minipumps . ^^^ Moreover , the trophic effects of PBD and of the combination of PBD and PCS could be prevented by CCK A receptor blockade ( devazepide infusion ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Proglumide ( 1 and 10 mg / kg SC ) and devazepide , ( a selective CCK A receptor antagonist ; 0 . 01 and 1 mg / kg SC ) , as well as caerulein ( 0 . 01 , 0 . 1 and 1 microgram / kg SC ) and CCK 4 ( a selective CCK B receptor agonist ; 25 and 50 micrograms / kg SC ) had no reliable effect . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine if endogenous cholecystokinin ( CCK ) was responsible for the decrease in food intake caused by MCT , birds were injected with the CCK A receptor antagonist devazepide ( DVZ , 1 mg / kg BW ) before diet presentation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Furthermore , 10 micrograms / kg of L 365 , 260 , a CCK B receptor antagonist , and 1 mg / kg of devazepide , a CCK A receptor antagonist , even tended to augment the effect of NMDA in the plus maze . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Activation by CCK related peptides of the CCK A receptor subtype accounts for 85 90 % of the maximal changes in cellular function , and activation of the CCK B / gastrin receptor accounts for 10 20 % of maximal changes . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The anorexic effect caused by 4 . 0 micrograms / kg was attenuated by 100 micrograms / kg of the type A CCK receptor antagonist MK 329 but not by 300 micrograms / kg of the type B CCK receptor antagonist L 365 , 260 , suggesting that CCK induced suppression of food intake in this species is mediated by a CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Despite decreased affinity for the human CCK A receptor , relative to CCK 8 , some of these compounds are equipotent to CCK as anorectic agents in rats following intraperitoneal administration . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In our study , we used loxiglumide , a potent CCK A receptor antagonist , to investigate the role of CCK A receptors in pancreatic consumption of circulating AAs and enzyme secretion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor mRNA level was determined by Northern blot analysis with a rat CCK A receptor cDNA probe . ^^^ The level of CCK A receptor mRNA first decreased , reaching the lowest level 7 days after occlusion , and then began to increase . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To gain a better understanding of the roles of CCK A and CCK B receptors in spinal nociceptive transmission during inflammation , this study evaluated the effects of intrathecally administered FK 480 ( a CCK A receptor antagonist ) and YM 022 ( a CCK B receptor antagonist ) . ^^^ These data indicate that a CCK B receptor antagonist , but not a CCK A receptor antagonist , produces an antinociceptive effect in the rat formalin test . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We assessed the duration of the anti cholecystokinin ( CCK ) action of FK 480 , a new non peptide CCK A receptor antagonist developed in Japan , in an in vivo study in rats , comparing it with CR 1505 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK XLR shares approximately 50 % homology at the amino acid level with both the human CCK BR and the peripheral CCK A receptor subtypes . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
RESULTS : By means of Northern blots , CCK A receptor mRNA was detected in rat fundus mucosa and pancreas but not in the remaining GI tract or brain . ^^^ By means of RT PCR , CCK A receptor mRNA was demonstrated in the brain and the mucosa of the fundus , antrum , duodenum , and colon , kidney , pancreas and pancreatic islets . ^^^ In man , CCK A receptor mRNA was detected in the brain , stomach , pancreas , and kidney , whereas CCK B receptor mRNA was found in the brain , stomach , and pancreas but not in the kidney . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Expression of CCK A receptor mRNA in the pancreas , small intestine and brain were not detected in OLETF rats by the reverse transcriptase polymerase chain reaction . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Role of cholecystokinin ( CCK ) A receptor for pancreatic growth after weaning : a study in a new rat model without gene expression of the CCK A receptor . ^^^ The CCK A receptor is known to be involved in regulating pancreatic exocrine function and growth . ^^^ These results suggest that the CCK A receptor plays some role in the increase in cell size associated with normal growth of the pancreas from 5 to 25 weeks of age ( after weaning ) . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Therefore , depending on the agonists used , CCK A receptor activation in pancreatic acini may result in differential involvement of second messenger systems , Ca2+ signal transduction , and amylase secretion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These compounds displayed micromolar affinities for CCK B rather than CCK A receptor and the obtained results confirm that the 4 ( 3H ) quinazolinone nucleous represent a useful template for the development of selective CCK B receptor ligands . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Results indicate that pig pancreatic acini are sensitive to Cch and relatively insensitive to caerulein with no response to JMV 180 , a CCKA agonist , or secretin ; MK 329 , a CCK A receptor antagonist , significantly inhibited caerulein induced enzyme secretion from 10 ( 8 ) M . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Tests were undertaken in 10 DU patients without or with elimination of the action of endogenous CCK using loxiglumide ( LOX ) , a selective CCK A receptor antagonist , before and 4 wk . after eradication of Hp with triple therapy ( omeprazole , amoxycillin and bismuth ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aim of the present experiment was to study the effects on the rat liver and biliary tract of long term stimulation of CCK 8S and the CCK A receptor antagonist devazepide , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We have shown that Otsuka Long Evans Tokushima Fatty ( OLETF ) rats show little or no expression of the CCK A receptor gene in the pancreas . ^^^ We examined whether the CCK A and CCK B receptor genes are expressed in the islets and the role of CCK A receptor in insulin secretion . ^^^ CCK A receptor mRNA was detected in the islets of LETO rats but not OLETF rats . ^^^ These results suggest that the occurrence of pancreatic endocrine dysfunction in OLETF rats may be due to a defect in expression of the CCK A receptor gene , not to insulin deficiency . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor mRNA was not expressed in the small intestine of OLETF rats but was in LETO rats . ^^^ The pancreatic responses to various stimuli in OLETF rats were well conserved except for the involvement of CCK A receptor function . ^^^ OLETF rats are confirmed as a new experimental model deficient in CCK A receptor gene expression and represent a useful tool for studying the physiological role of these in vivo . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Evaluation of cholecystokinin , gastrin , CCK A receptor , and CCK B / gastrin receptor gene expressions in gastric cancer . ^^^ In this study , reverse transcription polymerase chain reaction ( RT PCR ) was used to evaluate messenger RNA expression for CCK , gastrin , CCK A receptor , and CCK B / gastrin receptor in surgical specimens of gastric cancers and in normal antrum and body mucosa of the stomach . ^^^ The CCK A receptor mRNA expression was detectable in 5 / 14 ( 36 % ) samples of gastric cancer and in 7 / 12 ( 58 % ) body mucosa . ^^^ Three cases out of 14 ( 21 % ) of gastric cancer expressed both CCK gene and CCK A receptor gene . ^^^ These findings may suggest a greater role for CCK and CCK A receptor than for gastrin and CCK B receptor in gastric cancers . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
It is suggested that the decreased exploration in OLETF rats may be due to the lack of CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The binding of labeled CCK 8 was markedly inhibited by CCK 8 and CCK A receptor antagonists , but it was only weakly affected by gastrin and CCK B receptor antagonists . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The antagonist ( 1 microM ) for CCK B receptor , but not CCK A receptor , significantly inhibited the number of GH 3 cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The application of modern molecular biological techniques has identified two CCK receptors , CCK A receptor ( CCKAR ) and CCK B / gastrin receptor ( CCKBR ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Plasma CCK concentrations rose significantly from 6 . 6 + / 1 . 9 to 14 . 3 + / 2 . 9 pmol / l , and the pancreatic response was abolished by CCK A receptor blockade ( 0 . 0 + / 0 . 1 mg / h ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Binding of 125I BH CCK 8 to the pancreas was inhibited by agonists with the affinities ( dissociation constant ) of CCK ( 0 . 11 nmol / L ) approximately gastrin ( 0 . 15 nmol / L ) and by antagonists with the affinities of CCK B receptor antagonist ( L 365 , 260 , 0 . 18 nmol / L ) > CCK A receptor antagonist ( lorglumide , 8 . 1 nmol / L ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Moreover , specificity for CCK A receptor was also demonstrated by the inability of TP 680 to antagonize pentagastrin stimulated gastric acid secretion . ^^^ These results indicate that TP 680 is a potent , competitive and specific CCK A receptor antagonist with long duration of action . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Therefore , we studied the possible presence of alterations also in the parotid glands during TPN , after PBD and during infusion of sulfated cholecystokinin ( CCK 8S ) and the CCK A receptor antagonist devazepide , respectively . ^^^ The CCK A receptor antagonist devazepide induced a reduction in protein and DNA contents in the pancreas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We therefore studied the effect of the CCK A receptor antagonist loxiglumide on gastric emptying of a high caloric solid liquid meal in humans . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The modeling of the CCK A receptor and the docking of the peptide agonists [ Thr , Nle ] CCK 9 and CCK 8 indicated that their N terminus was connected to the receptor through a strong bond network involving Trp 39 and Gln 40 thus confirming experimental data . ^^^ These first molecular data identifying the agonist binding site of the human CCK A receptor represent an important step toward the complete delineation of the agonist binding site and the understanding of the molecular mechanisms that govern differential activation of this receptor by CCK related peptides . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The ethanol induced increase in amylase output can be completely inhibited by the CCK A receptor antagonist L 364 , 718 and partially inhibited by the muscarinic cholinergic antagonist atropine . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
For maximal reduction of endogenous bile output the CCK A receptor antagonist loxiglumide was infused intravenously . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The present studies were undertaken to evaluate the involvement of endogenous CCK and the CCK A receptors in the development of severe acute pancreatitis induced in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats that have a selective defect in the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
From day 3 to day 10 of life , male and female Wistar rat pups were treated with the CCK A receptor antagonist L 364 . 718 and the CCK A + B agonist CCK 8S . 3 . ^^^ These data show that early postnatal treatment with the CCK A receptor antagonist L364 . 718 has an impact on the hypophagic response to CCK 8S in later life . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This suggests that enzyme release is probably mediated by the same receptors in both adults and neonates , and in adults previous work has shown this to be the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pre treatment with intravenous MK 329 , benzodiazepine CCK A receptor antagonist , blocked the duodenal oleate effect on drug plasma levels in a single dog preliminary study . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Role of the cholecystokinin ( CCK ) A receptor in pancreatic growth in rats during the suckling period : a study in a naturally occurring CCK A receptor gene `` knockout ' ' rat . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist devazepide reduced the activation of GVAD induced by bombesin from 107 + / 11 to 63 + / 6 % , while abolishing the CCK response . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Alligator gallbladder smooth muscle expresses a CCK A receptor subtype , and stomach oxyntic mucosa expresses a distinct receptor subtype , termed CCK B / X because of its similarities to both CCK B and CCK 10 receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To investigate the role of the carboxyl terminus of cholecystokinin ( CCK ) receptors in receptor internalization , the rat wild type ( WT ) CCK A receptor ( WT CCKAR ) and the rat WT CCK B receptor ( WT CCKBR ) were truncated after amino acid residue 399 ( CCKAR Tr 399 ) and 408 ( CCKBR Tr 408 ) , thereby deleting the carboxyl terminal 45 and 44 residues , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In situ hybridization , using receptor specific riboprobes , localized CCK A receptor expression to ductal cells , the presumed origin of most human pancreatic adenocarcinomas . ^^^ Southern blot analysis revealed no evidence of CCK A receptor gene amplification or rearrangement in pancreatic adenocarcinomas . ^^^ Because of its selective expression , the CCK A receptor may serve as selective biomarker for pancreatic adenocarcinoma . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Porta caval shunted rats displayed an increased CCK A receptor mRNA concentration in the pancreas ( after stimulation with CCK 8s ) and an increased CCK B receptor mRNA concentration in the oxyntic mucosa . ^^^ In conclusion , the porta caval shunting evoked enhancement of the trophic effect of CCK A receptor activation on the pancreas and of CCK B receptor activation on the ECL cells is associated with enhanced expression of CCK A receptor mRNA in the pancreas and of CCK B receptor mRNA in the oxyntic mucosa . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The level of CCK mRNA and CCK concentration in the small intestinal mucosa , and the level of CCK A receptor mRNA in the pancreas were examined . ^^^ The CCK A receptor mRNA level also increased with age in LETO rats . ^^^ It is suggested that the long term defect of CCK A receptor may decrease CCK release and transcription . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The agonists used were CCK ( 1 30 nmol i . c . v . ) , a CCK A receptor agonist ( SNF 9019 ; 0 . 3 10 nmol i . c . v . ) , and a CCK B receptor agonist ( SNF 9007 ; 0 . 3 10 nmol i . c . v . ) . ^^^ The antagonists used were the CCK A receptor antagonist , L 364 , 718 ( 12 . 5 nmol i . c . v . ) , CCK B receptor antagonist , L 365 , 260 ( 2 . 5 25 nmol i . c . v . ) , and the nonselective opioid receptor antagonist naloxone ( 1 mg / kg s . c . ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Gastric emptying in OLETF rats not expressing CCK A receptor gene . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Retardation of pancreatic regeneration after partial pancreatectomy in a strain of rats without CCK A receptor gene expression . ^^^ In conclusion , the CCK A receptor is not an absolute requirement for pancreatic normal growth but is important for pancreatic regeneration . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
During distensions , saline , CCK ( 30 ng / kg / h ) or the CCK A receptor antagonist loxiglumide ( 10 mg / kg / h ) was perfused in a random double blind order . ^^^ CONCLUSIONS : In humans , CCK A receptor subtype is involved in the occurrence of transient lower oesophageal sphincter relaxations induced by gastric distension . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor agonists A 71378 ( desamino Tyr ( SO3H ) Nle Gly Trp Nle ( N methyl ) Asp Phe NH 2 ) , and A 71623 ( Boc Trp Lys ( epsilon N 2 methylphenylamino carbonyl ) Asp ( N methyl ) Phe NH 2 , as well as the CCK B receptor agonist Suc CCK 4 ( Suc Trp ( N methyl ) Nle Asp Phe NH 2 ) were iontophoretically administered with multibarrel capillaries . ^^^ About one third of the neurons responded to the CCK A receptor agonists . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Infusion of CCK A receptor mRNA antisense oligodeoxynucleotides inhibits lordosis behavior . ^^^ Neurons in the medial preoptic nucleus ( MPN ) express CCK A subtype receptor mRNA , and site specific infusions of CCK facilitate lordosis , suggesting that CCK A receptor activation positively modulates lordosis . ^^^ Antisense oligodeoxynucleotides ( ODN ) specific for CCK A receptor mRNA were infused into the MPN of ovariectomized female rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The selective CCK A receptor antagonist , devazepide , ( 0 . 03 3 . 0 mg / kg ) administered alone had no intrinsic effect on gastric emptying . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Three experiments were performed in random order : intravenous infusion of 1 ) placebo , 2 ) low dose atropine ( 5 micrograms . kg . h 1 ) , and 3 ) the CCK A receptor antagonist loxiglumide ( 22 mumol . kg . h 1 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Full and partial agonist activity of C terminal cholecystokinin peptides at the cloned human CCK A receptor expressed in Chinese hamster ovary cells . ^^^ The agonist activities of the C terminal cholecystokinin peptides sulfated cholecystokinin octapeptide ( CCK 8S ) , non sulfated cholecystokinin octapeptide ( CCK 8NS ) , pentagastrin and CCK 4 at the cloned human CCK A receptor expressed in Chinese hamster ovary cells were evaluated in two functional assays of receptor activation . [ 125I ] CCK 8S displacement studies employing membranes derived from these cells revealed the expected rank order of affinity for a number of CCK receptor ligands . ^^^ These results demonstrate that CCK 8S represents the minimum ligand requirement for both high affinity and full agonist activity at the human CCK A receptor subtype . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In contrast , CCK A receptor antagonists inhibited the stimulatory effect of G 17 in SIIA cells , whereas CCK B receptor antagonists had no effect . ^^^ Gly G stimulated the growth of AGS and SIIA cells ; neither the CCK B nor the CCK A receptor antagonists blocked this effect . ^^^ Furthermore , Gly G stimulates growth of human gastric cancer cell lines , possibly through a receptor other than the CCK B or CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Leptin CCK action was blocked by systemic capsaicin at a dose inducing functional ablation of sensory afferent fibers and by devazepide , a CCK A receptor antagonist but not by the CCK B receptor antagonist , L 365 , 260 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aim of this study was to identify the vagal CCK A receptor affinity state that mediates the effect of CCK on pancreatic protein secretion . ^^^ Infusion of CCK JMV 180 ( 22 88 micrograms . kg 1 . h 1 ) caused dose dependent increases in pancreatic protein secretion , which were blocked by the CCK A receptor antagonist L 364 , 718 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist MK 329 abolished the pancreatic secretory response to intraduodenally infused LCRF ( 1 35 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK B receptor antagonist L 365 , 260 almost totally blocked MAPK activation in AR42J cells after stimulation with gastrin and glycine extended gastrin and substantially reduced the activation of both kinases by CCK 8 , while the CCK A receptor antagonist L 364 , 718 was much less effective . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of a synthetic putative luminal cholecystokinin ( CCK ) releasing factor ( LCRF ) fragment ( 1 35 ) on pancreatic exocrine secretion were examined in conscious Wistar rats and a mutant strain of rats lacking the CCK A receptor . ^^^ No significant effect was observed in rats lacking the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
One half of the hamsters fed a high fat diet received the CCK A receptor antagonist devazepide ( 25 nmol / kg / hr ) for the duration of the experiment . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pretreatment with the CCK A receptor antagonist MK 329 ( devazepide ; 1 mg / kg and 2 mg / kg i . p . ) reduced the CCK induced increase in c fos expression in the LC / SC by 54 % and 75 % , respectively ; the CCK B receptor antagonist L 365 , 260 had no effect . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor mRNA was detected in 5 out of 8 esophageal cancers ( 0 . 1 1 fg / microg ) , in 5 out of 8 gastric cancers ( 0 . 05 4 . 2 fg / microg ) and in 5 out of 12 colon cancers ( 0 . 1 1 fg / microg RNA ) . ^^^ The expression of the CCK A receptor in esophageal , gastric and colon cancers and of the CCK B / gastrin receptor in the majority of gastric adenocarcinomas screened may be an important indicator of the influence of CCK and gastrin of local or systemic origin on the growth of these cancers . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effect of a new CCK A receptor antagonist , dexloxiglumide , on the exocrine pancreas in the rat . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist MK 329 ( 0 . 1 mg / kg i . p . ) diminished the FLI increase in LC , NTS , AP , and PVN by 39 100 % ; the CCK B receptor antagonist L 365 , 260 reduced the increased FLI in the AP by 54 % . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
On one day they received an i . v . infusion of Loxiglumide , a CCK A receptor antagonist ( 30 mg / kg / h for 10 min then 10 mg / kg / h for 3 h 10 min ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Compound 6 produces potent anorectic activity via the CCK A receptor system . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In this report , we show that the intraperitoneal administration of a CCK B receptor antagonist , PD 135158 ( 0 . 1 mg / kg ) , but not a CCK A receptor antagonist , lorglumide , inhibited hyperlocomotion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We examined the cholecystokinin ( CCK ) B / gastrin receptor , H+ / K+ ATPase and somatostatin gene expression , the histology and immunohistochemistry of gastrin and somatostatin of the stomach , plasma gastrin levels , and gastric acid secretion in naturally occurring CCK A receptor gene knockout ( Otsuka Long Evans Tokushima fatty , OLETF ) rats . ^^^ The overexpression of CCK B / gastrin receptor mRNA and the hyperfunction of parietal cells were observed in rats without CCK A receptor gene expression . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Six healthy male volunteers were studied in random order on five occasions using : ( a ) IVAA , ( b ) loxiglumide ( CR 1505 , a selective CCK A receptor antagonist ) , ( c ) IVAA plus loxiglumide , ( d ) atropine and ( e ) IVAA plus atropine . ^^^ CONCLUSION : In healthy volunteers intravenous infusion of high doses of amino acids results in a significant gallbladder contraction , which is inhibited by CCK A receptor blockade and by atropine . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Role of cholecystokinin A ( CCK A ) receptor in pancreatic regeneration after pancreatic duct occlusion : a study in rats lacking CCK A receptor gene expression . ^^^ We examined the role of the cholecystokinin A ( CCK A ) receptor in acute inflammatory and regenerative stages of experimental pancreatitis using a rat model lacking the CCK A receptor [ Otsuka Long Evans Tokushima Fatty ( OLETF ) rats ] . ^^^ These observations indicate that the absence of the CCK A receptor did not modify the acute phase of pancreatitis but significantly retarded regeneration of the pancreatic tissue . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results indicate that the affinity of loxiglumide to CCK A receptor is at least 63 times greater than that to CCK B / gastrin receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Suppression of sham feeding by exogenous CCK 8 or intraintestinal oleate infusion is attenuated by peripheral administration of the CCK A receptor antagonist , devazepide , but not by the CCK B antagonist , L 365260 . ^^^ Although originally categorized as a `` peripheral ' ' receptor subtype , the CCK A receptor is also present in the brain . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To compare the roles of CCK receptors , the effects of the CCK A receptor agonist A 71378 , the CCK A / B receptor agonist CCK 8S and the CCK B receptor agonist BOC CCK 4 on anxiety related behavior and the 5 HT release in the prefrontal cortex were determined . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Furthermore , we emphasize the important physiologic roles of CCK and CCK receptors by the discovery of disrupted CCK A receptor gene in rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Receptor gene expression for the CCK B / gastrin receptor , but not for the CCK A receptor , was found by reverse transcription polymerase chain reaction . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The lectins wheat germ agglutinin ( WGA ) and Ulex europaeus agglutinin ( UEA 1 ) are used for affinity chromatography to isolate the highly glycosylated CCK A receptor of pancreatic acinar cells . ^^^ The results are discussed with respect to a possible influence of both lectins on the interaction of CCK or cerulein with the CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Sulfation of the tyrosine at the seventh position from the C terminus of cholecystokinin ( CCK ) is crucial for CCK binding to the CCK A receptor . ^^^ Using three dimensional modeling , we identified methionine 195 of the CCK A receptor as a putative amino acid in interaction with the aromatic ring of the sulfated tyrosine of CCK . ^^^ The high affinity sites of the wild type CCK A receptor were highly selective ( 800 fold ) toward sulfated versus nonsulfated CCK , whereas low and very low affinity sites were poorly selective ( 10 and 18 fold ) . ^^^ This interaction is essential for CCK dependent transition of the CCK A receptor to a high affinity state . ^^^ Our data should represent an important step toward the identification of the residue ( s ) of the receptor in interaction with the sulfate moiety of CCK and the understanding of the molecular mechanisms that govern CCK A receptor activation . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This tactic yielded a series of monocyclic 2 oxopyrrolidine derivatives 4 with selectivity for CCK A or CCK B receptors and with slightly improved binding affinity at the CCK A receptor subtype with respect to the model 3 oxoindolizidines . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A bolus injection of the CCK A receptor antagonist , loxiglumide , CR 1505 ( 0 . 1 , 0 . 5 and 1 . 0 mg / kg ip ) , prior to clinimeal blocked the inhibitory action of CCK on the motor activity in a concentration dependent manner . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The gastrin / cholecystokinin ( CCK ) B and CCK A receptor antagonist activities of these compounds were evaluated by investigation of their affinities for human gastrin / CCK B receptors and human CCK A receptors , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide ( a CCK A receptor antagonist , 1 mg / kg , i . p . ) prevented the increase in Fos expression induced by leptin CCK in the PVN and by CCK alone in the PVN , CeA and NTS / AP . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A 40 % increase in cell numbers was observed in the presence of 10 ( 10 ) MCCK 8 and this increase was inhibited by the addition of 25 microM CCK A receptor antagonist ( CR 1505 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
BACKGROUND : Recently , it has been shown that infusion of the CCK A receptor antagonist devazepide induced proliferation of hepatocytes and bile duct epithelium in the rat liver . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aim of this study was to determine the effect of the CCK A receptor antagonist , loxiglumide , on postprandial LES function and fundic tone in humans . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
It describes the effects of CCK 8 infused intravenously ( i . v . ) at physiological doses and endogenous CCK released by intraduodenal ( i . d . ) oleate on gastric mucosal damage , as brought about by ethanol without or with pretreatment with loxiglumide , a selective CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Augmentation of the inhibitory effect of FK 480 , a CCK A receptor antagonist , on pancreatic exocrine secretion by achlorhydria . ^^^ FK 480 ( CCK A receptor antagonist ) inhibited pancreatic exocrine secretion dose dependently at doses of 0 . 01 1 . 0 mg / kg . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effect of lintitript , a new CCK A receptor antagonist , on gastric emptying of a solid liquid meal in humans . ^^^ We studied the role of endogenous CCK in the emptying of a solid / liquid meal administering the new , highly specific and potent CCK A receptor antagonist lintitript . ^^^ The study demonstrates for the first time the marked gastrokinetic properties of the new CCK A receptor antagonist lintitript in humans . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In 7 additional volunteers , the effect of cholestyramine was studied during intravenous perfusion of saline or the CCK A receptor antagonist loxiglumide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results demonstrate that radiation increases the release of CCK in the hypothalamus , and that this effect is inhibited by vagotomy and the administration of a CCK A receptor antagonist . ^^^ A CCK A receptor antagonist may be used to mitigate a radiation induced deficit in food intake . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effect of FK 480 , a CCK A receptor antagonist , on spontaneously developed chronic pancreatitis in WBN / Kob rats . ^^^ Although blockade of the CCK A receptor could be considered to exacerbate chronic pancreatitis due to possible inhibition of the trophic action of CCK , our results suggest that CCK A receptor antagonists may not be detrimental to chronic pancreatitis . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor is the predominant peripheral CCK receptor subtype and the CCK B receptor is the predominant central CCK receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In animal strains which do not have a CCK A receptor due to a genetic abnormality AP induced by a certain noxious factor does not develop to the same severity when compared to animals with a normal CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A 12 carbon but not a 10 carbon long chain fatty acid reduced antral contractile amplitude , an effect that was abolished by loxiglumide ( a specific CCK A receptor antagonist ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This study was designed to compare the effect of CCK 8 and intraduodenal ( i . d . ) instillation of sodium oleate , or diversion of the pancreatic biliary secretions that are known to release CCK , on the gastric mucosal lesions induced by topical application of 100 % ethanol or acidified aspirin ( ASA ) in rats with or without the pretreatment with a CCK A receptor antagonist , loxiglumide , or with L 365 , 260 to block CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effect of intermittent injections of CCK 8S and the CCK A receptor antagonist devazepide on cell proliferation in exocrine rat pancreas . ^^^ When studying the influence of stimulation and inhibition of the CCK A receptor on cell proliferation in the exocrine pancreas , not only are the drugs and doses of importance but also the mode of administration . ^^^ BACKGROUND : Continuous infusion of CCK 8S or the CCK A receptor antagonist devazepide induces transient changes in acinar cell proliferation in rat pancreas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In particular , the data imply a CCK A receptor mechanism in the regulation of individual sensitivity towards ethanol and a CCK B receptor mechanism in the regulation of individual sensitivity towards cocaine . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The sensory experience evoked by lipid was diminished by both topical mucosal anaesthesia and CCK A receptor blockade . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
PYY antibody ( anti PYY ) at a dose of 0 . 5 mg / kg or CCK A receptor antagonist ( devazepide ) at a dose of 0 . 1 mg / kg was administered alone or in combination 10 min before the proximal half of the gut was perfused with 60 mM oleate or buffer . ^^^ We found that 1 ) peptone induced gastric acid secretion was inhibited by intestinal fat ( P < 0 . 0001 ) , 2 ) inhibition of acid secretion by intestinal fat was reversed by CCK A receptor antagonist ( P < 0 . 0001 ) but not by anti PYY , and 3 ) slowing of gastric emptying by fat was reversed by CCK A antagonist ( P < 0 . 05 ) but not by anti PYY . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor antagonists have selective effects on nutrient induced food intake suppression in rats . ^^^ To provide additional support to the hypothesis that only dietary protein ( Pro ; chicken egg albumin ) and not amino acids ( AA ; patterned after albumin ) , carbohydrates ( CHO ; cornstarch ) , or fats ( Fat ; corn oil ) produces a satiating effect via CCK receptors , two CCK A receptor antagonists ( PD 140 , 548 and devazepide ) were coadministered with each nutrient . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Highly constrained dipeptoid analogues containing a type 2 ' beta turn mimic as novel and selective CCK A receptor ligands . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Localization of CCK A receptor in the human duodenum . ^^^ CCK A receptor mRNA was not expressed in the human pancreas , but was expressed in the gallbladder and duodenum , although it was expressed in the pancreas by RT PCR . ^^^ These results suggest that localization of CCK A receptor in human duodenum provides a biochemical and morphological basis for some physiological functions of CCK . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We investigated the pharmacologic characteristics of a newly developed benzodiazepine derivative ( S ) ( ) N [ 2 , 3 dihydro 2 oxo 5 phenyl 1 [ ( 1H tetrazol 5 yl ) methyl ] 1H 1 , 4 benzodiazepine 3 yl ] 2 indolecarboxamide ( TS 941 ) , a cholecystokinin type A ( CCK A ) receptor antagonist , in the isolated rat pancreatic acini and compared with those of well known CCK A receptor antagonists , devazepide and loxiglumide . ^^^ These results indicate that TS 941 is a potent , competitive , and selective CCK A receptor antagonist for the pancreas . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Inhibition of gastric emptying in response to 50 mg lipid in the proximal small intestine was unaffected by administration of PYY antibody but was abolished by administration of the CCK A receptor antagonist devazepide ( 0 . 1 mg / kg ip ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
High affinity CCK A receptor agonists JMV 180 and CCK OPE ( 1 1 , 000 nM ) did not increase the intensities of the RhoA band , suggesting that stimulation of RhoA is mediated by the low affinity CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The simultaneous administration of equimolar doses of a selective CCK A receptor antagonist blocked the effect of CCK , while a CCK B antagonist was ineffective . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Defects of cholecystokinin ( CCK ) A receptor gene expression and CCK A receptor mediated biological functions in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats . ^^^ Recent studies in genetically obese and diabetic Otsuka Long Evans Tokushima Fatty ( OLETF ) rats suggest defects of cholecystokinin ( CCK ) A receptor gene expression and CCK A receptor mediated biological functions such as pancreatic juice , protein , and gastric acid secretion . ^^^ The present studies were undertaken to further examine CCK A receptor gene expression and CCK A receptor mediated biological functions in the pancreas , stomach , and brain of OLETF rats . ^^^ Expression of the CCK A receptor gene could not be detected in the stomach , pancreas and brain by the reverse transcription polymerase chain reaction ( RT PCR ) method and Southern blotting of the PCR products . ^^^ Southern blot analysis of genomic DNA from OLETF and control Long Evans Tokushima Otsuka ( LETO ) rats with CCK A receptor fragment as a probe revealed different restriction bands . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Northern blot analysis showed a strong signal for CCK B receptor mRNA in adult pancreas , but no detectable signal for CCK A receptor mRNA . ^^^ However , RT PCR / Southern blotting showed the presence of CCK A receptor mRNA in adult pancreas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist CR 1409 , but not the CCK B antagonist L 365260 , blocked the vagal response to endogenous CCK stimulation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The expression of CCK A receptor mRNA and cNOS mRNA was significantly increased in rats treated with CCK 8 and camostate , whereas CCK B receptor mRNA remained unaffected . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The role of CCK in mediating neuronal activity in the brain in response to dietary carbohydrate was measured by detecting Fos immunoreactivity in response to duodenal glucose load in rats after administration of the CCK A receptor antagonist devazepide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Rat adipocytes exclusively contain gastrin / CCK B receptor mRNA , but not CCK A receptor mRNA . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Role of CCK A receptor in the regulation of pancreatic bicarbonate secretion in conscious rats : a study in naturally occurring CCK A receptor gene knockout rats . ^^^ Whether cholecystokinin ( CCK ) has a direct action on duct cells and the role of CCK A receptor in bicarbonate secretion were examined by comparing the results obtained from OLETF ( CCK A receptor deficient rats ) and control ( LETO ) rats . ^^^ In conclusion , intravenous injection of CCK did not stimulate bicarbonate secretion , and the lack of CCK A receptor decreased bicarbonate secretion in response to luminal stimulants . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The dose range of activity ( 0 . 5 60 micrograms / kg ) together with the evidence that another CCK B receptor antagonist , L 365 , 260 ( 5 micrograms / kg ) increased , while devazepide ( a CCK A receptor antagonist ; 20 micrograms / kg ) decreased non REM sleep and total sleep time , support the original hypothesis that the activity of GV 150013 on sleep progress through CCK B receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Similar results were observed in binding studies with the CCK A receptor antagonist [ 3H ] L 364 , 718 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
As OLETF rats lack CCK A receptor because of a genetic abnormality , we examined whether learning and memory were impaired in these animals using an elevated eight arm radial maze . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist loxiglumide completely abolished the effect of cerulein on DNA fragmentation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
However , the binding sites in CCK A receptor seem to be slightly rigid as compared to those in CCK B or gastrin receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We investigated how heat shock protein 27 ( HSP 27 ) and its phosphorylation are involved in the action of cholecystokinin ( CCK ) on the actin cytoskeleton by genetic manipulation of Chinese hamster ovary ( CHO ) cells stably transfected with the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Second , 12 subjects received either intraduodenal fat or saline perfusion plus a concomitant infusion of saline or loxiglumide , a specific CCK A receptor antagonist , together with a preload of banana shake . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In contrast , LPC 1 responded with increased cell number to CCK 8S and decreased cell number to the CCK A receptor antagonist devazepide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To determine whether the inhibition of gastric emptying by BN like peptides is mediated by a CCK dependent mechanism , we examined the ability of the CCK A receptor antagonist , devazepide , to block the inhibition of saline gastric emptying produced by BN , GRP 18 27 and NMB . ^^^ These results suggest that BN like peptides inhibit gastric emptying through an indirect mechanism that is dependent upon CCK A receptor activation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aim of this study was to elucidate the cellular sites of expression of CCK A receptor in the rat stomach and small intestine . ^^^ METHODS : We developed and characterized an antibody to the N terminal region ( LDQPQPSKEWQSA ) of rat CCK A receptor and used it for localization studies with immunohistochemistry . ^^^ RESULTS : Specificity of the antiserum was demonstrated by ( 1 ) detection of a broad band at 85 95 kilodaltons in Western blots of membranes from CCK A receptor CHO transfected cells ; ( 2 ) cell surface staining of CCK A receptor transfected cells , ( 3 ) translocation of CCK A receptor immunostaining in CCK A receptor transfected cells after exposure to CCK ; and ( 4 ) abolition of tissue immunostaining by preadsorbtion of the antibody with the peptide used for immunization . ^^^ CCK A receptor immunoreactivity was localized to myenteric neurons and to fibers in the muscle and mucosa . ^^^ Many CCK A receptor myenteric neurons contained the inhibitory transmitter vasoactive intestinal polypeptide , and some were immunoreactive for the excitatory transmitter substance P . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Thus pretreatment of rats with a CCK A receptor antagonist ( L 364718 ) attenuated the immediate ( < or = 90 min ) pancreas secretory response to PHA but could not prevent a PHA associated increase in digestive enzyme output in the longer term ( after 90 min ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor gene possibly associated with auditory hallucinations in schizophrenia . ^^^ The present study suggests that the CCK A receptor gene may be associated with auditory hallucinations in schizophrenia . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Small intestinal and pancreatic microstructures are modified by an intraduodenal CCK A receptor antagonist administration in neonatal calves . ^^^ The aim of the present study was to investigate the role of CCK on the upper gut and pancreas microstructure and on pancreatic juice secretion in neonatal calves assessed by a repetitive intraduodenal administration of FK 480 , a CCK A receptor antagonist , during the first 6 days of life . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The specific CCK B receptor antagonist L 740 , 093 blocks the gastrin but not the CCK response , indicating that both the CCK B and the CCK A receptor can mediate ICER gene activation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Our study provided the possibility that polymorphism in the promoter region of the CCK A receptor gene may be one of genetic factors affecting fat deposition . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Recently , a strain of rats lacking the CCK A receptor , Otsuka Long Evans Tokushima Fatty ( OLETF ) , has been discovered making it possible to study the mesolimbic DA regulatory role of CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Inhibition of the hypothalamic pituitary adrenal axis in food deprived rats by a CCK A receptor antagonist . ^^^ Under these conditions we observed that the CCK A receptor antagonist , SR 27897 ( 0 . 3 mg kg ( 1 ) ) , but not the CCK B receptor antagonist , L 365260 ( 1 mg kg ( 1 ) ) , increases food intake . ^^^ These results indicate that CCK A receptor blockade during fasting prevents the activation of the HPA axis . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor activation induces fos expression in myenteric neurons of rat small intestine . ^^^ Neuronal Fos responsiveness in both brain and myenteric neurons was mediated by CCK A receptors , as CCK induced Fos expression was eliminated in rats pretreated with a CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor mRNA was selectively expressed only in pancreatic adenocarcinomas . ^^^ These data suggest that selective CCK A receptor expression in pancreatic adenocarcinomas reflects neoantigen expression in humans . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist might be therapeutically useful in acute pancreatitis by stopping the vicious circle . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
SUBJECTS AND METHODS : Three sequential double blind , three period crossover studies were performed in 12 healthy males each : ( 1 ) subjects received intraduodenal fat with or without 120 mg of tetrahydrolipstatin , an inhibitor of gastrointestinal lipases , or saline ; ( 2 ) volunteers received intraduodenal long chain fatty acids , medium chain fatty acids , or saline ; ( 3 ) subjects received long chain fatty acids or saline together with concomitant intravenous infusions of saline or loxiglumide , a specific CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Intact acini were stimulated with cholecystokinin ( CCK ) 8 , carbachol ( CCh ) and the high affinity CCK A receptor agonist , CCK OPE , and the cell lysates were used for REA . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These pancreatic changes by the diets were abolished by treatment with devazepide , a CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Moreover , CCK , CCK A receptor , and gastrin / CCK B receptor mRNA were measured by reverse transcriptase polymerase chain reaction . ^^^ CCK A receptor mRNA was detected in most tumors , but neither the mature ligands ( alpha amidated and O sulfated CCK peptides ) nor their precursors were expressed in carcinoma and normal pancreatic tissue . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To test the possibility that cholecystokinin ( CCK ) mediates anorexia induced by IL 1 beta and LPS , mice trained to poke their noses in a hole to obtain a food reward according to a fixed ratio ( 1 reward per 20 actions ) were pretreated with the CCK A receptor antagonist L 364 , 718 ( at 1 mg / kg ) or with the CCK B receptor antagonist L 365 , 260 ( 50 microg / kg ) before being injected with LPS ( 100 microg / kg ) or IL 1 beta ( 20 microg / kg ) . ^^^ In spite of its ability to block the effects of exogenous CCK 8 on food motivated behavior in mice , the CCK A receptor antagonist did not block the depressive actions of LPS and IL 1 beta on food motivated behavior . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The SAR of the hexa and tetrapeptide classes suggests that the Hpa ( SO ( 3 ) H ) and Tac groups may not interact at the CCK A receptor in the same location . ^^^ However , the C terminal dipeptide part of the hexapeptides and tetrapeptides appear to interact at the CCK A receptor in a similar manner . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
BACKGROUND : Infusion of sulphated cholecystokinin 8 ( CCK 8S ) in rats transiently increased the proliferation of pancreatic acinar cells , whereas the CCK A receptor antagonist devazepide decreased such proliferation . ^^^ The aim of this study was to examine the effect of continuous infusion of CCK 8S and devazepide on CCK A receptor gene expression . ^^^ The pancreas was dissected , and indirect immunofluorescence for BrdU and CCK A receptor was performed . ^^^ In situ hybridization to CCK A receptor mRNA was performed for examination and semiquantification of receptor gene expression . ^^^ Immunofluorescence for the CCK A receptor showed a decreased labeling intensity after CCK 8S infusion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist devazepide was used to antagonize the effect of CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In other experiments , rats were treated with either antagonists to the 5 HT ( 3 ) receptor ( ondansetron HCl ; 100 microgram / kg ) or the CCK A receptor ( L 364 , 718 , 100 or 200 microgram / kg ) in combination with LPS or IL 1beta . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We have also demonstrated that when the tryptophan residue is connected to the C or N terminal sides of the anthranilic acid dimer , compounds with similar micromolar CCK A receptor affinities are obtained . ^^^ Among the compounds synthesized , the N 1H indol 3 propionyl derivative exhibited an improved , at the micromolar range , affinity for the CCK A receptor in comparison to that of either , the N unsubstituted derivative and asperlicin . ^^^ The lead compound emerging from this key step of our investigation represents the new starting point for the development of a new class of CCK A receptor ligands . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We observed that peripheral gastric effects of CCK ( 300 nM ) produced a mean activation response of 271 + / 3 . 9 % compared with control level ( 100 % ) in 33 ( 60 % ) neurons tested ( P < . 01 ) , and this response was abolished by a CCK A receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Rats that lack the CCK A receptor become obese , but transgenic mice lacking CCK A receptors do not become obese . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Cefaclor , a cephalosporin antibiotic , delays gastric emptying rate by a CCK A receptor mediated mechanism in the rat . ^^^ Cefaclor delays gastric emptying via capsaicin sensitive afferent pathways , which involve CCK A receptor interaction . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The potentiating effect induced by the co injection of ip CCK and leptin to inhibit food consumption in mice is mediated by the CCK A receptor and capsaicin sensitive afferents . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of cholecystokinin octapeptide ( CCK ( 8 ) ) , the CCK A receptor antagonist , MK 329 , and the CCK B receptor antagonist , L 365 , 260 , microinfused into the paraventricular nucleus of hypothalamus ( PVN ) on colonic motor function was investigated in awake rats , chronically implanted with a microinjection cannula into the PVN and a catheter into the proximal colon . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK 8 induced contraction was blocked by the CCK A receptor antagonists loxiglumide ( IC 50 11 micromol L 1 ) and SR 27897 ( IC 50 74 nmol L 1 ) but not by CCK B receptor antagonists ( 1 micromol L 1 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
NAP , a peripheral CCK A receptor antagonist , modulates the development of a preference for the mother by the newborn lamb . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The obtained micromolar affinities for CCK A rather than CCK B receptor confirm that the anthranilic acid dimer represents a useful template for the development of selective CCK A receptor ligands . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aim of this study was as follows : ( 1 ) to compare the effect of continuous infusion and of intermittent injections of CCK 8S on cell proliferation , weight gain , and induction of apoptosis and ( 2 ) to examine the effect of injections of CCK 8S on CCK A receptor gene expression in the rat pancreas . ^^^ The pancreas was dissected and immunohistochemistry was performed for analysis of the expression of the apoptosis promoting protein bax and the apoptosis inhibiting protein bcl 2 , and for BrdU and CCK A receptor localization . ^^^ In situ hybridization ( ISH ) was used for examination and semiquantification of CCK A receptor mRNA expression . ^^^ Immunofluorescence and ISH for the CCK A receptor and its gene expression , respectively , showed a lowest intensity at 3 hours after CCK 8S injections . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Reviews describe the regulation of CCK gene expression and CCK release , the nature of the hormone binding site of the CCK A receptor , interaction of CCK , dopamine and GABA , the role of CCK in thermoregulation , sexual behavior and satiety in rodents and humans . ^^^ The research articles document features of cardiovascular regulation , reduced cocaine sensitization and decreased satiety in rats that lack the CCK A receptor . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
We investigated the effects of a CCK A receptor antagonist on the development of mother preference . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Furthermore , pretreatment with the CCK A receptor antagonist , devazepide , attenuated intestinal nutrient induced reduction of food intake only in LETO , but not OLETF rats . ^^^ In addition , our results indicate : 1 ) that OLETF rats have deficits in the satiation response to a variety of intestinal nutrient infusions ; 2 ) that the temporal pattern for CCK A receptor participation in satiation by intestinal nutrients is different during ingestion of liquid and solid foods and 3 ) that intestinal nutrients provide some satiation signals that are CCK A receptor mediated and some that are not . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effect of oleate was abolished by the CCK A receptor antagonist Devazepide ( 0 . 5 mg / kg ) , whereas the effect of butyrate persisted despite pretreatment with either Devazepide or a combination of the calcium channel inhibitors nifedipine ( 1 mg / kg ) and the omega conotoxins GVIA and SVIB ( each 25 microg / kg ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Although these compounds exhibited a regnylogical type organization similar to that of CCK 4 , they are characterized by about 1000 fold greater affinity for CCK A receptor than the C terminal tetrapeptide . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In fundic mucosa , CCK A receptor mRNA and protein mapped to D cells ( 37 . 4+ / 7 . 7 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Nine neonatal Friesian calves ( five controls and four treated intraduodenally with FK 480 , a CCK A receptor antagonist ) were surgically fitted with a pancreatic duct catheter and a duodenal cannula before the first colostrum feeding . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
METHODS : CCK 8S or the CCK A receptor antagonist devazepide were infused subcutaneously by osmotic minipumps for 4 weeks in 11 and 7 hamsters , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The authors characterize the behavioral properties of Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , which lack the CCK A receptor because of a genetic abnormality . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Vagotomy abolished the effects of CCK on MAP and SSND as did the CCK A receptor antagonist devazepide ( 0 . 5 mg / kg 4 ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The mRNA levels of the CCK A receptor were determined by reverse transcription polymerase chain reaction ( RT PCR ) . ^^^ However , in contrast to the decreased contractility , the steady state mRNA levels of the gallbladder CCK A receptor were significantly increased in the animals fed a high cholesterol diet in comparison with the corresponding control animals . ^^^ Up regulation of the CCK A receptor mRNA in the gallbladder of animals fed a high cholesterol diet associated with decreased contractility may be due to an impairment of CCK signaling related to increased membrane cholesterol contents and its related reaction of biological compensation in order to increase the receptor concentration . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK is a major mediator of the sensitisation of gastric perception by lipids in patients with functional dyspepsia as the CCK A receptor antagonist dexloxiglumide markedly diminishes this effect . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
AIMS : The therapeutic efficacy of a CCK A receptor antagonist , loxiglumide , in patients with painful acute attacks of chronic pancreatitis was evaluated . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Importance of CCK A receptor for gallbladder contraction and pancreatic secretion : a study in CCK A receptor knockout mice . ^^^ Bile and pancreatic secretions were determined in a CCK A receptor deficient mouse mutant generated by gene targeting in embryonic stem cells . ^^^ In some CCK A receptor ( + / ) animals , LacZ staining was performed . ^^^ CCK 8 significantly increased amylase and bile acid outputs in CCK A receptor ( + / + ) and ( + / ) mice , whereas no response was observed in ( / ) mice . ^^^ Neuromedin C and acetylcholine increased amylase secretion in CCK A receptor ( / ) mice similar to ( + / ) and ( + / + ) mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These data suggest that CCK A receptor mechanisms may contribute to the therapeutic and the extrapyramidal motor effects associated with antipsychotic drug treatment . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
INTRODUCTION : In humans , cholecystokinin ( CCK ) stimulates pancreatic secretion , and CCK A receptor antagonists prevent it in vivo . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Administration of MK 329 , a CCK A receptor antagonist , significantly reduced the number of postprandially activated neurons in both gastrectomized and control rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the present study , we determined whether oral administration of camostat showed a trophic effect in mice as observed in rats and whether the trophic effect , if substantial , was mediated via the CCK A receptor , using CCK A receptor gene targeting mice . ^^^ Three and seven day treatments with camostat did not affect pancreatic wet weight in CCK A receptor ( + / ) mice . ^^^ After 14 day treatment , the ratio of pancreatic wet weight / body weight was significantly lower in CCK A receptor ( / ) than ( + / + ) mice . ^^^ The protein and chymotrypsin contents were lower and amylase content was higher in CCK A receptor ( / ) mice , compared to ( + / + ) mice . ^^^ Camostat has a trophic effect on the pancreas in mice and this effect is mediated via the CCK A receptor , but is less potent than in rats . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist , devazepide ( which reverses protein induced food intake suppression ) , when given at 0 . 25 mg / kg , i . p . , 60 min before preloads of each of three soy hydrolysates , also blocked suppression of food intake , but the strength and duration of the interaction depended on the preparation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
MK 801 [ ( + / ) 5 methyl 10 , 11 dihydro 5 H dibenzo [ a , d ] cyclohepten 5 , 10 imine maleate ] , a competitive N methyl D aspartic acid ( NMDA ) receptor antagonist , or CNQX ( 6 cyano 7 nitroquinoxaline 2 , 3 dione ) , a non NMDA receptor antagonist , muscimol ( a GABA ( A ) receptor agonist ) , or baclofen ( a GABA ( B ) receptor antagonist ) , or sulfated cholecystokinin ( CCK 8 s ; CCK A receptor agonist ) , injected i . c . v . significantly reduced the inhibition of the tail flick response induced by platycodin D administered i . c . v . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Actions of CCK in the controls of food intake and body weight : lessons from the CCK A receptor deficient OLETF rat . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
L 364 , 718 , an antagonist for the CCK A receptor , blocked [ Ca ( 2+ ) ] ( 1 ) response to CCK 8 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The response was eliminated by the CCK A receptor antagonist lorglumide . ^^^ These results demonstrate that CCK acts at the low affinity site of the CCK A receptor to trigger the entry of extracellular calcium into vagal afferent neurons . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Systemic injection of CCK A receptor antagonists , devazepide ( 0 . 1 and 1 mg / kg , i . p . ) , 30 min before cocaine priming , significantly attenuated cocaine induced reinstatement of CPP , while CCK B receptor antagonist , L 365 , 260 ( 0 . 1 and 1 mg / kg , i . p . ) , did not show a similar effect . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Using a multifistulated model , intestinal transit was measured in four dogs , while 60 mM oleate was delivered into the proximal gut with either 0 or 6 mg naloxone , and 0 . 1 mg / kg devazepide ( a peripheral CCK A receptor antagonist ) administered intraluminally and intravenously , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
V . ) were compared between wild type Long Evans ( LE ) rats and the CCK A receptor deficient Otsuka LE Tokushima Fatty ( OLETF ) rats . ^^^ We studied whether the normally low phase 3 of LE rats can be enhanced by a CCK A receptor antagonist , sodium lorglumide ( 4 . 3 microg kg 1 min 1 , 120 min , I . ^^^ V . ) , and whether the normally high phase 3 of Wistar rats can be attenuated by a CCK A receptor agonist , sulphated CCK 8 ( up to 0 . 17 microg kg 1 min 1 , 120 min , I . ^^^ We conclude that the exaggeration of phase 3 in OLETF rats reflects a secondary trait of this strain and not the lack of the CCK A receptor per se . ^^^ None of the three known phases of the febrile response of rats to LPS requires the CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Association between the CCK A receptor gene and panic disorder . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
RESULTS : CCK 8 ( 10 nM ) or gastrin ( 10 nM ) reduced CCK A receptor mRNA expression to 56 % and 53 % , respectively 2 h after hormonal exposure . ^^^ The phorbolester PMA ( 100 nM ) , a protein kinase C activator , downregulated CCK A receptor expression but did not affect CCK B receptor gene transcription . ^^^ Both elevated CCK B and decreased CCK A receptor mRNA expression returned to basal levels 6 h after continuous stimulation . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In Experiment 2 , the effects of lecithin and a CCK A receptor antagonist on gastric emptying were examined using a modified phenol red recovery technique . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The pharmacological profile of CCK CHR resembled that of CCK B receptors using agonists ( CCK 8 , CCK 4 , gastrin 17 ) , whereas CCK CHR showed higher affinity for the CCK A receptor antagonist , devazepide , than for the CCK B receptor antagonist , L 365 , 260 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Functional vagal deafferentation by perineural capsaicin or CCK A receptor antagonist ( devazepide , 1 mg kg ( 1 ) , i . v . ) significantly reduced chylous lymph induced inhibition of gastric motility . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In donor gallbladders , the CCK contraction was abolished with the CCK A receptor antagonist , L 364718 , and significantly reduced by indomethacin . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor activates RhoA through G alpha 12 / 13 in NIH3T3 cells . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The series of in vivo and in vitro experiments included studies of 1 ) the feeding effect of peripheral enterostatin on Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lacking CCK A receptors , 2 ) the effect of CCK 8S on the intake of a two choice high fat ( HF ) / low fat ( LF ) diet , 3 ) the effects of peripheral or central injection of the CCK A receptor antagonist lorglumide on the feeding inhibition induced by either central or peripheral enterostatin , and 4 ) the ability of enterostatin to displace CCK binding in a 3T3 cell line expressing CCK A receptor gene and in rat brain sections . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK A receptor antagonist abolished the beta 51 63 induced suppression of food intake . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pancreatic regeneration after ethionine induced acute pancreatitis in rats lacking pancreatic CCK A receptor gene expression . ^^^ We used Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , a model lacking pancreatic CCK A receptor gene expression . ^^^ METHODS : Ethionine induced pancreatitis was induced in the 7 week old male OLETF rats and in a control group that does not lack the pancreatic CCK A receptor , Long Evans Tokushima Otsuka ( LETO ) rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Recently , a strain of rats ( Otsuka Long Evans Tokushima Fatty ( OLETF ) ) , lacking the CCK A receptor due to a genetic mutation , was discovered , providing a potentially useful tool to study the DA regulatory role of CCK A receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Activation of the high affinity state of the CCK A receptor with the synthetic peptide JMV 180 confirmed the physiologic relevance of the response . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Confocal immunofluorescence studies showed that the CCK A receptor and leptin were colocalized in the endoplasm . ^^^ This was reproduced by the high affinity CCK A receptor agonist , CCK OPE . ^^^ These results indicate that canine chief cells synthesize and secrete leptin in response to CCK via the high affinity state of the CCK A receptor . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK A receptor antagonist ( L 364 , 718 ) or CCK B receptor antagonist ( L 365 , 260 ) was injected intraperitoneally 15 min before leptin or CCK treatments . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
As Otsuka Long Evans Tokushima Fatty ( OLETF ) rats lack CCK A receptor because of a genetic abnormality , we examined whether learning and memory were impaired in these animals using both Morris water maze ( MWM ) and step through type passive avoidance ( PA ) learning test . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The recent discovery that subsets of rat taste receptor cells ( TRCs ) express the peptide cholecystokinin ( CCK ) and that subsets of TRCs respond to CCK with altered potassium currents or elevated intracellular calcium via CCK A receptor has lead to the hypothesis that CCK may play a novel signaling role within the taste bud , perhaps modifying tastant responses by co transmission with a classic transmitter . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In order to confirm this observation more directly in vivo , the EA mediated analgesic effects are compared between Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , the natural knockout rats with the homozygously disrupted CCK A receptor gene , with Long Evans Tokushima Otsuka ( LETO ) rats . ^^^ Our results suggest that the analgesic effect of acupuncture is closely related with the amount of CCK A receptor expression . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
MK 329 ( 0 . 4 mg / kg , 4 ) , the CCK A receptor antagonist , L 365 , 260 ( 0 . 4 mg / kg , 4 ) , the CCK B receptor antagonist and atropine ( 0 . 2 mg / kg , 4 ) , the M receptor antagonist , did not affect the OT effect on gallbladder motility . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Prior intraperitoneal treatment with lorglumide ( CR 1409 ) , a selective CCK A receptor antagonist , abolished the inhibitory effect of ethanol on the gastric emptying . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK and the Ca ( 2+ ) ionophore enhanced the Src related PTK activity , whereas the high affinity CCK A receptor agonists , fibroblast growth factor ( FGF ) , and the protein kinase C ( PKC ) activator had no or little effect . ^^^ Thus , Src cascades appear to be coupled to the low affinity CCK A receptor and utilize G ( q ) PLC pathways for their activation , independent of PKC and CaMK cascades . ^^^ The low affinity CCK A receptor regulates ROCI via mediation of Src related PTK and activates Src pathways to cause [ Ca ( 2+ ) ] ( o ) dependent pancreatic exocytosis . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This increased contractility was associated with up regulation of CCK A receptor mRNA levels in antral muscle . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A non invasive method for measurement of gastric emptying in mice : effects of altering fat content and CCK A receptor blockade . ^^^ Gastric emptying of cooked whole egg was also determined following administration of either vehicle or CCK A receptor antagonist , devazepide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pretreatment with lorglumide ( 1 . 0 mg / kg ip ) , a selective CCK A receptor antagonist , reversed CCK induced inhibition of sucrose intake . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The gene expressions of cholecystokinin ( CCK ) in the proximal small intestinal mucosa and CCK A receptor in the pancreas were examined in male and female young ( 4 8 months old ) and old ( 26 29 months old ) rats . ^^^ In males , but not in females , the mRNA levels of CCK in the intestine and those of the CCK A receptor in the pancreas were significantly lower in old than young rats . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pretreatment with the selective CCK A receptor antagonist lorglumide ( 0 . 3 3 microM ) attenuated the CCK8s induced inward current in a concentration dependent manner , with a maximum inhibition of 69 + / 12 % obtained with 3 microM lorglumide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In RT PCR , the presence of CCK A receptor and CCK B / gastrin receptor mRNA was detected in all biliary and pancreatic cancer cell lines . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The cholecystokinin A receptor ( CCK A receptor ; CCKAR ) and duodenal cholecystokinin 8 ( CCK ) revealed the associations of dioxin treatment with hormonal changes . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Furthermore , CCK ' s enhancement of distension induced Fos in Cap rats was reversed by the selective CCK A receptor antagonist lorglumide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effects of cholecystokinin ( CCK ) 8 on hypothalamic oxytocin secreting neurons in rats lacking CCK A receptor . ^^^ We examined the effects of intravenous ( 4 ) administration of CCK 8 on the neuronal activity of hypothalamic OXT secreting neurons and plasma OXT level in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats that have a congenital defect in the expression of the CCK A receptor gene . ^^^ These results suggest that peripheral administration of CCK 8 may selectively activate the hypothalamic OXT secreting neurons and brainstem neurons through CCK A receptor in rats . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Reverse transcription of meningioma derived RNA into cDNA followed by amplification by the polymerase chain reaction using specific primers for CCK peptide and its CCK A and / B receptor revealed 100 % presence of CCK peptide and CCK B receptors mRNA whereas CCK A receptor was expressed in 66 % of the meningiomas . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The expression of ghrelin , IAPP , and PYY and the CCK A receptor genes were examined in both gastrin and gastrin CCK double knockout ( KO ) mice using immunocytochemistry and quantitative RT PCR . ^^^ Fundic ghrelin cells expressed the CCK A receptor , and ghrelin expression increased after CCK infusion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
No amplified fragments of orexin 2 , NT 2 , and CCK A receptor cDNA were generated with GT 1 7 RNA , indicating that the GT 1 7 cells did not express mRNA of them . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Injection of the CCK A receptor antagonist 2 NAP abolished both the responses to CCK 8S and to gastric distension . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pretreatment with the CCK A receptor antagonist , lorglumide ( 1 microM ) , antagonized the effects of CCK 8s , whereas perfusion with the CCK B preferring agonist CCK 8 nonsulfated ( CCK ns , 1 microM ) did not affect the frequency of sEPSCs . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Those increases were abolished by the CCK A receptor blocker ( lorglumide ) , but not by the CCK B receptor blocker ( itriglumide ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The aims of the present study were to determine the time point when the administration of the CCK A receptor antagonist loxiglumide had its maximal suppressive effect on the proliferation of pancreatic acinar cells and to investigate the effects of loxiglumide on the cell cycle time of pancreatic acinar cells during transient acinar cell proliferation induced by endogenous or exogenous CCK . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Molecular cloning , expression and pharmacological characterization of the canine cholecystokinin 1 receptor . 1 The full length , canine cholecystokinin 1 ( CCK 1 ) receptor was cloned from gallbladder tissue using RT PCR with a combination of primers designed to interact with conserved regions of the human and rat CCK 1 receptor , which also shared homology with the canine genomic sequence . 2 Analysis of the sequence of the canine CCK 1 receptor revealed a 1287 base pair product , which encoded a 429 amino acid protein . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To examine the role of cholecystokinin 1 receptor ( CCK 1 ) in the activation of brainstem and myenteric neurons by CCK , we compared the ability of exogenous CCK 8 to induce Fos like immunoreactivity ( Fos LI ) in these neurons in Otsuka Long Evans Tokushima Fatty ( OLETF ) rats , lacking CCK 1 receptors , and Long Evans Tokushima Otsuka ( LETO ) controls . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The mouse cholecystokinin type A receptor ( CCK ( A ) R ) gene was cloned and sequenced , and the exon / intron boundaries were determined by cDNA cloning . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
A cyclic CCK 8 analogue selective for the cholecystokinin type A receptor : design , synthesis , NMR structure and binding measurements . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Behavioural studies performed after local injection of CCK 8 or BC 264 into the postero median part of the nucleus accumbens have shown the involvement of CCK A receptors in motivation and / or emotional states of rats . ^^^ These results suggest that endogenous CCK could play a critical role in mood modulation through CCK A / CCK B receptor stimulation . ^^^ Dysfunctioning of the CCK A / CCK B pathways could be implicated in anxiety and panic attacks . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Both the CCK A receptor antagonist lorglumide ( 48 mg kg ( 1 ) , i . v . ) and the CCK B receptor antagonist itriglumide ( 5 . 5 mg kg ( 1 ) , i . v . ) , given separately , prevented the expected increase in pentagastrin and , in addition , reduced the glandular protein synthesis by 16 and 12 % , respectively , below the level of saline treated rats . ^^^ In rats treated with saline only , the glandular protein synthesis was reduced by 22 % by the CCK A receptor antagonist and by 17 % by the CCK B receptor antagonist ; combined , the two antagonists caused no further reduction ( 20 % ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Intermolecular interactions were determined between a synthetic peptide corresponding to the third extracellular loop and several residues from the adjoining sixth and seventh transmembrane domains of the human cholecystokinin 1 receptor , CCK ( 1 ) R ( 329 357 ) , and the synthetic agonists Ace Trp Lys [ NH ( epsilon ) CONH o ( MePh ) ] Asp MePhe NH ( 2 ) ( GI 5269 ) and the C 1 N isopropyl N ( 4 methoxyphenyl ) acetamide derivative of 3 ( 1H Indazol 3ylmethyl ) 3 methyl 5 pyridin 3 yl 1 , 5 benzodiazepine ( GI 0122 ) , using high resolution nuclear magnetic resonance spectroscopy and computer simulations . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The Cholecystokinin 1 receptor ( CCK1R ) mediates actions of CCK in areas of the central nervous system and of the gut . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These data support the existence of a CCK receptor , located on raphe neurones in the rat , with a pharmacological profile very similar to that described for the CCKA type . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Incubation of nerve sections in the presence of both antagonists produced an additive effect , indicating that both CCK A and CCK B binding sites are transported towards the periphery . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Provided that devazepide acts solely by inhibiting CCK A receptors , we can conclude that endogenous CCK plays an important role in both normal and stimulated growth of the rat pancreas . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Both CCK A and CCK B / gastrin receptors are present on rabbit vagus nerve . ^^^ Autoradiographic studies in rats have demonstrated the presence of CCK A type receptors on vagus nerves . ^^^ A 71378 , a selective CCK A agonist , showed biphasic displacement curves , with the high affinity portion ( less than 10 nM ) accounting for approximately 60 % and the low affinity portion for approximately 40 % . ^^^ Under conditions which selectively examined vagal CCK A or CCK B / gastrin receptors , we demonstrated that a number of CCK subtype selective agonists and antagonists possessed similar affinities for the vagal CCK A and B / gastrin receptors as those found on the guinea pig pancreas ( CCK A ) and cerebral cortex ( CCK B ) , respectively . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK interacts with at least two types of receptor called CCK A and CCK B receptors . ^^^ Moreover , selective nonpeptide antagonists have been developed for CCK A and CCK B receptors . ^^^ CCK A receptors occur predominantly at the peripheral level where they are responsible for the digestive effects of CCK : intestinal and biliary smooth muscle contraction , pancreatic enzyme secretion , trophic effects on gastric and intestinal mucosa and regulation of feeding . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The CCK receptors can be subdivided into at least two subtypes , CCKA and CCKB on the basis of pharmacological studies . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Similarly , i . c . v . administration of CCK8s ( 0 . 1 microgram / kg ) abolished both ES and CRH stimulated colonic motility , an effect reproduced by central injection of JMV 180 , a cholecystokinin ( CCK ) derivative with high affinity for CCKA receptors , ( 1 microgram / kg ) , but not by JMV 170 , a CCK derivative with low affinity for CCKA receptor at similar or higher dose . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pharmacological experiments using selective CCK A and CCK B receptor antagonists demonstrate that CCK B is the prominent CCK receptor subtype in trigeminal and dorsal root ganglia neurons in the rat , rabbit , and monkey . ^^^ In the rat and rabbit spinal cord , CCK B binding sites are the prominent subtype , whereas in the monkey cord , CCK A is the prominent receptor subtype . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Subtype selective antagonists of the peripheral type ( CCK A ) and the central type ( CCK B ) cholecystokinin ( CCK ) receptors were employed to determine the receptor subtype ( s ) mediating the modulatory actions of CCK on dopamine induced changes in exploratory activity at three sites in the mesolimbic pathway of the rat . ^^^ The CCK A antagonist L 364 , 718 ( 10 ng ) blocked CCK potentiation of dopamine induced hyperlocomotion in the medial posterior nucleus accumbens . ^^^ These data indicate a CCK B pharmacology in the cell body and anterior terminal field , and a CCK A pharmacology in the posterior terminal field , of the mesolimbic dopamine pathway . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This effect was suppressed by the selective CCK B antagonist : L 365 , 260 , but not by the selective CCK A antagonist : MK 329 . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Pharmacological responses to CCK are mediated through at least two receptor subtypes termed CCK A and CCK B . ^^^ Using selective antagonists and a behavioural recognition test based on the olfactory discriminative capacities of rats , we found that endogenous CCK acting at CCK A and CCK B receptors modulates olfactory recognition positively and negatively , respectively . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Devazepide antagonizes the inhibitory effect of cholecystokinin on intake in sham feeding rats . 3S ( ) N ( 2 , 3 Dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepine 3 yl ) 1H indole 2 carboxamide ( devazepide ) , a potent and selective cholecystokininA ( CCKA ) antagonist , has been shown to reverse the inhibitory effect of exogenously administered CCK 8 on food intake . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Tetronothiodin inhibited [ 125I ] CCK 8 binding to rat brain CCKB receptors with an IC 50 of 3 . 6 nM , whereas it showed only weak affinity for rat CCKA receptors ( IC 50 = 70 microM ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
L 364 , 718 , a selective antagonist of CCK A receptors , caused further increase in gastric HCl and plasma gastrin responses to duodenal peptone but reduced the pancreatic protein outputs in these tests by about 75 % . ^^^ We conclude that CCK released by intestinal peptone meal , containing fat or acid , exerts a tonic inhibitory influence on gastric acid secretion and gastrin release through the CCK A receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK 8 stimulated insulin secretion in vivo is mediated by CCKA receptors . ^^^ The effects of the cholecystokinin A ( CCKA ) receptor antagonist , L 364 , 718 , and the CCKB receptor antagonist , L 365 , 260 , on CCK 8 stimulated insulin secretion were studied in vivo in the mouse . ^^^ It is concluded that the CCK 8 stimulated insulin release in vivo is mediated by CCK receptors of the CCKA subtype . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The brainstem solitary complex , which receives projections from primary sensory afferents of the vagus nerve , appears to be a crucial site for the action of the cholecystokinin octapeptide ( CCK 8 ) , because both peripheral type ( CCKA ) and central type ( CCKB ) binding sites are present in this structure . ^^^ L 364 , 718 , a potent antagonist of CCKA receptors , blocked delayed inhibition and replaced brief CCK 8 induced excitation by prolonged excitation . ^^^ Altogether , these results show that CCK 8 exerts , on neurons of the solitary complex , mixed effects due to simultaneous activation of CCKA inhibitory and CCKB excitatory binding sites . ^^^ The hypothesis that exogenous CCK 8 acts , in the solitary complex , through CCKA sites to slow down the motility of the digestive tract and through CCKB sites to modulate anxiety will be developed . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Satiety induced by endogenous and exogenous cholecystokinin is mediated by CCK A receptors in mice . ^^^ To investigate the relative participation of peripheral ( CCK A ) and central ( CCK B ) cholecystokinin ( CCK ) receptors in satiety induced by endogenous CCK , we examined the effect of the CCK A antagonist MK 329 ( 10 315 micrograms / kg ) and the CCK B antagonist L 365260 ( 0 . 1 315 micrograms / kg ) on intake of a 20 % sucrose solution in mildly food deprived mice . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To further explore the role of CCK in humans , the effect on satiety and eating behavior of a specific CCK receptor antagonist , loxiglumide , that preferentially inhibits peripheral ( CCK A ) receptors was investigated . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The ability of the CCKA receptor antagonists , lorglumide and loxiglumide , to inhibit CCK 8s induced contraction was also examined . ^^^ These results indicate that the primate iridial sphincter muscle exhibits a high sensitivity to CCK , and that CCKA receptor antagonists effectively block the CCK induced contraction . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
H ] pBC 264 , a suitable probe for studying cholecystokinin B receptors : binding characteristics in rodent brains and comparison with [ 3H ] SNF 8702 . [ 3H ] Propionyl Tyr ( SO3H ) gNle mGly Trp ( NMe ) Nle Asp Phe NH 2 ( [ 3H ] pBC 264 ) ( 98 100 Ci / mmol ) , a new peptidase resistant cholecystokinin ( CCK ) agonist that is 1000 fold more potent for CCK B than for CCK A receptors , interacts , with a similar subnanomolar affinity , with a single class of binding sites ( Kd , 0 . 15 0 . 2 nM ) in brain membranes of mouse , rat , guinea pig , and cat , in Tris and Krebs buffers . ^^^ The concentration of CCK A receptors in rodent brain was estimated to be 8 10 fmol / mg of protein , by measurement of the Bmax values of the nonselective agonist [ 3H ] propionyl CCK 8 , with or without 10 nM pBC 264 to saturate CCK B sites . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Although it has been demonstrated that the receptors which mediate this action are located in the periphery and are of the CCK A subtype , their anatomical location has not been firmly established . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCK B and CCK A binding affinities of these analogues are described and their CCK B affinity and selectivity rationalized by consideration of the pK ( a ) values , charge distribution , and geometry of the respective acid mimics . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
CCKA receptor antagonism inhibits mechanisms underlying CCK 8 stimulated insulin release in isolated rat islets . ^^^ It is concluded that insulin secretion , phosphoinositide hydrolysis , Ca2+ and K+ movements stimulated by CCK 8 in isolated islets are all events mediated by CCKA receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The neuroprotective effects of CCK were antagonized by L 365260 , a CCKB receptor antagonist , but not by L 364718 , a CCKA receptor antagonist . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Based on their relative affinities for cholecystokinin octapeptide ( 26 33 ) ( CCK 8 ) , cholecystokinin tetrapeptide ( 30 33 ) ( CCK 4 ) , desulfated CCK 8 , and gastrin , cholecystokinin ( CCK ) receptors have been classified as CCK A ( alimentary ) and CCK B ( brain ) . ^^^ Selective nonpeptide antagonists of CCK A and CCK B receptors , as well as highly selective CCK A and CCK B peptide agonists , have been described . ^^^ In radioligand binding assays , the IC 50 values for A 71623 and A 70874 were 3 . 7 and 4 . 9 nM in guinea pig pancreas ( CCK A ) and 4500 and 710 nM in cerebral cortex ( CCK B ) , respectively . ^^^ Both were agonists in stimulating pancreatic amylase release , and their stimulatory effects were potently inhibited by the CCK A antagonist L 364 , 718 . ^^^ Both peptides also were potent agonists in stimulating CCK A receptors in the ileum . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
To study the interdependence between gastric histamine release and acid secretion , we examined the effects of gastrin ( 1 17 ) [ G ( 1 17 ) ] or cholecystokinin ( 1 33 ) [ CCK ( 1 33 ) ] alone or combined with the gastrin ( CCK B ) antagonist L 365 , 260 or the CCK A antagonist L 364 , 718 in the isolated vascularly perfused rat stomach . ^^^ Gastrin or CCK A antagonist alone did not stimulate histamine release or acid secretion . ^^^ Maximally G ( 1 17 ) or CCK ( 1 33 ) stimulated histamine release and acid secretion was unchanged by the CCK A antagonist , while the gastrin antagonist induced a parallel and concentration dependent decrease in stimulated histamine and acid secretion . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
With Asperlicin as a guide , the new , selective , orally bioavailable , high affinity CCK A antagonist , MK 329 ( L 364 , 718 ; Devazepide ) and CCK B / gastrin antagonist , L 365 , 260 have been developed . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
With increasing age , significant changes were found only in CCK a true neural enteral peptide . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These results suggest that CCK acts at CCK A receptors to produce satiety during the dark period in ad lib feeding rats . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These findings indicate that CER stimulates the release of ir beta END from the adenohypophysis through CCK A receptors and that elevated plasma ir beta END levels is partly involved in some behavioural effects induced by CER . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Nonpeptide antagonists selective for the CCKA and CCKB receptors have recently been developed , and provide long awaited tools to test hypotheses about the role of endogenous CCK as a modulator of dopaminergic function , and the potential of CCK based drugs as treatments for neuropsychiatric disorders . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Hypolocomotion induced by peripheral or central injection of CCK in the mouse is blocked by the CCKA receptor antagonist devazepide but not by the CCKB receptor antagonist L 365 , 260 . ^^^ The pharmacological mechanisms underlying the hypolocomotion induced by intraperitoneal ( i . p . ) and intracerebroventricular ( i . c . v . ) injections of cholecystokinin octapeptide sulphated ( CCK ) in the mouse were examined using selective CCKA and CCKB receptor antagonists . ^^^ The hypolocomotion induced by i . p . injection of 10 micrograms / kg CCK and i . c . v . injection of 3 . 5 micrograms CCK was reversed by the selective CCKA antagonist devazepide , but not by the selective CCKB antagonist L 365 , 260 . ^^^ This suggests that CCK induced hypolocomotion is mediated by CCKA receptors . ^^^ CCK may be due to leakage of the peptide from the brain and subsequent activation of peripheral CCKA receptors . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
They are significant pharmacological tools for the study of CCK A ( peripheral ) and CCK B ( central ) receptors , their biological actions and their associated intracellular messengers . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The specific CCK A antagonist ( L 364 , 718 ) increased gastric emptying of protein rich meals . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
It is concluded that CCK 8 released after a meal is responsible for the postprandial increase in colonic motility and that these effects may be mediated through activation of central CCKA receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
These CCK binding sites displayed a typical CCK B pharmacological profile , established by use of several agonists and antagonists selective for the CCK receptor types , namely compound L 364 , 718 , the Merck CCK antagonist selective for the peripheral CCK receptor ( CCK A ) , and compound L 365 , 260 , the Merck CCK antagonist selective for the central CCK receptor ( CCK B ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
Effect of intracerebroventricular and systemic injections of caerulein , a CCK analogue , on electrical self stimulation and its interaction with the CCKA receptor antagonist , L 364 , 718 ( MK 329 ) . ^^^ It is concluded that self stimulation performance may be subject to modulation by CCK receptors distributed predominantly in the peripheral nervous system and that some but not all of these receptors are CCKA receptors . . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In the present study , we analyzed the proliferative effects of cholecystokinin ( CCK ) and gastrin peptides on a rat tumoral pancreatic cell line , AR42J , which possesses both CCKA and CCKB receptor subtypes . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In contrast , after administration into the postero median nucleus accumbens , the hypoexploration , the increase of emotionality of rats , or the potentiation of dopamine induced hyperlocomotion were obtained after injection of CCK 8 but not of BC 264 , supporting the involvement of peripheral CCKA receptors in these CCK 8 responses . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
In homogenate binding studies , L 365 , 260 displayed nanomolar affinity for CCK B receptors in the cerebral cortex of several species including man ( pIC 50 congruent to 8 . 2 ) but showed low affinity for CCK A receptors in the rat pancreas ( pIC 50 congruent to 6 . 3 ) . ^^^ By contrast , the CCK A antagonist MK 329 showed the reverse selectivity ( cortex : pIC 50 congruent to 6 . 9 , pancreas : pIC 50 = 9 . 6 ) . ^^^ L 365 , 260 inhibited binding to most areas of the brain , but in the rat medial nucleus tractus solitarii and the monkey nucleus tractus solitarii . dorsomedial nucleus and infundibular hypothalamic nuclei together with the dorsomedial aspects of the caudate nucleus , where CCK A sites are present , L 365 , 260 failed to displace all 125I BH CCK binding . ^^^ In the primate spinal cord , L 365 , 260 was a relatively weak inhibitor of 125I BH CCK binding ( pIC 50 congruent to 6 . 0 ) whereas MK 329 showed high affinity for the CCK A sites present there ( pIC 50 congruent to 9 . 6 ) . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
The effects of the selective CCK A antagonist L 365 , 031 and the selective CCK B antagonist L 365 , 260 on morphine analgesia and opiate tolerance and dependence in rats were examined . ^^^
Interacting proteins: P32238 and P06307 Pubmed SVM Score :0.0
This effect was reversed by prior treatment with MK 329 , a selective antagonist of CCK at alimentary type CCK ( CCK A ) receptors . ^^^ Thus , endogenous , small intestinal CCK can cause satiety in the neonatal rat and this effect involves CCK A receptors . . ^^^