| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.88841056 |
| 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 . 0.88841056^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Potent and selective CCK B agonists with good bioavailability have been designed by modifying the natural CCK 8 peptide . ^^^ Thus , BC 264 [ Boc Tyr ( SO3H ) gNle mGly Trp Me ( Nle ) Asp PheNH 2 ] is a highly potent ( 0 . 15 nM ) and selective agonist for CCK B receptors which cross the blood brain barrier . ^^^ In the anterior part , CCK B receptor stimulation could be involved in attention and memory processes . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Some brain CCK receptors belong to the A type , but the majority of them are CCK B receptors . ^^^ High densities of brain CCK B receptors are present in cortical and limbic areas such as the amygdala and the hippocampus . ^^^ At the peripheral level , CCK B receptor antagonists are active on gastrin receptors , and these two receptors are similar if not identical . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| This is the case of BUBU , Tyr D Ser ( OtBu ) Gly Phe Leu Thr ( OtBu ) and BUBUC , Tyr D Cys ( OtBu ) Gly Phe Leu Thr ( OtBu ) for the opioid delta receptors and of BC 254 , Boc gamma D Glu Tyr ( SO3H ) Nle D Lys Trp Nle Asp PheNH 2 and of BC 264 , Boc Tyr ( SO3H ) gNle mGly Trp MeNle Asp PheNH 2 for central CCK B receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Both CCK A and CCK B / gastrin receptors are present on rabbit vagus nerve . ^^^ Competitive binding studies using A 63387 , a selective CCK B / gastrin receptor agonist , also showed biphasic displacement curves , with the high affinity portion ( less than 30 nM ) at approximately 40 % and the low affinity portion at approximately 60 % . ^^^ 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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ These results demonstrate that CCK B receptors are expressed by a substantial percentage of dorsal root ganglion neurons at all spinal levels , and that CCK may antagonize opiate analgesia at the level of the primary afferent neuron itself . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| This was quantified by measuring the effects of both inhibitors on the in vivo binding of [ 3H ] propionyl Tyr ( SO3H ) gNle mGly Trp ( N Me ) Nle Asp Phe NH 2 ( [ 3H ] pBC 264 ) , a selective and highly potent CCK B agonist . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The pharmacologic properties of the parietal cell gastrin receptor are very similar to the predominant CCK receptor in the brain , CCK B . ^^^ Neither the gastrin nor the CCK B receptor have been cloned thus far , making it difficult to resolve whether these two receptors are distinct . ^^^ Gastrin receptor transcripts were identified by high stringency RNA blot analysis in both parietal cells and cerebral cortex , suggesting that the gastrin and CCK B receptors are either highly homologous or identical . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , CCK binding sites accumulating distal to the ligature possessed the pharmacological characteristics of the CCK B receptor sub type only . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ However , intraventricular administration of the CCK B receptor agonist A 63387 at 10 nmol / kg had no effect on 30 min meal size ( % suppression = 18 + / 29 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ CCK B receptor antagonists therefore have facilitatory potentialities on memory processes . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The new compounds were assayed in CCK binding assays using homogenated rat pancreatic membranes and bovine striatum as a source of CCK A and CCK B receptors respectively and in vivo in rats for anorectic activity . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In the present study , we investigated gastrin ( CCK B ) receptor expression in the azaserine induced rat pancreatic carcinoma DSL 6 , comparing it to normal rat pancreas , and we also characterized CCK receptor subtypes in this tumor . ^^^ 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 . ^^^ The binding capacity of CCK B receptors constitutes 34 % of the total high affinity CCK binding sites . ^^^ Gastrin ( CCK B ) receptors , which were not detected in normal rat pancreas , constitute about one third of the total high affinity CCK receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| To this end , we tested the effects of both unselective CCK agonists CCK 8 and caerulein , and CCK B selective agonists CCK 4 and pentagastrin as well as the selective CCK antagonists ( devazepide and L 365 , 260 ) at wide dose ranges on the cold stimulated and TRH induced TSH and PRL secretion . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B agonist , BC 264 injected in the antero lateral part of the nucleus accumbens , reduces the spontaneous alternation behaviour of rats . ^^^ The aim of this study was to examine the behavioural effects induced by stimulation of CCK receptors in the nucleus accumbens of the rat , which contains a high density of heterogenously distributed CCK B receptors . ^^^ The drug BC 264 ( Boc Tyr ( SO3H ) gNle mGly Trp ( NMe ) Nle Asp Phe NH 2 ) , a highly potent and selective CCK B agonist , injected into the postero median or antero median n . accumbens did not modify the spontaneous alternation and exploratory behaviour observed in a Y maze . ^^^ This effect was suppressed by the selective CCK B antagonist : L 365 , 260 , but not by the selective CCK A antagonist : MK 329 . ^^^ These results emphasize the functional heterogeneity of the CCK network in the n . accumbens of the rat and the participation of the peptide in the expression of alternation behaviour , through stimulation of CCK B receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 B antagonist CI 988 ( 20 ng ) blocked CCK inhibition of dopamine induced hyperlocomotion in the anterior nucleus accumbens . ^^^ The CCK B antagonists CI 988 ( 20 ng ) and L 365 , 260 ( 10 ng ) blocked CCK potentiation of dopamine induced hypolocomotion in the ventral tegmental area . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ However , the effect of CCK on cortisol secretion does not appear to involve either CCK A or CCK B receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| A Free Wilson / Fujita Ban analysis of some alpha methyltryptophan derivatives as CCK B antagonists . ^^^ A Free Wilson / Fujita Ban ( FW / FB ) analysis is reported on 36 `` dipeptoid ' ' antagonists of the CCK B receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In contrast , i . c . v . , but not i . p . , injections of the selective CCK B receptor agonist A 63387 , reduced food intakes , although on a molar basis the effect was much less than that seen with A 71623 . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , in rat brain the affinity of [ 3H ] pBC 264 was decreased and the maximal number of binding sites was increased by NaCl and the guanyl nucleotide or by alkaline treatment , suggesting that a proportion of CCK B receptors are linked to guanine nucleotide binding proteins . ^^^ The CCK B antagonist L 365 , 260 was 18 , 30 , and 64 fold less potent than [ 3H ] pBC 264 in guinea pig , mouse , and rat , respectively . ^^^ PD 134308 , a CCK B antagonist , was 20 fold less potent in rat brain than in guinea pig brain . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Acid mimics of the potent and selective non peptide CCK B receptor antagonist CI 988 . ^^^ This paper outlines the synthesis of selected acid mimics of the non peptide CCK B selective antagonist CI 988 , 1 . ^^^ 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 . ^^^ Several of the compounds have CCK B binding affinities similar to the parent carboxylic acid 1 ( CCK B , IC 50 = 1 . 7 nM ; pK ( a ) = 5 . 6 ) and span a pK ( a ) range of less than 1 ( sulfonic acid 27 ) to greater than 9 . 5 ( 5 thio 1 , 2 , 4 triazole 24 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| However , the specific CCK B receptor antagonist , L 365 , 260 ( 10 nM ) , did not alter the presynaptic facilitatory effect of CCK 8 . 6 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Four analogues of cholecystokinin ( CCK ) octapeptide having analgesic activity after i . c . v . administration and high affinity for CCK B receptors were studied for their ability to displace specific ligands , [ 3H ] D Phe Cys Tyr D Trp Orn Thr Pen Thr NH 2 . [ 3H ] [ D Pen 2 , 4 ' Cl Phe 4 , D Pen 5 ] enkephalin and [ 3H ] U 69 , 593 , for mu , delta and kappa opioid receptors , respectively . ^^^ The results suggest a relationship between the ligand requirements of CCK B and delta opioid receptors which further implies a possible structural relationship between these receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Rationally designed `` dipeptoid ' ' analogues of CCK . alpha Methyltryptophan derivatives as highly selective and orally active gastrin and CCK B antagonists with potent anxiolytic properties . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Neurochemical actions of CCK underlying the therapeutic potential of CCK B antagonists . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In an effort to evaluate CCK antagonists as potential antipsychotic drugs , we have examined the effects of a selective CCK B antagonist , LY 262691 , on the number of spontaneously active midbrain dopamine neurons using extracellular , single unit recordings in anesthetized rats . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) analogues ( JMV 310 , JMV 320 , JMV 328 , and JMV 332 ) , obtained by side chain to side chain cyclization of a lysine residue in position 28 with a lysine residue in position 31 , were found to be highly selective for the brain CCK receptor ( CCK B receptor ) , both in guinea pig and rat . ^^^ In these analogues , the C terminal tetrapeptide region of the molecule , which is the crucial determinant for binding to CCK B receptors , has been constrained by cyclization . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , the CCK B receptor antagonist , L 365 , 260 , did not affect contraction to CCK 8S ( log KB less than 7 ) but potently inhibited contraction to CCK 4 ( log KB = 9 . 24 ) . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ They were , however , weak and behaved as partial agonists in calcium studies in NCI H 345 cells , which possess CCK B / gastrin receptors . ^^^ In guinea pig gastric glands , the affinities of A 71623 and A 70874 for the CCK B / gastrin receptor were 11 and 1 . 6 microM , respectively . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B ( gastrin ) receptor regulates gastric histamine release and acid secretion . ^^^ 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 . ^^^ We conclude that G ( 1 17 ) and CCK ( 1 33 ) stimulate histamine and acid secretion by a CCK B ( gastrin ) receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The effect of intravenous ( i . v . ) PD 134308 , which is a CCK B antagonist , morphine and intrathecal ( i . t . ) galanin ( GAL ) on the excitability of the spinal nociceptive flexor reflex and in the hot plate test was examined in rats . ^^^ The results demonstrate that a CCK antagonist directed to the central CCK B receptor potentiates the analgesic effects of opioid and non opioid drugs at spinal level in the rat , thus supporting the notion that CCK in the CNS may be an endogenous , physiological opioid antagonist . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ L 365 , 260 is the more potent , suggesting a role for central CCK B type receptors in satiety . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Chemical manipulations of the structure of lorglumide led to the discovery of selective antagonists of the CCK B / gastrin receptors . ^^^ Some of these new derivatives exhibit different affinities with rabbit gastric gland cells and rat cortex membranes , suggesting that the stomach gastrin receptor ( arbitrarily termed CCK B 1 receptor ) is not as closely related to the CCK central receptor ( termed CCK B 2 ) as previously hypothesized . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Compound 9 possesses a selectivity of greater than 500 fold for the pancreatic CCK A receptor over the CCK B receptor . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Development of CCK B antagonists . ^^^ Our approach to design small molecule non peptide analogues of the neuropeptide cholecystokinin ( CCK ) has led to the discovery of the CCK B antagonist ' dipeptoids ' . ^^^ This dipeptide has been systematically chemically modified at the N and C terminal to increase CCK B binding affinity 10 , 000 fold . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Three of the rats that increased food intake after DVZ were also tested with L 365 , 260 , an antagonist selective for the CCK B receptor ( 10 ng / kg 100 micrograms / kg ) . ^^^ They do not , however , demonstrate a role for the CCK B receptor in mediating the satiating effect of ingested food under the same experimental conditions . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| PD 134308 and PD 135158 are potent and selective antagonists at the cholecystokinin type B ( CCK B ) receptors with IC 50 values of 1 . 6 nM and 3 . 5 nM , respectively , in the radioligand binding assay and Ke values of 7 . 82 and 12 . 9 nM , respectively , in their blocking action on CCK responses in the rat lateral hypothalamic slice . ^^^ Both CCK B antagonists were able to suppress the withdrawal anxiogenesis and produce an anxiolytic effect in mice previously made tolerant to diazepam . ^^^ The CCK B antagonists also showed powerful anxiolytic activity in the `` marmoset human threat test . ' ' These results provide evidence of a selective role for CCK B receptors in the control of anxiety . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ L 365 , 260 was more potent , suggesting that central CCK B type receptors may mediate the satiety effects of endogenously released CCK . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ The intracerebroventricular administration of the nonselective CCK receptor agonist caerulein or the selective CCK B receptor agonist pentagastrin increased dose dependently the level of anxiety . ^^^ These results strongly suggest that activation of the brain CCK B receptor induces anxiety and that selective antagonists of this receptor represent a separate class of anxiolytic agents . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B receptor agonist , BC 264 , in doses ranging from 0 . 88 to 7 nmol . kg 1 . h 1 , had no effect on milk intake under sham feeding conditions , although it dose dependently stimulated gastric acid output . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Proglumide does not discriminate between CCK A and CCK B ( central type ) receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ The CCK cyclic analogue recently developed in our laboratory that is highly selective for the CCK B receptor ( i . e . , JMV 320 ) also showed high affinity for the CCK receptor on the JURKAT cell line . ^^^ The presence of CCK B like binding sites on a lymphoid cell line could provide a useful model for pharmacological characterization of CCK B binding sites and could contribute to a better understanding of their regulation . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| BC 264 , a highly selective CCK B receptor agonist , did not decrease consumption of a palatable meal when administered either i . p . or into the lateral ventricles of the brain , whereas CCK decreased feeding when administered i . p . at the same doses . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We showed that : 1 ) Suppression of the C terminal phenylalanine residue leads to peripheral as well as central cholecystokinin receptor antagonists ; 2 ) Suppression of the C terminal amide function produces `` partial agonists ' ' exhibiting interesting biological and pharmacological activities ; 3 ) Replacement of L tryptophan residue by D tryptophan in such `` partial agonist analogues ' ' resulted in potent CCK receptor antagonists ; 4 ) The peptide bond between methionine 28 and glycine 29 , as well as the glycine residue are quite significant for the central biological activity ; 5 ) It is possible to obtain highly potent and selective CCK analogues for the central receptor ( CCK B ) by cyclization including the C terminal tetrapeptide . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The results suggest that the exploratory behaviour of rats can be altered by pharmacological manipulations at CCK B receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK antagonists interact with CCK B receptors on human small cell lung cancer cells . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| A new , highly selective CCK B receptor radioligand ( [ 3H ] [ N methyl Nle 28 , 31 ] CCK 26 33 ) : evidence for CCK B receptor heterogeneity . [ N methyl Nle 28 , 31 ] CCK 26 33 ( SNF 8702 ) is a nonsulfated cholecystokinin octapeptide analog that is highly selective for cholecystokinin B ( CCK B ) receptors . ^^^ In contrast to findings of single site binding in some brain regions , evidence for CCK B receptor heterogeneity is observed under other conditions . [ 3H ] SNF 8702 binding to membranes prepared from whole guinea pig brain shows biphasic association kinetics at a concentration of 2 . 0 nM consistent with the presence of binding site heterogeneity . ^^^ CCK B receptor heterogeneity is suggested by the effect of the guanyl nucleotide analogue , guanylyl imidodiphosphate ( Gpp ( NH ) p ) , on [ 3H ] SNF 8702 binding to CCK B receptors in the cerebellum . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B receptor antagonist L 365 , 260 enhances morphine analgesia and prevents morphine tolerance in the rat . ^^^ 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 . ^^^ This rank order correlates well with the potency of the antagonists in blocking CCK B receptors in rodents and suggests that CCK / opiate interactions in this species are mediated by CCK B receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ 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 . ^^^ In contrast , A 71378 was relatively weak ( EC 50 = 600 nM ) in mobilizing intracellular calcium from NCI H 345 cells , which express CCK B / gastrin receptors . ^^^ The high potency and selectivity of A 71378 for the CCK A over CCK B and gastrin receptors is unprecedented among CCK peptides . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Activation of ornithine decarboxylase was triggered via a CCK B receptor type not involved in pancreatic secretion . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Postponement of satiety by blockade of brain cholecystokinin ( CCK B ) receptors . ^^^ 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 . ^^^ These results suggest that endogenous CCK causes satiety by an agonist action on CCK B receptors in the brain . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ We describe here the properties of tert butyloxycarbonyl Trp Leu Asp Phe NHNH 2 ( A 57696 ) , a C terminal hydrazide analogue of tert butyloxycarbonyl CCK 4 ( Boc Trp Met Asp Phe NH 2 ) , at four cholecystokinin ( CCK ) receptor bearing tissues , the guinea pig pancreas and gall bladder ( Type A ) , guinea pig cortex ( Type B ) , and NCI H 345 cells , a human small cell lung cancer cell line that expresses CCK B / gastrin receptors . ^^^ 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 ) . ^^^ In contrast , A 57696 behaved as a partial agonist ( 80 % of maximal CCK 8 response ) in stimulating calcium mobilization at CCK B / gastrin receptors on NCI H 345 cells . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 B receptors are found ubiquitously throughout other regions of the neuraxis . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , selective and biologically active CCK B agonist had no effect . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Binding of raclopride to dopamine D 2 , SCH 23390 to dopamine D 1 , ketanserin to serotonin 5 HT 2 , 8 hydroxy 2 ( di n propylamino ) tetralin to serotonin 5 HT1A , and cholecystokinin ( CCK ) 8 to CCK B sites was measured in tissue homogenates from the striatum or fronto parietal cortex . ^^^ Binding to striatal D 1 and frontoparietal cortex CCK B sites was reduced over the course of a 27 h postmortem delay . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK B selective antagonist L 365 , 260 ( ( 3R ( + ) 2 , 3 dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepine 3yl ) N ( 3 methylphenyl ) urea ) was inactive up to a concentration of 30 nM . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| METHODS : In the present study we examined the effect of cionin on histamine release and acid secretion of the stomach , both effects being mediated by CCK B / gastrin receptors . ^^^ 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 . ^^^ CONCLUSION : Cionin is a potent and efficient stimulator of gastric histamine release and acid secretion interacting via a CCK B receptor . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We examined neuroendocrine responses to intravenous infusions of pentagastrin , a selective CCK B receptor agonist , in 10 patients with panic disorder and 10 normal control subjects . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor mRNA was expressed in fetal and adult pancreas in both strains . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Conformationally readdressed CCK B / delta opioid peptide ligands . ^^^ The sequence of a cholecystokinin ( CCK ) related peptide was modified to obtain analogues , which interact selectively either with CCK B , or with delta opioid receptors . ^^^ 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 . ^^^ The results of this study demonstrate a possibility to redirect a peptide sequence that interacts with one type of receptors ( CCK B receptors ) toward interaction with another type ( delta opioid receptors ) belonging to a different physiological system . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Since CCK can function as a satiety factor when administered to rodents , localization of Cckbr near the tub mutation identifies this receptor as a possible candidate gene for this obesity mutation . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Exogenously applied CCK depolarizes supraoptic neurons , acting at postsynaptic CCK B type receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK B receptor antagonist Cl 988 reverses tolerance to morphine in rats . ^^^ The ability of the selective cholecystokinin B ( CCK B ) receptor antagonist Cl 988 to reverse tolerance to morphine ' s antinociceptive effect was investigated with the hot plate test in Sprague Dawley rats . ^^^ Significant antinociception was observed in the group that received the CCK B antagonist plus morphine , whereas the saline plus morphine group exhibited total tolerance . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK B receptor gene was expressed in the hypothalamus in both strains . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Derived by chemical modification of the benzodiazepine ring system embedded within the CCK B antagonist L 365 , 260 , these compounds display CCK B / CCK A selectivity and some analogs have receptor binding affinities in the subnanomolar range . ^^^ This group of novel imidazobenzodiazepines , among which N [ ( 2S , 4R ) methyl 6 phenyl 2 , 4 dihydro 1H imidazo [ 1 , 2 alpha ] [ 1 , 4 ] benzodiazepin 4 yl ] N ' [ 3 methylphenyl ] urea ( 12 ) is the principal compound , expands the structural diversity of the collection of non peptide CCK B antagonists and will be useful in further delineating the function of CCK in the central nervous system . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B agonist , BC 264 , impairs socially reinforced memory in the three panel runway test in rats . ^^^ The role of CCK B receptor activation in memory processes has been reassessed using the three panel runway task , under conditions which avoid the effects of CCK on satiety and reduce emotional responses . ^^^ BC 264 , a highly selective CCK B agonist , peripherally administered or infused into the anterolateral part of the nucleus accumbens also impaired memory . ^^^ These effects were suppressed by L 365 , 260 supporting the involvement of CCK B receptors and of the nucleus accumbens in memory processes . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Absence of detectable cholecystokinin ( CCK ) A and CCK B receptors . ^^^ Receptor subtypes , cholecystokinin ( CCK ) A and CCK B , for a closely related peptide , cholecystokinin , were recently cloned . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Gastrin ( 2 17 ds ) increased cell proliferation by 2 fold with an IC 50 of 150 pM , corresponding to the occupancy of the CCK B receptors . ^^^ CR 1409 , at concentrations that fully occupied CCK B receptors , inhibited the gastrin ( 2 17 ds ) effects . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| RESULTS : In the cardiac and fundic stomach , CCK B / gastrin receptors were found in the mucosa and in a subpopulation of neuronal elements in the circular muscle . ^^^ The antrum expressed CCK B / gastrin receptors in a few neurons in the circular muscle and in the entire myenteric plexus ; no receptors were observed in the antral mucosa or esophagus . ^^^ The duodenum showed a high concentration of CCK B / gastrin receptors in the myenteric plexus . ^^^ CCK B / gastrin receptor expression in a subset of neurons in gastric circular muscle suggests a novel site of action for CCK and / or gastrin . . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Heterogeneity of CCK B receptors involved in animal models of anxiety . ^^^ The effects of the selective CCK B agonists , BC 264 and BC 197 , and the nonselective CCK agonist BDNL were investigated in the elevated plus maze in rats . ^^^ 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 . ^^^ Together these results give pharmacological and behavioral evidence for the existence of CCK B receptor subtypes . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In this review , the studies evaluating the putative involvement of CCK , and especially CCK B receptors , in panic disorder will be discussed . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ These results demonstrate directly for the first time that guinea pig chief cells possess CCK A R and CCK B R . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Receptors for cholcystokinin ( CCK ) can be pharmacologically classified into at least two distinct subtypes , CCKAR and CCKBR . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We compared the gastrin / CCK B receptor blocking properties of this compound with those of the racemate ( mixture of YM 022 and its S form ) , its enantiomer ( S form ) , L 365 , 260 and Cl 988 in vitro and in vivo . ^^^ YM 022 replaced specific binding of [ 125I ] CCK 8 to rat brain gastrin / CCK B receptors in a stereoselective and competitive manner . ^^^ The Ki value of YM 022 for gastrin / CCK B receptors in brain were estimated to be 0 . 068 nM . ^^^ The racemate , the S form of YM 022 , L 365 , 260 and Cl 988 also replaced gastrin / CCK B receptor binding , with Ki values of 0 . 11 , 140 , 19 and 6 . 3 nM , respectively . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| All had essentially the same sequence contained within 2 of these clones consisted of 427 amino acids and was 92 % homologous ( 87 % identity ) to the known rat pancreatic CCK A sequence but only 43 % homologous to the gastric CCK B sequence . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ This effect appears to be mediated by CCK B receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Electrophysiological studies on slices of rat ventromedial hypothalamic nucleus showed that L 740 , 093 produced rightward shifts of the concentration response curve for the CCK B receptor agonist pentagastrin ( Kb of 0 . 06 nM ) . ^^^ These studies demonstrate that L 740 , 093 is the most potent and selective CCK B antagonist yet described and that it has excellent central nervous system penetration . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ) . ^^^ In contrast , the selective CCK B agonist BC 264 ( 62 micrograms / kg i . v . ) produced a hyperalgesic effect that was antagonized by 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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The present findings demonstrate an opposing physiological role of endogenous CCK , acting on CCK B receptors , and opioid peptides in the control of pain perception at both spinal and supraspinal levels . ^^^ These results could have important clinical applications because a combination of a CCK B antagonist and RB 101 , which has been showed to be almost devoid of morphine side effects , would increase the overall antinociceptive efficacy into a range that will be more clinically useful . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Modification of `` peptoid ' ' CCK B antagonists to probe requirements for CCK B agonist activity . ^^^ This paper describes the use of the non peptidal N ( 2 adamantyloxycarbonyl ) alpha methyl tryptophan phenylethylamide template of the `` peptoid ' ' CCK B antagonist compounds 1 as a basis to probe the functional group requirements of the CCK B receptor in order to produce an agonist response . ^^^ Comparison of the peptoid template with inter group distances in a fully extended conformation of the endogenous CCK B agonist CCK 30 33 led to the design of a series of compounds 2 containing additional Ph , COOH and CONH 2 , functions at distances from the Trp indole ring that are able to mimic those in the natural ligand . ^^^ The effect of these modifications was then assessed by measurement of CCK B binding affinities and potential agonist efficacy was investigated by comparison with contraction of guinea pig isolated stomach corpus muscle strip stimulated by the CCK B agonist pentagastrin . ^^^ All compounds ( except 2f ) were shown to be good CCK B antagonists ; no compounds showed significant agonist activity up to a concentration of 1 microM . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Conformationally restricted analogues of the potent CCK B antagonist CI 988 . ^^^ This strategy has led to conformationally more rigid derivatives that have increased CCK B receptor binding affinity . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Effects induced by BC 264 , a selective agonist of CCK B receptors , on morphine dependent rats . ^^^ Rats were made dependent to morphine and the ability of cholecystokinin octapeptide ( CCK 8 ) and Tyr ( SO3H ) gNle mGly Trp ( NMe ) Nle Asp Phe NH 2 ( BC 264 ) , a selective agonist of CCK B receptors , to induce signs of morphine withdrawal after ICV injection was tested . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B antagonists inhibit the activity of brain dopamine neurons . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Since the effect of L 365 , 260 was 25 times more potent than Devazepide , it suggests that the anti opiod effect of CCK in amygdala is mediated by CCK B receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The effects of cholecystokinin ( CCK ) A , CCK B , and 5 hydroxytryptamine 2 ( 5 HT 2 ) receptor antagonists on the postprandial myoelectric activity of the ileum and the proximal and distal colon in rats were studied . ^^^ In contrast , L 365 , 260 , a CCK B receptor antagonist , had no effect . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| L 365 , 260 ( [ 3R ( + ) 2 , 3 dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepine 3 yl ] N ' [ 3 methyl phenyl ] urea ) , a CCK B antagonist , also decreased ceruletide induced protection . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The mechanisms of its analgesic actions were assessed by administering antagonists selective for CCK ( cholecystokinin octapeptide , sulfated ) A and CCK B receptors , as well as specific antagonists for the mu opioid receptor ( D Phe Cys Tyr D Trp Arg Thr Pen Thr NH 2 , 1 microgram i . c . v . ) , the delta 1 opioid receptor [ D Ala 2 Leu5 , Cys 6 ] enkephalin , 4 . 57 nmol i . c . v . , 24 hr pretreatment ) , the delta 2 opioid receptor ( naltrindole benzofuran , 25 pmol i . c . v . ) and the kappa opioid receptor ( nor binaltorphimine , 10 mg / kg s . c . ) . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Novel CCK analogs for studying CCK B receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The cholecystokinin ( CCK ) B receptor cloned from human brain was characterized as a gastrin receptor by using heterologous expression systems of COS 7 cells and Xenopus oocytes . 125I gastrin binding to human CCK B receptor expressed in COS 7 was time dependent , saturable and also specific , as well as 125 1 CCK 8 . ^^^ Addition of GTP gamma S , a nonhydrolysable analog of GTP , dose dependently inhibited 125I gastrin binding , and lowered the gastrin binding affinity , Gastrin ( 10 ( 9 ) 10 ( 7 ) M ) also evoked a Ca ( 2+ ) dependent Cl current in Xenopus oocytes expressing CCK B receptors . ^^^ These results suggest that the pharmacological profile of the cloned human CCK B receptor using 125I gastrin is closely parallel to that reported in gastric mucosa , and that the receptor transduces cellular signals of gastrin as well as those of CCK 8 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Previous studies have shown that central administration of nanogram dose of CCK 8 totally abolished morphine analgesia in the rat , an effect mediated by CCK B receptor in central nervous system . ^^^ In the present study CCK B antagonist L 365 , 260 was injected intracerebroventricularly ( icv ) to Wistar rats to see its effect on the analgesic effect induced by electroacupuncture ( EA ) stimulation . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Details of the ability to modulate the receptor interactions of these benzodiazepines by appropriate structure modifications are discussed which imply the possibility of further refining the CCK B receptor affinity and selectivity of this class of compounds . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Using receptor binding assays , we have previously demonstrated the overexpression of the high affinity cholecystokinin ( CCK ) receptor and the novel expression of the gastrin ( CCK B ) receptor in the azaserine induced rat pancreatic carcinoma DSL 6 . ^^^ 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 . ^^^ The 32P labelled cDNA probe of the CCK B receptor coding region hybridized with an approximately 2 . 7 kb mRNA from DSL 6 pancreatic carcinoma ; no hybridizing mRNA could be identified from 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The effects of intracerebroventricular administration of the cholecystokinin ( CCK ) analogue , BDNL , and the selective CCK B agonist , BC 264 , were determined using the hot plate test in mice . ^^^ In contrast , the selective CCK B agonist BC 264 produced , at one dose ( 2 . 5 nmol ) , a slight decrease in the lick latency that was only antagonized by the CCK B antagonist . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Temporal expression of the gastrin ( CCK B ) receptor during azaserine induced pancreatic carcinogenesis . ^^^ Cholecystokinin ( CCK A ) and gastrin ( CCK B ) receptors have been demonstrated in the azaserine induced rat pancreatic carcinoma DSL 6 . ^^^ In order to determine at what stage in azaserine induced pancreatic carcinogenesis gastrin ( CCK B ) receptors are first expressed , we examined the binding of [ 125I ] gastrin 1 to normal rat pancreas , azaserine induced premalignant pancreatic nodules , grossly normal internodular pancreas , and DSL 6 carcinoma . ^^^ We observed that specific gastrin binding was absent in normal pancreas , premalignant nodules , and internodular pancreas , and also reconfirmed our previous report of marked overexpression of gastrin ( CCK B ) receptors in the DSL 6 carcinoma . ^^^ Therefore , we conclude that the presence of gastrin ( CCK B ) receptors in the azaserine induced pancreatic carcinoma DSL 6 , in contrast to their absence in premalignant nodules , suggests that the expression of the gastrin ( CCK B ) receptor may be important in the transformation from premalignant nodules to pancreatic cancer . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Human brain CCK B receptors possessed slightly but significantly higher affinities for CCK 8 than for gastrin 1 , while both ligands bound equally to Mastomys enterochromaffin like cell derived gastrin receptors . ^^^ Both CCK 8 and gastrin 1 markedly augmented phosphoinositide hydrolysis and cytosolic free calcium levels in the CHO transfectants , indicating that the cloned CCK B receptor could functionally couple with intracellular signaling molecules . ^^^ The CCK B receptor mRNA was abundantly expressed in particular areas of the human brain and stomach , such as the cerebral cortex and mucosa of the gastric fundus . ^^^ This is the first demonstration of trophic effects of CCK and gastrin through the normal human brain CCK B receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , the selective CCK B agonist [ ( 2R , 3S ) beta MePhe 28 , N MeNle 31 ] CCK 26 33 had no effect . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ These results suggest that CCK may play a predominant role during the early postnatal development , while gastrin and CCK B receptors can function progressively to regulate proliferation and exocrine secretion in the calf pancreas , especially from the weaning period . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Association of the peptidase inhibitor RB 101 and a CCK B antagonist strongly enhances antinociceptive responses . ^^^ This has been definitely demonstrated in this study by co administration of the CCK B selective antagonist L 365 , 260 with RB 101 , a systemically active inhibitor of peptidases , which fully protects the endogenous opioids , the enkephalins , from their inactivation . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin peptidomimetics as selective CCK B antagonists : design , synthesis , and in vitro and in vivo biochemical properties . ^^^ Antagonists of cholecystokinin B ( CCK B ) receptors have been shown to alleviate CCK 4 induced panic attacks in humans and to potentiate opioid effects in animals . ^^^ In order to improve this property , new , peptoid derived CCK B antagonists , endowed with high affinity , selectivity , and increased lipophilicity have been developed . ^^^ Most of these compounds proved to be selective for the CCK B receptor , the most potent analog , N [ N [ ( 2 adamantyloxy ) carbonyl ] D alpha methyltryptophanyl ] N [ 2 ( 4 chlorophenyl ) ethyl ] glycine ( 26A ) , having a Ki value of 6 . 1 nM for guinea pig cortex membranes in vitro and a good selectivity ratio ( Ki CCK A / Ki CCK B = 174 ) . ^^^ Furthermore , the in vivo affinity of 26A for mouse brain CCK B receptors , following intracerebroventricular injection at different concentrations , was found to be 10 nmol . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In the present study , three structural analogs of LY 262691 with high selectivity for CCK B receptors , LY 262684 , LY 191009 and LY 242040 , also decreased the number of spontaneously active A 10 DA cells . ^^^ L 365 , 260 , a benzodiazepine CCK B antagonist , also decreased 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 . ^^^ CCK B antagonists may therefore represent a novel class of antipsychotic drugs . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ The potent CCK B selective agonist , A 63387 , at doses up to 100 nmol / kg did not increase serum OT . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Clearly , the receptor responsible for activation of the ECL cells distinguishes poorly between gastrin 17 and CCK 8s , which is in line with the characteristics of the CCK B receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ These data suggest that in the substantia nigra there may be a tonic level of CCK release that , through actions on CCK B receptors , may modulate DA agonist induced inhibition of DA neuronal activity . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Increased release of immunoreactive CCK 8 by electroacupuncture and enhancement of electroacupuncture analgesia by CCK B antagonist in rat spinal cord . ^^^ Intrathecal ( i . t . ) administration of CCK B antagonist L 365 , 260 per se did not affect tail flick latency ( TFL ) to any significant extent , yet it potentiated EA induced analgesia in a dose and frequency dependent manner . ^^^ The results suggest that an increased release of CCK 8 following EA may limit the effect of opioid peptides , and that the CCK B receptor mediates the anti opioid effect of CCK 8 in rat spinal cord . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Administration of both CCK A and CCK B receptor antagonists alone resulted in no change in meal size . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ It would be expected that YM 022 , a potent and selective gastrin CCK B receptor antagonist , inhibits gastric acid secretion without inducing gastrin mediated side effects such as hypergastrinemia and hyperplasia of oxyntic mucosa . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| METHODS : The effect of a new , potent and selective CCK B receptor antagonist , CI 988 on the growth of LoVo , a human colon cancer cell line both in vitro and in vivo was instigated . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B agonists stimulated calcium mobilization in a dose dependent manner in T cells . ^^^ CCK B antagonists suppressed CCK 4 induced calcium mobilization more potently than CCK A antagonist . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ This effect of a CCK B receptor antagonist was not mediated by the spinal opioid receptor activation . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Using site directed mutagenesis in this segment of the CCKBR , we identified a sequence of 5 amino acids in the second extracellular loop responsible for this 100 fold selective loss in gastrin affinity . 125I labeled Bolton Hunter CCK 8 binding displacement by L 365 , 260 ( a CCKBR selective antagonist ) was unaffected by the changes in these 5 amino acids . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We utilized intravenous infusions of pentagastrin , a selective CCK B receptor agonist , and studied behavioral and cardiovascular responses in 10 patients with panic disorder and 10 normal controls . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Recently , we have demonstrated that the human brain CCK B receptors are identical to the gastrin receptors derived from the stomach mucosa , and that the brain gut peptides , CCK 8 and gastrin 1 are mitogenic for mouse NIH 3T3 fibroblasts expressing human CCK B / gastrin receptors ( N hCCKBR ) . ^^^ In this report , we evaluated the antiproliferative potency of CCK B / gastrin receptor antagonists by using N hCCKBR cells . ^^^ Interestingly , a potent antagonist for rat CCK B / gastrin receptors did not have such activities in N hCCKBR cells . ^^^ These results suggest that YM 022 could intervene in the autocrine stimulation of human tumor cell lines through CCK B / gastrin receptors . ^^^ N hCCKBR cells are an excellent tool to screen for novel human CCK B / gastrin receptor antagonists possessing antiproliferative activity for human cancer cells . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ CCK B receptor mRNA was detected by Northern blot analysis in the brain and the fundus mucosa but not in the rest of the digestive tract and not in the pancreas , pancreatic islets , or kidney . ^^^ By RT PCR , expression of CCK B receptor mRNA could also be detected in antrum mucosa . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| No changes in measures of anxiety , hunger , or short term memory were observed at doses of L 365 , 260 shown to have antagonist activity at the CCK B receptor . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In morphine tolerant rats , addition of the CCK B receptors antagonist CI 988 or the NMDA receptor blocker dextromethorphan enhanced the antinociceptive effect of morphine on the hot plate test . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| A hallmark of the mammalian brain cholecystokinin ( CCK ) receptor , CCK B / gastrin ( CCK BR ) , is its high affinity for two structurally related peptides , CCK and gastrin . ^^^ CCK XLR shares approximately 50 % homology at the amino acid level with both the human CCK BR and the peripheral CCK A receptor subtypes . ^^^ We used CCK XLR to map the human CCK BR domains that confer high affinity for gastrin . ^^^ A series of chimeric CCK BR / CCK XLR constructs was generated and pharmacologically characterized . ^^^ While maintaining wild type affinity for sulfated cholecystokinin octapeptide , receptors with increasing amino terminal contributions from CCK BR demonstrated a stepwise increase in gastrin affinity . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Structure activity relationship studies of this series suggested that a number of analogues retained good in vitro potency for gastrin / CCK B receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Role of N and C terminal substituents on the CCK B agonist antagonist pharmacological profile of Boc Trp Phg Asp Nal NH 2 derivatives . ^^^ Among the CCK derivatives , the tetrapeptide Boc Trp Phg Asp Nal NH 2 ( 1 ) behaves as a short potent CCK B agonist which led to the development of an efficient peptidase resistant CCK B antagonist by bismethylation of its terminal CONH 2 group . ^^^ Introduction of more bulky substituents than NalNH 2 on the C terminal part decreased the CCK B receptor binding affinity . ^^^ In the newly synthesized compounds , 13 : 2Adoc D alpha MeTrp Phg Asp NalN ( CH 3 ) 2 and 16 : 2Adoc D alpha MeTrp Phg Asp NalNH 2 had the best CCK B receptor affinities ( KI = 3 . 5 and 3 . 4 nM , respectively ) and were selected for further biological evaluation . ^^^ Interestingly , when tested for their capacity to influence inositol phosphate formation , induced by CCK 8 in CHO cells transfected with the rat CCK B receptor , compound 13 behaved as a full CCK B antagonist with an IC 50 value of 18 + / 1 nM , being as potent as the antagonist L 365 , 260 and PD 134 , 308 ( IC 50 values respectively , 39 + / 17 and 30 + / 2 nM ) , whereas compound 16 was found to behave as a partial CCK B agonist . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Highly specific , CCK B receptor antagonists have reached clinical trials and have potential clinical utility as anxiolytics , antipsychotics , anti anorexics , or analgesics . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Pig pancreatic acinar cells possess predominantly the CCK B receptor subtype . ^^^ RNA were extracted for CCK A and CCK B receptor expression using specific cRNA probes . ^^^ The pig pancreas expresses few CCK A mRNA receptors but a majority of CCK B . ^^^ These data demonstrate that the pig pancreas expresses a majority of CCK B receptors . ^^^ In conclusion , the pig pancreas possesses a large majority of CCK B receptors responsible for their low sensitivity to CCK . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| To gain a better understanding of the role of cholecystokinin ( CCK ) B receptor in the maintenance of thermal hyperalgesia induced by unilateral constriction injury to the sciatic nerve in the rat , this study evaluated the effects of intrathecally administered YM 022 ( a CCK B receptor antagonist ) on thermal hyperalgesia . ^^^ These data indicate that a CCK B receptor antagonist attenuates the level of thermal hyperalgesia and this effect of a CCK B receptor antagonist is time dependent . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ Expression of the CCK B receptor gene was detected in both strains by RT PCR . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The use of topographical constraints in receptor mapping : investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp Tyr D Phe Gly Trp ( N Me ) Nle Asp Phe NH 2 ( SNF 9007 ) , a cholecystokinin ( 26 33 ) analogue that binds to both CCK B and delta opioid receptors . ^^^ The cholecystokinin ( 26 33 ) [ CCK ( 26 33 ) ] octapeptide analog Asp Tyr D Phe Gly Trp ( N Me ) Nle Asp Phe NH 2 ( SNF 9007 ) is a potent and selective ligand for both the CCK B and delta opioid receptors . ^^^ Pharmacological studies of SNF 9007 suggest a relationship between the ligand requirements of CCK B and delta opioid receptors , which further implies a possible structural relationship between these receptors . ^^^ We have utilized topographical constrainment of the important Trp 30 residue to investigate structural features of SNF 9007 that would distinguish between binding requirements in this region for the CCK B and delta opioid receptors . ^^^ Receptor binding results suggest that the preferred topography of the Trp 30 residue for CCK B receptor binding may be the 2S , 3S ( erythro L ) configuration whereas for the delta opioid receptor it may be the 2S , 3R ( threo L ) configuration . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 B receptor mRNA expression was detectable in only 1 / 14 ( 7 % ) samples of gastric cancer , although it was detectable in 10 / 12 ( 83 % ) body mucosa of the stomach . ^^^ These findings may suggest a greater role for CCK and CCK A receptor than for gastrin and CCK B receptor in gastric cancers . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| It has recently been demonstrated that L 365 , 260 , a CCK B antagonist in mammals , causes an increase in food intake in chickens . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Northern blot analysis revealed a significant expression of CCK B receptor mRNA in GH 3 cells , but not in normal rat pituitary glands . ^^^ These findings provided the first evidence for an autocrine / paracrine role of CCK and gastrin on stimulation of GH 3 cell growth through the CCK B receptor . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| CCK release from the synaptosomes , and levels of CCK and CCK B receptor mRNAs were the same as those observed in normal rats . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The influence of guanyl nucleotide on agonist and antagonist affinity at guinea pig CCK B / gastrin receptors : binding studies using [ 3H ] PD 140376 . ^^^ These data are consistent with the notion that the receptor sites in brain and gastric glands , which recognise CCK and gastrin related compounds , are the same and of the CCK B / gastrin subtype . ^^^ These findings may explain previously reported differences between gastrin and CCK B receptors that were based upon binding studies using agonist ligands . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK B receptor gene . ^^^ A stable Chinese hamster ovary cell line expressing the human CCK B receptor gene is described ( hCCK B . ^^^ In radioligand binding experiments employing membranes derived from these cells the rank order of affinity estimated for a series of CCK receptor ligands ( CCK 8S > CI 988 > PD 135158 > pentagastrin > CCK 8NS > L 365 , 260 > CCK 4 > LY 288513 > devazepide > A 71378 > lorglumide ) was found to be in excellent agreement with CCK B receptor pharmacology described in guinea pig cortex . ^^^ The CCK B receptor selective agonist CCK 4 stimulated the mobilization of intracellular Ca2+ with an estimated pEC 50 value of 7 . 4 . ^^^ Consistent with CCK B receptor pharmacology , the rank order of potency for antagonism of this response was observed to be PD 135158 > CI 988 > L 365 , 260 > > devazepide > lorglumide . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The in vivo release of the selective CCK B agonist pBC 264 ( associated with a tracer dose of [ 3H ] pBC 264 ) from microspheres prepared with OVA was very fast ( 92 % after 6 h ) , whereas only 26 % ( 88 pmol ) of pBC 264 was released from the formulation with Pluronic F 68 after 24 h . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Association of enkephalin catabolism inhibitors and CCK B antagonists : a potential use in the management of pain and opioid addiction . ^^^ 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 . ^^^ Recently the existence of regulatory mechanisms between both systems have been proposed , and the physiological antagonism between CCK and endogenous opioid systems has been definitely demonstrated by coadministration of CCK B selective antagonists with RB 101 , a systemically active inhibitor , which fully protects enkephalins from their degradation . ^^^ This article will review the experimental pharmacology of association of enkephalin degrading enzyme inhibitors and CCK B antagonists to demonstrate the interest of these molecules in the management of both pain and opioid addiction . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| These results suggest that the disruption of the MMC mediated by CCK is due to stimulation of peripheral CCK B receptors located in vagal afferent fibers . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Upregulation of ECL function is determined by activation of CCK B receptors , by gastrin , and by activation of beta adrenergic receptors , as well as by acetylcholine in some ( 10 29 % ) of the cells . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) A and CCK B receptors are highly homologous members of the seven transmembrane domain G protein coupled receptor superfamily . ^^^ 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 . ^^^ The resultant receptor maintained high affinity binding to both CCK and gastrin and dose dependent calcium responses similar to wild type CCK BR . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ RESULTS : High concentrations of CCK B gastrin receptors were detected in the midglandular region of the human 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Porta caval shunting enhances the trophic effects of cholecystokinin ( CCK ) A receptor activation on the pancreas and of CCK B receptor activation on the ECL cells in the oxyntic mucosa of the rat . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptors , present in control pancreata , were not detected in any of the pancreatic cancers . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) A and CCK B / gastrin receptors in human tumors . ^^^ Cholecystokinin ( CCK ) A and CCK B / gastrin receptors were evaluated with in vitro receptor autoradiography in 406 human tumors of various origins using a sulfated 125I labeled CCK decapeptide analogue 125I ( D Tyr Gly , Nle 28 , 3l ) CCK 26 33 and 125I labeled Leu 15 gastrin as radioligands . ^^^ CCK B / gastrin receptors were found frequently in medullary thyroid carcinomas ( 92 % ) , in small cell lung cancers ( 57 % ) , in astrocytomas ( 65 % ) , and in stromal ovarian cancers ( 100 % ) . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The novel atypical antipsychotic olanzapine , but not the CCK B antagonist LY 288513 , blocks apomorphine induced disruption of pre pulse inhibition . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We compared the changes in pancreatic regeneration in terms of wet weight and protein and DNA contents after partial pancreatectomy ( 30 % resection ) in OLETF and control ( Long Evans Tokushima Otsuka : LETO ) rats and examined whether the CCK B receptor has a role in pancreatic regeneration after pancreatectomy . ^^^ CCK B receptor gene expression was not enhanced after pancreatectomy . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Role of gastrin / CCK B receptors in meal stimulated acid secretion in rats . ^^^ Basal and stimulated acid outputs and portal venous plasma gastrin , histamine , and somatostatin concentrations were measured before and after close arterial injection of a new , relatively selective , gastrin / CCK B receptor antagonist GR143330X . ^^^ Furthermore , we show for the first time in an intact , in vivo , anesthetized rat model that meal stimulated activation of gastrin / CCK B receptors stimulates acid secretion in part by regulating the release of histamine and somatostatin . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Selective activation of CCK B receptors does not induce sleep and does not affect EEG slow wave activity and brain temperature in rats . ^^^ 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 . ^^^ In the present experiments , we studied the effects of the selective activation of CCK B receptors by CCK tetrapeptide ( CCK 4 ) or nonsulfated CCK 8 ( CCK 8 NS ) on sleep and brain temperature ( Tbr ) . ^^^ These results suggest that the activation of CCK B receptors by systemic injection of CCK 4 or CCK 8 NS is not sufficient to elicit increased NREMS and hypothermia in rats . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK induced depolarization was significantly reduced by a CCK A , but not a CCK B , receptor antagonist . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Expression of CCK B receptors was detected in all tissues arising from pancreas and in most extrapancreatic tissues and tumors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ The CCK B receptor agonist also induced mainly increases in the neuronal firing . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The results confirmed and extended previous behavioural data indicating that blockade of CCK B receptors potentiated antinociception elicited by endogenous opioids protected from enzymatic degradation . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Subcutaneous injection of the CCK agonist caerulein dose dependently decreased food intake in Zucker obese and lean rats whereas the CCK B agonist gastrin 17 did not . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ In vivo , however , infusions of CCK A mRNA antisense ODN did not alter CCK B receptor binding levels . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptors in the limbic system modulate the antidepressant like effects induced by endogenous enkephalins . ^^^ Systemic administration of RB 101 , a complete inhibitor of enkephalin catabolism , has been reported to induce antidepressant like responses in mice which were potentiated by an ineffective dose of a CCK B antagonist . ^^^ The aim of this study was to investigate the neuroanatomical substrate involved in the facilitatory effects induced by CCK B antagonists on RB 101 behavioural responses . ^^^ Thus , the CCK B antagonist PD 134 , 308 was locally administered into different brain structures ( anterior nucleus accumbens , central amygdala and caudate nucleus ) and its effects on the antidepressant like response induced by systemic administration of RB 101 were evaluated in the conditioned suppression of motility ( CSM ) test in rats . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| However , when rats were pretreated with antigastrin serum or CCK B receptor antagonist , the acid secretion by TE was virtually abolished . ^^^ CONCLUSIONS : NGASP stimulates histamine release from ECL cells , but the release is not mediated via CCK B / gastrin receptor . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In an alternative approach , stably transfected CHO cells bearing either CCK A or CCK B receptors were stimulated with CCK 8 . ^^^ Each receptor induced a time dependent increase in activity of both MAPKs by five to sixfold in CCK A and CCK B bearing cells . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK B agonist , BC 264 , increases dopamine in the nucleus accumbens and facilitates motivation and attention after intraperitoneal injection in rats . ^^^ With this aim , we have investigated the biochemical and pharmacological effects resulting from the administration of BC 264 , a highly potent and selective CCK B agonist able to cross the blood brain barrier . ^^^ 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 . ^^^ These results show that activation of CCK B receptors by BC 264 does not produce anxiogenic like effects but appears to improve motivation and attention , whereas other CCK B agonists such as BocCCK 4 induce anxiogenic responses . ^^^ Several explanations , including the existence of different sub sites of the CCK B receptor , could account for these differential effects . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptors produce similar signals but have opposite growth effects in CHO and Swiss 3T3 cells . ^^^ Rat cholecystokinin B ( CCK B ) receptors were transfected into Chinese hamster ovary ( CHO ) K 1 ( CHO CCK B ) and Swiss 3T3 ( Swiss 3T3 CCK B ) cells , and the effects of receptor activation on cell proliferation and intracellular signaling were investigated . ^^^ CCK octapeptide ( CCK 8 ) treatment had no effect on cell growth in quiescent CHO CCK B cells but inhibited DNA synthesis , proliferation , and colony formation when the cells were grown in fetal bovine serum ( FBS ) . ^^^ In contrast , CCK 8 stimulated DNA synthesis in quiescent Swiss 3T3 CCK B cells and had no effect when the cells were grown in FBS . ^^^ In summary , receptor activation had opposite effects on growth parameters in CHO and Swiss 3T3 cells , but only minor differences were observed in the characteristics of CCK B receptor coupling to specific second messengers in the two cell types . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ These results suggest that CCK B receptor is involved in the behavior of TN gene knockout mouse through striatal DA transmission . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Furthermore , antagonists of CCK B receptors , which are found most frequently in the brain , inhibit the activity of brain dopamine neurons . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| All the compounds were evaluated in vitro towards both CCK B and CCK A receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ The results suggest that ' anxious ' behavior induced by CCK is associated with selective CCK B receptor stimulation . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The aim of this study was to evaluate whether radiolabelled gastrin may be suitable for targeting CCK B receptor expressing tumours in vivo . ^^^ Physiological CCK B receptors in the stomach , gallbladder and pancreas of the mice were targeted as well . ^^^ Future preclinical and clinical studies will address in more detail the molecular features that render CCK B receptor binding agents potentially useful candidates for in vivo scintigraphy and radionuclide therapy . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The effect of CI 988 , a CCK B receptor antagonist , on the facilitation of the flexor reflex induced by conditioning stimulation ( CS ) of C afferents was also examined . ^^^ Furthermore , it is suggested that CCK may not play a significant role in the phenomenon of wind up and central sensitization after repetitive C fiber input under normal conditions or after axotomy , when expression of CCK and CCK B receptors are increased in sensory neurons . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Unsulfated DTPA and DOTA CCK analogs as specific high affinity ligands for CCK B receptor expressing human and rat tissues in vitro and in vivo . ^^^ Recently , the CCK B receptor , which binds both gastrin and cholecystokinin with high affinity , was shown using in vitro methods to be overexpressed in a number of human tumor tissues , including medullary thyroid carcinomas , small cell lung cancers , astrocytomas , gastrointestinal tumors , and stromal ovarian cancers . ^^^ In the present study , we have designed novel , unsulfated CCK octapeptide analogs linked to the metal chelating DTPA and DOTA , and have tested them for their binding affinity to CCK B receptor positive tissue from human tumors : The most potent compounds assayed were DTPA [ Nle 28 , 31 ] CCK ( 26 33 ) ( MP 2286 ) and DTPA [ d Asp 26 , Nle 28 , 31 ] CCK ( 26 33 ) ( MP 2288 ) with an IC 50 of 1 . 5 nM . ^^^ 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 ) . ^^^ The CCK B receptor expressing gastric mucosa showed specific in vivo accumulation of 111In labeled MP 2288 which could be blocked in the presence of excess unlabeled MP 2288 . 111In labeled MP 2286 and MP 2288 were also found to be stable in human plasma whereas both compounds were degraded in urine ( > 40 % after 3 h at 37 degrees C ) . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK B antagonists L 365 , 260 and PD 134 , 308 decreased and completely blocked ( respectively ) the place aversion induced by naloxone in morphine dependent animals whereas BC 264 and devazepide were inactive in this model . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Furthermore , infusion of the CCK B receptor antagonist L 365 , 260 significantly blocked the increase of RMCP 2 concentration after OVH . ^^^ Our results indicate that mucosal mast cells are degranulated by endogenous CCK release through stimulation of CCK B receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Blockade of gastric acid secretion by YM 022 ( CCK B receptor antagonist ) or famotidine ( histamine 2 receptor antagonist ) resulted in a significant suppression of casein stimulated pancreatic exocrine secretion as determined by juice volume and amylase secretion . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| An increased expression of cholecystokinin ( CCK ) messenger RNA ( mRNA ) as well as CCK B receptor mRNA in dorsal root ganglion ( DRG ) cells following peripheral axotomy has previously been demonstrated . ^^^ We also compared the effects of the CCK B receptor antagonist CI 988 on basal and potassium stimulated CCK LI release in intact animals and in chronically axotomized rats . ^^^ The present data suggest that axotomy reduces the release of CCK like immunoreactivity in the spinal cord by a mechanism involving the CCK B receptor binding site . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Biodistribution studies in mice showed very low brain uptakes ( < 0 . 8 % dose / gram ) of the radioactivities after intravenous injections of these compounds , although that of brain CCK B receptor selective [ 11C ] L 365 , 260 was 2 fold that of [ 11C ] L 365 , 346 . ^^^ Owing to the very low brain permeability , however , [ 11C ] L 365 , 260 may have no potential as a PET tracer for probing brain CCK B receptors . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Microinjections of the selective CCK B receptor antagonist , LY 288513 ( 1 . 05 , 4 . 2 , 17 . 0 nmol / 0 . 25 microliter ) , into the PAG suppressed the hissing response in a dose and time dependent manner . ^^^ Microinjections of the CCK B agonist , pentagastrin , ( 0 . 5 and 1 . 0 nmol / 0 . 25 microliter ) facilitated the occurrence of defensive rage behavior . ^^^ In contrast , microinjections of the CCK B antagonist , LY 288513 ( 4 . 2 , 17 . 0 nmol / 0 . 25 microliter ) , facilitated the occurrence of predatory attack behavior elicited from the lateral hypothalamus . ^^^ This finding demonstrates the specificity of the effects of CCK B receptor blockade upon hissing . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Displacement experiments using [ 125I ] BH CCK and various agonists and antagonists identified binding sites with typical CCKBR pharmacology . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Neither its CCK B receptor antagonistic moiety of Compound 1 ( Compound 2 ) nor its histamine H 2 receptor antagonistic moiety of Compound 1 ( Compound 3 ) had any effect on [ 125I ] PYY binding , suggesting that the entire structure of Compound 1 is essential for Y 1 receptor blocking activity . ^^^ It showed no significant activity ( IC 50 > 1 microM ) in 30 receptor binding assays and 5 enzyme assays , with the exception of CCK B and histamine H 2 receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ CCK 8 stimulated total inositol phosphate accumulation in COS 1 cells transiently expressing the CCKBR H207F with full efficacy and a 3044 fold reduced potency , which suggests that the loss of radioligand binding was caused by a loss in affinity . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ The structurally related benzodiazepines L 365 , 260 , L 740 , 093 , and YM 022 are selective antagonists of the CCK B receptor subtype . ^^^ Their in vitro pharmacological profiles have been characterized using the human CCK B receptor expressed in CHO cells . 5 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| These effects were reversed by PD 135 , 158 , a selective CCK B receptor antagonist ( 0 . 1 mg / kg , s . c . ) , administered 5 min prior to ceruletide . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We have reported previously that the transmembrane domains of the cholecystokinin B / gastrin receptor ( CCK BR ) comprise a putative ligand binding pocket . ^^^ In the present study , we examined whether amino acid substitutions within the CCK BR pocket altered the affinities and / or functional activities of L 365 , 260 ( the prototypical nonpeptide CCK BR antagonist ) and two structural derivatives , YM 022 ( a higher affinity antagonist ) and L 740 , 093S ( a partial agonist ) . ^^^ Eight amino acids that project into the CCK BR pocket were individually replaced by alanine , using site directed mutagenesis . ^^^ For each of the nonpeptide ligands examined , a distinct series of mutations altered the affinity , suggesting that each ligand possessed a characteristic pattern of interactions within the CCK BR pocket . ^^^ Basal signaling levels and inositol phosphate formation induced by the full agonist CCK octapeptide were comparable for the wild type receptor and all of the mutant CCK BR forms . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Furthermore , several selective CCK B agonists produce anxiogenic like effects , while CCK B antagonists induce anxiolytic like responses in several models of anxiety . ^^^ However , BC 264 a highly selective CCK B agonist , does not produce anxiogenic like effects but increases attention and / or memory . ^^^ Together with biochemical data , this led to the hypothesis of the existence of two CCK B binding sites , CCK B 1 and CCK B 2 , which could correspond to different activation states of a single molecular entity . ^^^ Investigations into CCK B 1 and CCK B 2 systems might be of critical interest , since only one site , CCK B 1 , appears to be responsible for the effects of anxiety . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Moreover , the affinity of the different compounds towards the cholecystokinin CCK A and CCK B receptors was evaluated . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , mouse NIH3T3 fibroblasts transfected with human CCK B receptor ( NIH3T3CCK BR ) showed increased proliferation and phosphorylation to the peptides . ^^^ Also , radioligand binding studies indicated that Mia PaCa 2 cells had approximately 12 . 5 fold less CCK B receptors than NIH3T3CCK BR . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| However , sciatic nerve section was associated with a marked ipsilateral increase in both CCK B receptor mRNA levels in these ganglia ( +70 % ) and the autoradiographic labeling of CCK B receptors by [ 3H ] pBC 264 ( +160 % ) in the superficial layers of the lumbar dorsal horn . ^^^ Up regulation of CCK B receptors rather than CCK synthesis and release probably contributes to increased spinal CCKergic neurotransmission in neuropathic pain . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor mRNA was expressed in the pancreas , but not in gallbladder and duodenum . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Furthermore , CI 988 , an antagonist of the CCK B receptor , chronically coadministered with morphine , reduces autotomy , a behavior that may be a sign of neuropathic pain following peripheral nerve section . ^^^ Similarly , in the chronic phase of the spinal ischemic model of central pain , the allodynia like symptom is not relieved by systemic morphine , but is significantly reversed by the CCK B antagonist . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Expression of the CCK B receptor gene was observed in the stomach , pancreas , and brain in both OLETF and LETO rats by the RT PCR method , with expression of the CCK B receptor gene markedly enhanced in OLETF rats compared with that in LETO rats . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| To understand molecular basis of Gs coupling to cholecystokinin ( CCK ) A and CCK B receptor subtypes , we examined cAMP responses in three sets of human CCK receptor mutants expressed in human embryonic kidney ( HEK ) 293 cells . ^^^ 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 . ^^^ Ser 82 was further changed into Asp , Thr , or Ala to determine the specificity of this position in Gs coupling by the CCK BR . ^^^ Finally , CCK AR reverse mutants were studied to compare them with their corresponding CCK BR mutants that showed increased cAMP responses . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin B ( CCK B ) receptor antagonists improve `` aged ' ' sleep : a new class of sleep modulators . ^^^ GV 150013 , a selective CCK B receptor antagonist , was found to increase REM sleep , as well as non REM sleep , and therefore total sleep ( non REM + REM ) mainly in aged rats . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Dai , Novel gastrin receptors mediate mitogenic effects of gastrin and processing intermediates of gastrin on Swiss 3T3 fibroblasts : Absence of detectable cholecystokinin ( CCK ) A and CCK B receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor : chemistry , molecular biology , biochemistry and pharmacology . ^^^ CCK 8 interacts with nanomolar affinities with two different receptors designated CCK A and CCK B . ^^^ The physiological and pathological implication of CCK B receptor will be confirmed in CCK B receptor deficient mice obtained by gene targeting ( Nagata el al . , 1996 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK receptors have been classified into two subtypes : CCK A and CCK B . ^^^ A single nucleotide polymorphism has been found in the coding region of the CCK B receptor gene ( CCK BR ) and D Collier ( personal communication ) identified a highly polymorphic dinucleotide ( CT ) n microsatellite in the 5 ' regulatory region . ^^^ For the CCK B receptor gene polymorphism , PD patients showed a significant association . ^^^ Our genetic dissection of the CCK system thus far suggests that the CCK B receptor gene variation may contribute to the neurobiology of panic disorder . . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Excitatory responses to CCK 8 are due to stimulation of preganglionic receptors while inhibitory responses are NO mediated through stimulation of postganglionic CCK B receptors . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The involvement in memory processes of the neuropeptide cholecystokinin ( CCK ) through its interaction with the CCK B receptors was studied . ^^^ The improving effect of a selective CCK B agonist , BC 264 , intraperitoneally administered ( 0 . 3 microgram / kg ) in the retrieval phase of the task ( 6 hr time interval ) , was also observed after its injection ( 1 pmol / 0 . 5 microliter ) in the dorsal subiculum / CA1 of the hippocampus but not in the caudate / putamen nucleus or in the prefrontal cortex of rats . ^^^ The CCK B antagonist L 365 , 260 injected ( 10 ng / 0 . 5 microliter ) into this region of the hippocampus abolished the improving effect of BC 264 injected intraperitoneally . ^^^ Finally , CCK B receptor deficient mice have an impairment of performance in the memory task ( 2 hr time interval ) . ^^^ Together , these results support the physiological involvement of the CCKergic system through its interaction with CCK B receptors in the hippocampus to improve performance of rodents in the spatial recognition memory test . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Also , CCK B receptors have been found in some human pancreatic cancers . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ RT PCR / Southern blot analysis also showed CCK A and CCK B receptor mRNA expression in fetal and infant pancreas . ^^^ These results show that the both CCK receptor types are expressed in human pancreas at stages of early gestation , but there is predominant expression of CCK B receptor in adult pancreas . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Disruption of cholecystokinin ( CCK ) B receptor gene did not modify bile or pancreatic secretion or pancreatic growth : a study in CCK B receptor gene knockout mice . ^^^ Pancreatic exocrine function and bile secretion were examined in cholecystokinin ( CCK ) B receptor gene targeted mice and compared among different genotypes [ i . e . , CCK B receptor gene : ( + / + ) , wild type ; ( + / ) , heterozygous ; and ( / ) , homozygous deficient ] . ^^^ These results indicated that the CCK B receptor has no role in pancreatic growth , exocrine secretion , or bile secretion in adult mice . . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The aim of this study was to systematically screen and optimize , in a preclinical model and a pilot clinical study , suitable radioligands for targeting CCK B receptors in vivo . ^^^ In accordance with their comparably low affinity , nonsulfated members of the CCK family showed fairly low uptake in the tumor and other CCK B receptor expressing tissues . ^^^ This effect was probably due to their similar affinity for both CCK A and CCK B receptors . ^^^ Best tumor uptake and tumor to nontumor ratios were obtained with members of the gastrin family because of their selectivity and affinity for the CCK B receptor subtype . ^^^ In a pilot clinical study , radioiodinated and 111In labeled derivatives showed excellent targeting of physiological CCK B receptor expressing organs , as well as all known tumor sites . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ 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 . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| BACKGROUND & AIMS : Two distinct receptors , cholecystokinin ( CCK ) A and CCK B , mediate CCK effects in the digestive system . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In a pilot study , we have demonstrated the feasibility of radiolabeled gastrin 1 to target CCK B receptor expressing tissues in vivo in animals and patients ( T . ^^^ The aim of the present study was to systematically optimize , in a preclinical model , suitable radioligands for targeting CCK B receptors in vivo . ^^^ In accordance to their comparably low affinity , nonsulfated members of the CCK family showed fairly low uptake in the tumor and other CCK B receptor expressing tissues ( e . g . , the stomach ) . ^^^ Best tumor uptake and tumor : nontumor ratios were obtained with members of the gastrin family , probably because of their selectivity and affinity for the CCK B receptor subtype . ^^^ Pilot therapy experiments in MTC bearing animals showed significant antitumor efficacy as compared with untreated controls . ( 111 ) In Labeled diethylene triamine pentaacetate derivatives of minigastrin showed excellent targeting of CCK B receptor expressing tissues in animals and a normal human volunteer . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Indeed , 111In labeled DTPA derivatives of gastrin showed excellent targeting of CCK B receptor expressing tissues in animals and patients . ^^^ |
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| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Dose response of adrenocorticotropin and cortisol to the CCK B agonist pentagastrin . ^^^ To explore this hypothesis , we examined the effects of varying doses ( 0 to 0 . 8 microgram / kg ) of the CCK B agonist pentagastrin on adrenocorticotropin ( ACTH ) and cortisol release in healthy human subjects . ^^^ The HPA axis response to the CCK B agonist pentagastrin may be a direct pharmacological effect . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Placebo controlled trial of the CCK B antagonist , CI 988 , in panic disorder . ^^^ Selective antagonists of CCK B receptors can block the challenge induced symptoms in a dose dependent manner , leading to the hypothesis that these compounds may have anxiolytic effects . ^^^ METHODS : A randomized , double blind study was carried out to compare the effects of placebo with CI 988 , a selective antagonist of the CCK B receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK A receptor antagonist L 364 , 718 was 300 fold more potent than the CCK B receptor antagonist L 365 , 260 at inhibiting CCK 8 induced contraction . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The mutated receptor displayed similar expression levels and high affinity CCK binding compared with the wild type CCKBR . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Using reverse transcription polymerase chain reactions , CCK B receptor mRNA was expressed in all specimens of normal fetal and postnatal human pancreas , adult pancreas , and pancreatic adenocarcinomas . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Preclinical and initial clinical evaluation of 111In labeled nonsulfated CCK 8 analog : a peptide for CCK B receptor targeted scintigraphy and radionuclide therapy . ^^^ METHODS : The aim of this study was to evaluate in vitro and in vivo whether 111In labeled CCK B receptor specific CCK 8 analog [ D Asp 26 , Nle 28 , 31 ] CCK 26 33 ( D Asp Tyr Nle Gly Trp Nle Asp Phe NH 2 ) is suitable for CCK B receptor scintigraphy based on the finding that unlabeled nonsulfated diethylenetriamine pentaacidic acid [ DTPA 0 ] CCK 8 and tetraazacyclododecanetetraacetic acid [ DOTA 0 ] CCK 8 analogs show high and specific binding for CCK B receptors in human tumors . ^^^ RESULTS : In vitro , [ 111In DOTA 0 ] CCK 8 showed specific internalization in CCK B receptor positive rat pancreatic tumor cells AR42J . ^^^ From the data obtained with [ 111In DOTA 0 ] CCK 8 and ( 125I ) 1 gastrin , the latter being a specific ligand for the CCK B receptor , the rat pancreatic cell line CA 20948 also appeared to be CCK B receptor positive . ^^^ In vivo biodistribution experiments in CA 20948 tumor bearing Lewis rats showed rapid clearance of [ 111In DOTA 0 ] CCK 8 , and specific uptake was found in the CCK B receptor expressing stomach and tumor . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| RESULTS : The cell line LN 36 responded with increased cell number to stimulation by gastrin 17 and decreased cell number to inhibition by the CCK B receptor antagonist L 365 , 260 . ^^^ 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 P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| Structure and developmental expression of the mouse CCK B receptor gene . ^^^ Cholecystokinin ( CCK ) and gastrin exert their effects through two receptors , the CCK A and CCK B receptors . ^^^ We have cloned the mouse CCK B receptor gene ( Cckbr ) and determined its complete genomic structure , nucleotide sequence , and tissue specific expression pattern . ^^^ Prenatal expression of both CCK A and CCK B receptors in various tissues was analyzed by RT PCR . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ Gastrin / CCK B receptor mRNA was present in all carcinomas , resection margins , and normal pancreatic tissue . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 ) . ^^^ The CCK B receptor antagonist was not more effective at blocking . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| The present study demonstrated CCK , acting on CCK B receptors , participates in the development of the opiate dependence . ^^^ These findings suggest that CCK B receptor antagonists might be of some value in the treatment and prevention the relapse of opiate addicts . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| We injected the CCK B receptor antagonist PD 135 , 158 into the PVTh before restraint in control and chronically cold stressed rats . ^^^ In addition , CCK B receptor mRNA expression in the pPVTh was not altered by chronic cold stress . ^^^ Acting via CCK B receptors in pPVTh , CCK then constrains facilitated ACTH responses to novel stress in chronically stressed but not naive rats . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ The data suggest , that endogenous CCK in the paraventricular nucleus of the hypothalamus unfolds a stimulatory effect on colonic transit through action on CCK B receptors . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The serendipitously discovered panicogenic effect of the cholecystokinin fragment , the C terminal tetrapeptide amide ( CCK 4 ) , has suggested that the widespread network of CCK neurons and corresponding CCK B receptors in the brain are in some way involved in pathogenesis panic disorders in man . ^^^ This review focuses on three immediate questions . ( 1 ) Does endogenous CCK 4 exist . ( 2 ) Is the panicogenic effect mediated only through CCK B receptors . ( 3 ) Are measurements of CCK peptides in cerebrospinal fluid of use in elucidating the pathogenesis and / or diagnosis . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
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 P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| In all patients there was visualization of the CCK B receptor positive stomach . ^^^ In conclusion : ( 1 ) the CCK B receptor positive gastric mucosa and presumed MTC lesions could be visualized in patients using an octapeptide [ 111In DTPA ] CCK analogue that is probably internalized , proving the feasibility of CCK B receptor imaging in vivo ; ( 2 ) there was a relatively low uptake of the CCK analogue in the strongly CCK receptor positive stomach , and rapid degradation of the peptide in serum . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Pancreatic secretory response to feeding in the calf : CCK A receptors , but not CCK B / gastrin receptors are involved . ^^^ In bovine species , as in human , the pancreas predominantly expresses cholecystokinin B ( CCK B ) / gastrin receptors . ^^^ 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 participation of CCK B / gastrin receptors in this regulation was not demonstrated . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Since evidence points to the involvement of cholecystokinin ( CCK ) in nociception , we examined the effect of intrathecal CI 988 , an antagonist of the CCK B receptors , on mechanical hyperalgesia and allodynia in normal , mononeuropathic and diabetic rats , . ^^^ These results show the CCK B receptor blockade mediated antinociceptive effects and reveals the antinociceptive action of morphine in diabetic rats after CCKergic system inhibition . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Dose response of arginine vasopressin to the CCK B agonist pentagastrin . ^^^ To explore relationships between CCK B receptor activation , the HPA axis response , and AVP release , a dose response study using the CCK B receptor agonist pentagastrin was conducted . ^^^ AVP release appeared to increase with increasing doses of the CCK B agonist . ^^^ These findings suggest a possible role for the CCK B receptor in AVP release , which may be at least partially separate from its role in modulation of the HPA axis . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 P32239 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B receptor antagonist CI 988 ( 2 mg / kg , i . p . ) reduced the anxiety like behavior without affecting the increase in CCKLM outflow . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The results suggest that CCK 45C > T and CCKBR Val125Ile polymorphisms do not have a major role in alcohol dependence in the population studied . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We have previously shown in a rat model of central neuropathic pain after spinal cord injury that blockade of CCK B receptors lead to marked pain relief . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Indeed , 111In labeled DTPA derivatives of gastrin showed excellent targeting of CCK B receptor expressing tissues in animals and patients . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| Mitogenic effects of gastrin 1 on ductal complexes in vivo and of tetragastrin , pentagastrin , and gastrin 1 and 2 , with or without the CCK B receptor antagonist L 365 , 260 , on duct like cells in vitro were analyzed by 5 bromo 2 ' deoxyuridine labeling . ^^^ Immunocytochemistry , Western blotting , and reverse transcription polymerase chain reaction were applied for detection of the CCK B receptor . ^^^ Immunocytochemistry showed expression of CCK B receptors in these models and in fetal but not normal adult exocrine pancreas . ^^^ Additionally , up regulation of CCK B receptors during ductular metaplasia was shown by Western blotting and reverse transcription polymerase chain reaction . ^^^ CONCLUSIONS : Duct like pancreatic epithelial cells in vitro and ductal complexes in vivo express gastrin / CCK B receptors and proliferate in response to gastrin . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptors for instance have been identified in several types of neuroendocrine tumors . ^^^ One of the highest incidences of CCK B receptors has been reported in medullary thyroid cancers at the protein and at the mRNA level using in vitro receptor autoradiography and RT PCR . ^^^ As a proof of concept , it could be demonstrated that a majority of medullary thyroid cancer primary tumors and metastases are visualized in vivo with CCK B receptor scintigraphy using these radioligands . ^^^ More recently , radiotherapy of CCK B receptor expressing medullary thyroid cancers with radiolabeled minigastrin has been successfully reported in a small number of patients , giving support to the proposal that CCK B receptors overexpressed in tumors represent a useful target for clinical application . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| BACKGROUND & AIMS : Pancreatic acinar cells from various species express cholecystokinin ( CCK ) A , CCK B , or a combination of these CCK receptor subtypes . ^^^ 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 P32239 |
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 . ^^^ CCK B / gastrin receptor mRNA and protein were detected in parietal cells ( 57 . 4+ / 11 . 1 % ) and in neuroendocrine cells ( 33 . 2+ / 4 . 4 % ) expressing chromogranin A . ^^^ Furthermore , epithelial cells within the neck of the gastric gland were found to express the CCK B / gastrin receptor . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| In this study , we have investigated the CCK B receptor ( CCKBR ) gene , which is the main constituent of the CCK receptor in the CNS . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ QSAR studies verify that CCK B receptors are closely related structurally to gastrin receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The CCK receptors can be pharmacologically subdivided into two subtypes : CCK A and CCK B . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The aim of our work was to develop and systematically optimize suitable radioligands for targeting CCK B receptors in vivo and to investigate their role in the staging and therapy of MTC and other CCK B receptor expressing malignancies . ^^^ Best tumor uptake and tumor to nontumor ratios were obtained with members of the gastrin family , because of their superior selectivity and affinity for the CCK B receptor subtype . ^^^ Radiometal labeled derivates of minigastrin showed excellent targeting of CCK B receptor expressing tissues in animals and healthy human volunteers . ^^^ CCK B receptor scintigraphy was performed with ( 111 ) In diethylenetriamine pentaacetic acid d Glu ( 1 ) minigastrin . ^^^ The normal organ uptake was essentially confined to the stomach ( and , to a lesser extent , to the gallbladder and , in premenopausal women , to normal breast tissue ) as a result of CCK B receptor specific binding and to the kidneys , as excretory organs . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| However , the human pancreas has been reported to express mainly CCK B receptors . ^^^ Neither CCK A nor CCK B receptor mediates amylase release from human pancreatic acini in vitro . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| This effect is mediated by postsynaptic CCK B receptors and is attributable to potentiation of the A current . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| The substituents of the 1 , 4 benzodiazepine scaffold have been varied in the 3 , 5 , 7 , and 8 positions and the combinatorial library was evaluated in a chole cys to kinin ( CCK ) radioligand binding assay . 3 Alkylated 1 , 4 benzodiazepines with selectivity towards the CCK B ( CCK 2 ) receptor have been optimized on the lipophilic side chain , the ketone moiety , and the stereochemistry at the 3 position . ^^^ Various novel 3 alkylated compounds were synthesized and [ S ] 3 propyl 5 phenyl 1 , 4 benzodiazepin 2 one , [ S ] NV A , has shown a CCK B selective binding at about 180 nM . ^^^ |
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| Interacting proteins: P06307 and P32239 |
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 . ^^^ Energy metabolism and energy turnover were increased in mice with a disruption of the CCK BR gene , although the underlying mechanism is unknown . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ 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 . ^^^ We therefore conclude that a lack of CCK BR increases the anxiety related behavior of the mouse in the elevated plus maze . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Intravenous injection of the cholecystokinin ( CCK ) B receptor agonist , pentagastrin , produces robust , dose dependent release of adrenocorticotropin ( ACTH ) and cortisol , supporting the hypothesis that CCK B agonists pharmacologically activate the hypothalamic pituitary adrenal ( HPA ) axis . ^^^ These data support the hypothesis that CCK B receptor mediated activation of the HPA axis is relatively resistant to cortisol feedback inhibition . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| We hypothesized that circulating concentrations of endogenous CCK 4 and / or CCK 8 are increased in later life , possibly due to decreased enzymatic degradation , and that this is associated with desensitization of CCK B receptors . ^^^ The two groups were compared on fasting basal plasma concentrations of CCK 4 , sulfated CCK 8 ( CCK 8s ) and nonsulfated CCK 8 ( CCK 8 ns ) , and on binding capacity of lymphocyte CCK B receptors . ^^^ Compared with younger subjects , older subjects had a significantly higher basal plasma concentration of CCK 8s and significantly diminished binding capacity of CCK B receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ CCK B receptor antagonists might be of some value in the treatment and prevention of relapse to stress induced to drug craving following long term detoxification . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| A spliced variant of the CCK B receptor was identified which differed from the CCK B receptor by the presence of intron 4 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ In contrast , the level of CCK B receptor gene expression was upregulated to 157 % and 153 % , respectively . ^^^ These effects are most probably linked to the CCK B receptor in AR42J cells . ^^^ The phorbolester PMA ( 100 nM ) , a protein kinase C activator , downregulated CCK A receptor expression but did not affect CCK B receptor gene transcription . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Our recent work has focused on new methods to radiolabel the CCK 8 peptide with ( 111 ) In or ( 99m ) Tc for the purpose of developing radiopharmaceuticals for in vivo CCK B receptor imaging . ^^^ CCK BR positive and control cells were subcutaneously injected in opposite flanks of CD 1 female nude mice in order to obtain xenografts differing only in their ability to express CCK B receptors . ^^^ In particular , cholecystokinin ( CCK ) receptors of the subtype B ( CCK BR ) have been shown to be overexpressed in certain neuroendocrine tumors including medullary thyroid cancer . ^^^ The human epidermoid carcinoma cell line , A 431 , was transfected with a plasmid containing the full coding sequence of the human CCK BR under a strong viral promoter , obtaining a number of receptors in the range of 2 5 10 10 ( 6 ) per cell . ^^^ An animal tumor model utilizing these two cell lines was developed to evaluate the specificity of interaction with the CCK BR and biodistribution properties of the compounds . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin B ( CCK B ) / gastrin receptor targeting peptides for staging and therapy of medullary thyroid cancer and other CCK B receptor expressing malignancies . ^^^ The aim of our recent work was to develop and systematically optimize suitable radioligands for targeting CCK B receptors in vivo and to investigate their role in the staging and therapy of MTC and other CCK B receptor expressing malignancies . ^^^ Best tumor uptake and tumor to nontumor ratios were obtained with members of the gastrin family , due to their superior selectivity and affinity for the CCK B receptor subtype . ^^^ Radiometal labeled derivatives of minigastrin showed excellent targeting of CCK B receptor expressing tissues in animals and healthy human volunteers . ^^^ CCK B receptor scintigraphy was performed with ( 111 ) In DTPA D Glu ( 1 ) minigastrin . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CONCLUSIONS : Pancreatic enzyme secretion due to CCK 33 stimulation depends on the presence of short duodenal pancreatic peptidergic reflexes evoked mainly via low sensitive , probably CCK B , receptors located in the duodenum / stomach . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| Conversely , higher levels of stress can inhibit motivated behaviour , and evidence is presented that this may occur in part through the effects of the neuropeptide cholecystokinin ( CCK ) , acting through CCK B receptors in the nucleus accumbens . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Chronic anxiolytic treatment with the selective CCK B ( CCK ( 2 ) ) receptor antagonist , Ci 988 ( 0 . 3 mg / kg / day ip ) or diazepam ( 2 mg / kg / day ip ) , induced numerous effects throughout the central nervous system ( CNS ) , with Ci 988 inducing significant changes in the density of dopamine D ( 2 ) receptors , and diazepam producing marked changes in both dopamine D ( 2 ) and CCK B receptor binding density as well as preproCCK mRNA expression . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Blockade of CCK B receptors with intraperitoneal L 365 , 260 ( 25 mg / kg ) reversed bombesin induced gastroprotection . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
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 P32239 |
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 . ^^^ 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 P32239 |
Pubmed |
SVM Score :0.0 |
| BACKGROUND AND AIMS : Both cholecystokinin ( CCK ) A and CCK B receptors are expressed in the pancreas , and exogenous gastrin administration stimulates glucagon secretion from human islets . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Thus , bi daily antalarmin treatment ( 20 mg / kg ip ) induced a significant increase in CCK B receptor binding density throughout the neuraxis , indicative of either a global increase in receptor number or an increase in receptor affinity . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
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 . ^^^ To address this issue we investigated the effect of the prolonged ( 6 day ) administration of CCK , CCK R antagonists ( CCK RAs ) and pentagastrin ( PG ) , a CCK 2 R agonist , on adult rat HPA axis . ^^^ 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 . ^^^ Taken together , these findings allow us to draw the following main conclusions : 1 ) the prolonged exposure to elevated CCK concentrations down regulates CCK R expression in the pituitary gland , which accounts for the lack of effect of CCK on ACTH secretion ; 2 ) adrenal CCK 1 Rs and CCK 2 Rs inhibit and stimulate , respectively , corticosteroid secretion ; and 3 ) endogenous CCK system plays a minor role in the physiological regulation of rat HPA axis , its main effect being the CCK 2 R mediated maintenance of adrenocortical cell number . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Genomic DNA was analyzed for CCK , CCKAR , and CCKBR ( cholecystokinin B receptor ) polymorphisms by polymerase chain reaction . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| We therefore determined the allele and genotype frequencies of a single nucleotide polymorphism in the CCK gene ( 36C > T ) and one CT repeat polymorphism in the CCK B receptor gene in a German panic disorder sample ( n = 115 for CCK gene polymorphism , n = 111 for CCK B receptor polymorphism ) and compared them with gender and age matched controls . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| Central microinjection of CCK in rats induces a thermogenic response that can be attenuated by CCK B receptor antagonists , but some authors observed a hypothermia . ^^^ 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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Two distinct activity labels can have a significant similarity for a number of reasons : two activities can be nearly synonymous ( e . g . , CCK B antagonist vs Gastrin antagonist ) , one activity may be a subset of another ( e . g . , Dopamine ( D 2 ) agonist vs Dopamine agonist ) , or an activity can be the mechanism by which another activity works ( e . g . , ACE inhibitor vs Antihypertensive ) , etc . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Quantitative RT PCR was used to validate the results and demonstrated that there were predictable increases of three GPCRs selected for this analysis , including the dopamine D 4 , alpha 1b , and CCK B receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) has been shown to be implicated in panic attacks which can be induced by agonists at the CCK B subtype . ^^^ CCK B antagonists are thus potential antipanic agents although this has not yet been confirmed by clinical trials . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor antagonist YF 476 inhibits pancreatic enzyme secretion at a duodenal level in pigs . ^^^ BACKGROUND : To evaluate the mechanisms by which cholecystokinin ( CCK ) regulates the exocrine pancreas , the role and location of CCK receptors in the pig were investigated using the CCK B receptor antagonist YF 476 and different administration routes of CCK . ^^^ 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 . ^^^ CONCLUSIONS : These data indicate that CCK 33 given locally to the duodenum in doses raising CCK to physiological plasma levels stimulates the pancreatic enzyme secretion via duodenal CCK B receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Conversely , pretreatment with the selective CCK B antagonist triglumide did not attenuate the CCK8s induced inward current ; pretreatment with triglumide ( 3 microM ) and lorglumide ( 1 microM ) attenuated the CCK8s induced current to the same extent as pretreatment with lorglumide alone . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ CONCLUSIONS : Voluntary ingestion of ethanol differed between CCK AR ( / ) and CCK BR ( / ) mice . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
Pubmed |
SVM Score :0.0 |
| The stimulatory effect of CCK on meningioma cell growth was completely abolished by a CCK B specific receptor antagonist , L 365 , 260 . ^^^ 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 P32239 |
Pubmed |
SVM Score :0.0 |
| METHODS : Receptors of bombesin 3 , cholecystokinin ( CCK ) A , CCK B , glucagon like peptide ( GLP ) 1 , melanin concentrating hormone ( MCH ) 1 , orexin 1 , orexin 2 , neuromedin B , neuropeptide Y ( NPY ) 1 and NPY 5 , neurotensin ( NT ) 1 , NT 2 , NT 3 , and leptin receptor long form mRNA in GT 1 7 cells were detected by reversed transcriptase polymerase chain reaction . ^^^ RESULTS : Receptors of bombesin 3 , CCK B , GLP 1 , MCH 1 , orexin 1 , neuromedin B , NPY 1 , NPY 5 , NT 1 , NT 3 , and leptin receptor long form mRNA were expressed in GT 1 7 cells , of which , receptors of GLP 1 , neuromedin B , NPY 1 , and NT 3 were highly expressed . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| Colorectal and pancreatic cancers , but not the nonmalignant tissue , express a splice variant of the cholecystokinin 2 receptor ( CCK2R ) called CCK ( 2i4sv ) R that , because of intron 4 retention , contains an additional 69 amino acids within its third intracellular loop domain . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ Similarly , pretreatment with the CCK B receptor antagonist , triglumide ( 1 microM ) , did not prevent the actions of CCK 8s . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ CCK stimulates aldosterone secretion via specific receptors ( CCK 1 Rs and CCK 2 Rs in rats , and CCK 2 Rs in humans ) located in zona glomerulosa cells and coupled to the adenylate cyclase dependent signaling cascade ; and enhances glucocorticoid secretion from zona fasciculata reticularis cells via an indirect mechanism mainly involving the CCK 2 R mediated stimulation of corticotropin releasing hormone dependent ACTH release . . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| The respective receptors of these peptides , NK 3 , CCK B , and CRF 1 , were essentially expressed in pyramidal cells . ^^^ Neuropeptide effects were prevented by selective antagonists of NK 3 , CCK B , and CRF 1 receptors . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| This was blockaded by the cholecystokinin 2 receptor ( CCK 2R ) antagonists JB 95008 and JMV 1155 and by antiserum to gastrin and HB EGF . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 . ^^^ Both CCK and CCK B receptors are widely distributed in the hippocampal formation , but the functions of CCK there have been poorly understood . ^^^ Our results indicate that activation of CCK B receptors initially and transiently increased spontaneous IPSC ( sIPSC ) frequency , followed by a persistent reduction . ^^^ The effects of CCK were independent of the functions of phospholipase C , intracellular Ca ( 2+ ) release , protein kinase C or phospholipase A ( 2 ) , suggesting a direct coupling between the G proteins of CCK B receptors and 1 ( K ( Ca ) ) . ^^^ |
|
| Interacting proteins: P06307 and P32239 |
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 P32239 |
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: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P06307 and P32239 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.88841056 |
| 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 . 0.88841056^^^ |
|
| Interacting proteins: P32239 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 . ^^^ To address this issue we investigated the effect of the prolonged ( 6 day ) administration of CCK , CCK R antagonists ( CCK RAs ) and pentagastrin ( PG ) , a CCK 2 R agonist , on adult rat HPA axis . ^^^ 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 . ^^^ Taken together , these findings allow us to draw the following main conclusions : 1 ) the prolonged exposure to elevated CCK concentrations down regulates CCK R expression in the pituitary gland , which accounts for the lack of effect of CCK on ACTH secretion ; 2 ) adrenal CCK 1 Rs and CCK 2 Rs inhibit and stimulate , respectively , corticosteroid secretion ; and 3 ) endogenous CCK system plays a minor role in the physiological regulation of rat HPA axis , its main effect being the CCK 2 R mediated maintenance of adrenocortical cell number . . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ CCK stimulates aldosterone secretion via specific receptors ( CCK 1 Rs and CCK 2 Rs in rats , and CCK 2 Rs in humans ) located in zona glomerulosa cells and coupled to the adenylate cyclase dependent signaling cascade ; and enhances glucocorticoid secretion from zona fasciculata reticularis cells via an indirect mechanism mainly involving the CCK 2 R mediated stimulation of corticotropin releasing hormone dependent ACTH release . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| A hallmark of the mammalian brain cholecystokinin ( CCK ) receptor , CCK B / gastrin ( CCK BR ) , is its high affinity for two structurally related peptides , CCK and gastrin . ^^^ CCK XLR shares approximately 50 % homology at the amino acid level with both the human CCK BR and the peripheral CCK A receptor subtypes . ^^^ We used CCK XLR to map the human CCK BR domains that confer high affinity for gastrin . ^^^ A series of chimeric CCK BR / CCK XLR constructs was generated and pharmacologically characterized . ^^^ While maintaining wild type affinity for sulfated cholecystokinin octapeptide , receptors with increasing amino terminal contributions from CCK BR demonstrated a stepwise increase in gastrin affinity . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ The resultant receptor maintained high affinity binding to both CCK and gastrin and dose dependent calcium responses similar to wild type CCK BR . ^^^ |
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| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We have reported previously that the transmembrane domains of the cholecystokinin B / gastrin receptor ( CCK BR ) comprise a putative ligand binding pocket . ^^^ In the present study , we examined whether amino acid substitutions within the CCK BR pocket altered the affinities and / or functional activities of L 365 , 260 ( the prototypical nonpeptide CCK BR antagonist ) and two structural derivatives , YM 022 ( a higher affinity antagonist ) and L 740 , 093S ( a partial agonist ) . ^^^ Eight amino acids that project into the CCK BR pocket were individually replaced by alanine , using site directed mutagenesis . ^^^ For each of the nonpeptide ligands examined , a distinct series of mutations altered the affinity , suggesting that each ligand possessed a characteristic pattern of interactions within the CCK BR pocket . ^^^ Basal signaling levels and inositol phosphate formation induced by the full agonist CCK octapeptide were comparable for the wild type receptor and all of the mutant CCK BR forms . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ Ser 82 was further changed into Asp , Thr , or Ala to determine the specificity of this position in Gs coupling by the CCK BR . ^^^ Finally , CCK AR reverse mutants were studied to compare them with their corresponding CCK BR mutants that showed increased cAMP responses . ^^^ Substitution of a single residue Ser 82 to Asn in the CCK BR is sufficient to confer full cAMP responses to agonist stimulation . . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ A single nucleotide polymorphism has been found in the coding region of the CCK B receptor gene ( CCK BR ) and D Collier ( personal communication ) identified a highly polymorphic dinucleotide ( CT ) n microsatellite in the 5 ' regulatory region . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ Energy metabolism and energy turnover were increased in mice with a disruption of the CCK BR gene , although the underlying mechanism is unknown . . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ 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 . ^^^ We therefore conclude that a lack of CCK BR increases the anxiety related behavior of the mouse in the elevated plus maze . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In particular , cholecystokinin ( CCK ) receptors of the subtype B ( CCK BR ) have been shown to be overexpressed in certain neuroendocrine tumors including medullary thyroid cancer . ^^^ The human epidermoid carcinoma cell line , A 431 , was transfected with a plasmid containing the full coding sequence of the human CCK BR under a strong viral promoter , obtaining a number of receptors in the range of 2 5 10 10 ( 6 ) per cell . ^^^ An animal tumor model utilizing these two cell lines was developed to evaluate the specificity of interaction with the CCK BR and biodistribution properties of the compounds . ^^^ CCK BR positive and control cells were subcutaneously injected in opposite flanks of CD 1 female nude mice in order to obtain xenografts differing only in their ability to express CCK B receptors . ^^^ Both ( 111 ) In DTPA Glu G CCK 8 and ( 99m ) Tc Phos GC CCK 8 showed similar binding affinities for cultured CCK BR expressing cells , with dissociation constants in the range of 20 40 nM . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ 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 . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ CONCLUSIONS : Voluntary ingestion of ethanol differed between CCK AR ( / ) and CCK BR ( / ) mice . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In the anterior part , CCK B receptor stimulation could be involved in attention and memory processes . ^^^ These results suggest that endogenous CCK could play a critical role in mood modulation through CCK A / CCK B receptor stimulation . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| At the peripheral level , CCK B receptor antagonists are active on gastrin receptors , and these two receptors are similar if not identical . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Neither the gastrin nor the CCK B receptor have been cloned thus far , making it difficult to resolve whether these two receptors are distinct . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In contrast , CCK binding sites accumulating distal to the ligature possessed the pharmacological characteristics of the CCK B receptor sub type only . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| However , intraventricular administration of the CCK B receptor agonist A 63387 at 10 nmol / kg had no effect on 30 min meal size ( % suppression = 18 + / 29 ) . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor antagonists therefore have facilitatory potentialities on memory processes . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| A Free Wilson / Fujita Ban ( FW / FB ) analysis is reported on 36 `` dipeptoid ' ' antagonists of the CCK B receptor . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In contrast , i . c . v . , but not i . p . , injections of the selective CCK B receptor agonist A 63387 , reduced food intakes , although on a molar basis the effect was much less than that seen with A 71623 . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Together , these results suggest the presence of CCK B receptor subtypes . ^^^ Therefore , unlike [ 3H ] SNF 8702 , [ 3H ] pBC 264 can be used to study preparations with low receptor concentrations , such as rat brain , making this radiolabeled molecule the most appropriate ligand available to date for CCK B receptor studies . . ^^^ |
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| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Acid mimics of the potent and selective non peptide CCK B receptor antagonist CI 988 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| However , the specific CCK B receptor antagonist , L 365 , 260 ( 10 nM ) , did not alter the presynaptic facilitatory effect of CCK 8 . 6 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) analogues ( JMV 310 , JMV 320 , JMV 328 , and JMV 332 ) , obtained by side chain to side chain cyclization of a lysine residue in position 28 with a lysine residue in position 31 , were found to be highly selective for the brain CCK receptor ( CCK B receptor ) , both in guinea pig and rat . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ In contrast , the CCK B receptor antagonist , L 365 , 260 , did not affect contraction to CCK 8S ( log KB less than 7 ) but potently inhibited contraction to CCK 4 ( log KB = 9 . 24 ) . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The results demonstrate that a CCK antagonist directed to the central CCK B receptor potentiates the analgesic effects of opioid and non opioid drugs at spinal level in the rat , thus supporting the notion that CCK in the CNS may be an endogenous , physiological opioid antagonist . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Compound 9 possesses a selectivity of greater than 500 fold for the pancreatic CCK A receptor over the CCK B receptor . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Three of the rats that increased food intake after DVZ were also tested with L 365 , 260 , an antagonist selective for the CCK B receptor ( 10 ng / kg 100 micrograms / kg ) . ^^^ They do not , however , demonstrate a role for the CCK B receptor in mediating the satiating effect of ingested food under the same experimental conditions . . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ The intracerebroventricular administration of the nonselective CCK receptor agonist caerulein or the selective CCK B receptor agonist pentagastrin increased dose dependently the level of anxiety . ^^^ These results strongly suggest that activation of the brain CCK B receptor induces anxiety and that selective antagonists of this receptor represent a separate class of anxiolytic agents . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B receptor agonist , BC 264 , in doses ranging from 0 . 88 to 7 nmol . kg 1 . h 1 , had no effect on milk intake under sham feeding conditions , although it dose dependently stimulated gastric acid output . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK cyclic analogue recently developed in our laboratory that is highly selective for the CCK B receptor ( i . e . , JMV 320 ) also showed high affinity for the CCK receptor on the JURKAT cell line . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| BC 264 , a highly selective CCK B receptor agonist , did not decrease consumption of a palatable meal when administered either i . p . or into the lateral ventricles of the brain , whereas CCK decreased feeding when administered i . p . at the same doses . ^^^ 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| A new , highly selective CCK B receptor radioligand ( [ 3H ] [ N methyl Nle 28 , 31 ] CCK 26 33 ) : evidence for CCK B receptor heterogeneity . [ N methyl Nle 28 , 31 ] CCK 26 33 ( SNF 8702 ) is a nonsulfated cholecystokinin octapeptide analog that is highly selective for cholecystokinin B ( CCK B ) receptors . ^^^ In contrast to findings of single site binding in some brain regions , evidence for CCK B receptor heterogeneity is observed under other conditions . [ 3H ] SNF 8702 binding to membranes prepared from whole guinea pig brain shows biphasic association kinetics at a concentration of 2 . 0 nM consistent with the presence of binding site heterogeneity . ^^^ CCK B receptor heterogeneity is suggested by the effect of the guanyl nucleotide analogue , guanylyl imidodiphosphate ( Gpp ( NH ) p ) , on [ 3H ] SNF 8702 binding to CCK B receptors in the cerebellum . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B receptor antagonist L 365 , 260 enhances morphine analgesia and prevents morphine tolerance in the rat . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Activation of ornithine decarboxylase was triggered via a CCK B receptor type not involved in pancreatic secretion . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CONCLUSION : Cionin is a potent and efficient stimulator of gastric histamine release and acid secretion interacting via a CCK B receptor . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We examined neuroendocrine responses to intravenous infusions of pentagastrin , a selective CCK B receptor agonist , in 10 patients with panic disorder and 10 normal control subjects . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor mRNA was expressed in fetal and adult pancreas in both strains . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK B receptor antagonist Cl 988 reverses tolerance to morphine in rats . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK B receptor gene was expressed in the hypothalamus in both strains . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The role of CCK B receptor activation in memory processes has been reassessed using the three panel runway task , under conditions which avoid the effects of CCK on satiety and reduce emotional responses . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Together these results give pharmacological and behavioral evidence for the existence of CCK B receptor subtypes . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We compared the gastrin / CCK B receptor blocking properties of this compound with those of the racemate ( mixture of YM 022 and its S form ) , its enantiomer ( S form ) , L 365 , 260 and Cl 988 in vitro and in vivo . ^^^ The racemate , the S form of YM 022 , L 365 , 260 and Cl 988 also replaced gastrin / CCK B receptor binding , with Ki values of 0 . 11 , 140 , 19 and 6 . 3 nM , respectively . ^^^ 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Electrophysiological studies on slices of rat ventromedial hypothalamic nucleus showed that L 740 , 093 produced rightward shifts of the concentration response curve for the CCK B receptor agonist pentagastrin ( Kb of 0 . 06 nM ) . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This paper describes the use of the non peptidal N ( 2 adamantyloxycarbonyl ) alpha methyl tryptophan phenylethylamide template of the `` peptoid ' ' CCK B antagonist compounds 1 as a basis to probe the functional group requirements of the CCK B receptor in order to produce an agonist response . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This strategy has led to conformationally more rigid derivatives that have increased CCK B receptor binding affinity . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In contrast , L 365 , 260 , a CCK B receptor antagonist , had no effect . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Novel CCK analogs for studying CCK B receptor . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The cholecystokinin ( CCK ) B receptor cloned from human brain was characterized as a gastrin receptor by using heterologous expression systems of COS 7 cells and Xenopus oocytes . 125I gastrin binding to human CCK B receptor expressed in COS 7 was time dependent , saturable and also specific , as well as 125 1 CCK 8 . ^^^ These results suggest that the pharmacological profile of the cloned human CCK B receptor using 125I gastrin is closely parallel to that reported in gastric mucosa , and that the receptor transduces cellular signals of gastrin as well as those of CCK 8 . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Previous studies have shown that central administration of nanogram dose of CCK 8 totally abolished morphine analgesia in the rat , an effect mediated by CCK B receptor in central nervous system . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ The 32P labelled cDNA probe of the CCK B receptor coding region hybridized with an approximately 2 . 7 kb mRNA from DSL 6 pancreatic carcinoma ; no hybridizing mRNA could be identified from normal rat pancreas . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ Details of the ability to modulate the receptor interactions of these benzodiazepines by appropriate structure modifications are discussed which imply the possibility of further refining the CCK B receptor affinity and selectivity of this class of compounds . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Both CCK 8 and gastrin 1 markedly augmented phosphoinositide hydrolysis and cytosolic free calcium levels in the CHO transfectants , indicating that the cloned CCK B receptor could functionally couple with intracellular signaling molecules . ^^^ The CCK B receptor mRNA was abundantly expressed in particular areas of the human brain and stomach , such as the cerebral cortex and mucosa of the gastric fundus . ^^^ This is the first demonstration of trophic effects of CCK and gastrin through the normal human brain CCK B receptor . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Most of these compounds proved to be selective for the CCK B receptor , the most potent analog , N [ N [ ( 2 adamantyloxy ) carbonyl ] D alpha methyltryptophanyl ] N [ 2 ( 4 chlorophenyl ) ethyl ] glycine ( 26A ) , having a Ki value of 6 . 1 nM for guinea pig cortex membranes in vitro and a good selectivity ratio ( Ki CCK A / Ki CCK B = 174 ) . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Clearly , the receptor responsible for activation of the ECL cells distinguishes poorly between gastrin 17 and CCK 8s , which is in line with the characteristics of the CCK B receptor . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The results suggest that an increased release of CCK 8 following EA may limit the effect of opioid peptides , and that the CCK B receptor mediates the anti opioid effect of CCK 8 in rat spinal cord . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Administration of both CCK A and CCK B receptor antagonists alone resulted in no change in meal size . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ It would be expected that YM 022 , a potent and selective gastrin CCK B receptor antagonist , inhibits gastric acid secretion without inducing gastrin mediated side effects such as hypergastrinemia and hyperplasia of oxyntic mucosa . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| METHODS : The effect of a new , potent and selective CCK B receptor antagonist , CI 988 on the growth of LoVo , a human colon cancer cell line both in vitro and in vivo was instigated . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ This effect of a CCK B receptor antagonist was not mediated by the spinal opioid receptor activation . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We utilized intravenous infusions of pentagastrin , a selective CCK B receptor agonist , and studied behavioral and cardiovascular responses in 10 patients with panic disorder and 10 normal controls . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Structure activity relationship studies of this series suggested that a number of analogues retained good in vitro potency for gastrin / CCK B receptor . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ CCK B receptor mRNA was detected by Northern blot analysis in the brain and the fundus mucosa but not in the rest of the digestive tract and not in the pancreas , pancreatic islets , or kidney . ^^^ By RT PCR , expression of CCK B receptor mRNA could also be detected in antrum mucosa . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| No changes in measures of anxiety , hunger , or short term memory were observed at doses of L 365 , 260 shown to have antagonist activity at the CCK B receptor . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Pig pancreatic acinar cells possess predominantly the CCK B receptor subtype . ^^^ RNA were extracted for CCK A and CCK B receptor expression using specific cRNA probes . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| To gain a better understanding of the role of cholecystokinin ( CCK ) B receptor in the maintenance of thermal hyperalgesia induced by unilateral constriction injury to the sciatic nerve in the rat , this study evaluated the effects of intrathecally administered YM 022 ( a CCK B receptor antagonist ) on thermal hyperalgesia . ^^^ These data indicate that a CCK B receptor antagonist attenuates the level of thermal hyperalgesia and this effect of a CCK B receptor antagonist is time dependent . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ Expression of the CCK B receptor gene was detected in both strains by RT PCR . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Receptor binding results suggest that the preferred topography of the Trp 30 residue for CCK B receptor binding may be the 2S , 3S ( erythro L ) configuration whereas for the delta opioid receptor it may be the 2S , 3R ( threo L ) configuration . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Introduction of more bulky substituents than NalNH 2 on the C terminal part decreased the CCK B receptor binding affinity . ^^^ In the newly synthesized compounds , 13 : 2Adoc D alpha MeTrp Phg Asp NalN ( CH 3 ) 2 and 16 : 2Adoc D alpha MeTrp Phg Asp NalNH 2 had the best CCK B receptor affinities ( KI = 3 . 5 and 3 . 4 nM , respectively ) and were selected for further biological evaluation . ^^^ Interestingly , when tested for their capacity to influence inositol phosphate formation , induced by CCK 8 in CHO cells transfected with the rat CCK B receptor , compound 13 behaved as a full CCK B antagonist with an IC 50 value of 18 + / 1 nM , being as potent as the antagonist L 365 , 260 and PD 134 , 308 ( IC 50 values respectively , 39 + / 17 and 30 + / 2 nM ) , whereas compound 16 was found to behave as a partial CCK B agonist . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Highly specific , CCK B receptor antagonists have reached clinical trials and have potential clinical utility as anxiolytics , antipsychotics , anti anorexics , or analgesics . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK B receptor mRNA expression was detectable in only 1 / 14 ( 7 % ) samples of gastric cancer , although it was detectable in 10 / 12 ( 83 % ) body mucosa of the stomach . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK release from the synaptosomes , and levels of CCK and CCK B receptor mRNAs were the same as those observed in normal rats . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ Northern blot analysis revealed a significant expression of CCK B receptor mRNA in GH 3 cells , but not in normal rat pituitary glands . ^^^ These findings provided the first evidence for an autocrine / paracrine role of CCK and gastrin on stimulation of GH 3 cell growth through the CCK B receptor . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK B receptor gene . ^^^ A stable Chinese hamster ovary cell line expressing the human CCK B receptor gene is described ( hCCK B . ^^^ In radioligand binding experiments employing membranes derived from these cells the rank order of affinity estimated for a series of CCK receptor ligands ( CCK 8S > CI 988 > PD 135158 > pentagastrin > CCK 8NS > L 365 , 260 > CCK 4 > LY 288513 > devazepide > A 71378 > lorglumide ) was found to be in excellent agreement with CCK B receptor pharmacology described in guinea pig cortex . ^^^ The CCK B receptor selective agonist CCK 4 stimulated the mobilization of intracellular Ca2+ with an estimated pEC 50 value of 7 . 4 . ^^^ Consistent with CCK B receptor pharmacology , the rank order of potency for antagonism of this response was observed to be PD 135158 > CI 988 > L 365 , 260 > > devazepide > lorglumide . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Porta caval shunting enhances the trophic effects of cholecystokinin ( CCK ) A receptor activation on the pancreas and of CCK B receptor activation on the ECL cells in the oxyntic mucosa of the rat . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin induced antinociception is not blocked by CCK A or CCK B receptor antagonists . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We compared the changes in pancreatic regeneration in terms of wet weight and protein and DNA contents after partial pancreatectomy ( 30 % resection ) in OLETF and control ( Long Evans Tokushima Otsuka : LETO ) rats and examined whether the CCK B receptor has a role in pancreatic regeneration after pancreatectomy . ^^^ CCK B receptor gene expression was not enhanced after pancreatectomy . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 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 . ^^^ The CCK B receptor agonist also induced mainly increases in the neuronal firing . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In vivo , however , infusions of CCK A mRNA antisense ODN did not alter CCK B receptor binding levels . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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 . ^^^ 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 . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| However , when rats were pretreated with antigastrin serum or CCK B receptor antagonist , the acid secretion by TE was virtually abolished . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In summary , receptor activation had opposite effects on growth parameters in CHO and Swiss 3T3 cells , but only minor differences were observed in the characteristics of CCK B receptor coupling to specific second messengers in the two cell types . ^^^ Thus cellular context is a principal determinant of the biological effects of CCK B receptor activation , and differences in biological responses may occur independently of major differences in receptor coupling . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Several explanations , including the existence of different sub sites of the CCK B receptor , could account for these differential effects . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ These results suggest that CCK B receptor is involved in the behavior of TN gene knockout mouse through striatal DA transmission . . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ The results suggest that ' anxious ' behavior induced by CCK is associated with selective CCK B receptor stimulation . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The aim of this study was to evaluate whether radiolabelled gastrin may be suitable for targeting CCK B receptor expressing tumours in vivo . ^^^ Future preclinical and clinical studies will address in more detail the molecular features that render CCK B receptor binding agents potentially useful candidates for in vivo scintigraphy and radionuclide therapy . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The effect of CI 988 , a CCK B receptor antagonist , on the facilitation of the flexor reflex induced by conditioning stimulation ( CS ) of C afferents was also examined . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Unsulfated DTPA and DOTA CCK analogs as specific high affinity ligands for CCK B receptor expressing human and rat tissues in vitro and in vivo . ^^^ Recently , the CCK B receptor , which binds both gastrin and cholecystokinin with high affinity , was shown using in vitro methods to be overexpressed in a number of human tumor tissues , including medullary thyroid carcinomas , small cell lung cancers , astrocytomas , gastrointestinal tumors , and stromal ovarian cancers . ^^^ In the present study , we have designed novel , unsulfated CCK octapeptide analogs linked to the metal chelating DTPA and DOTA , and have tested them for their binding affinity to CCK B receptor positive tissue from human tumors : The most potent compounds assayed were DTPA [ Nle 28 , 31 ] CCK ( 26 33 ) ( MP 2286 ) and DTPA [ d Asp 26 , Nle 28 , 31 ] CCK ( 26 33 ) ( MP 2288 ) with an IC 50 of 1 . 5 nM . ^^^ The CCK B receptor expressing gastric mucosa showed specific in vivo accumulation of 111In labeled MP 2288 which could be blocked in the presence of excess unlabeled MP 2288 . 111In labeled MP 2286 and MP 2288 were also found to be stable in human plasma whereas both compounds were degraded in urine ( > 40 % after 3 h at 37 degrees C ) . ^^^ The affinity , specificity , biodistribution , and stability of these two DTPA CCK analogs indicate that these compounds have substantial promise for use in the in vivo visualization of CCK B receptor expressing tumors . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Blockade of gastric acid secretion by YM 022 ( CCK B receptor antagonist ) or famotidine ( histamine 2 receptor antagonist ) resulted in a significant suppression of casein stimulated pancreatic exocrine secretion as determined by juice volume and amylase secretion . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ Microinjections of the selective CCK B receptor antagonist , LY 288513 ( 1 . 05 , 4 . 2 , 17 . 0 nmol / 0 . 25 microliter ) , into the PAG suppressed the hissing response in a dose and time dependent manner . ^^^ This finding demonstrates the specificity of the effects of CCK B receptor blockade upon hissing . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Neither its CCK B receptor antagonistic moiety of Compound 1 ( Compound 2 ) nor its histamine H 2 receptor antagonistic moiety of Compound 1 ( Compound 3 ) had any effect on [ 125I ] PYY binding , suggesting that the entire structure of Compound 1 is essential for Y 1 receptor blocking activity . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ The structurally related benzodiazepines L 365 , 260 , L 740 , 093 , and YM 022 are selective antagonists of the CCK B receptor subtype . ^^^ Their in vitro pharmacological profiles have been characterized using the human CCK B receptor expressed in CHO cells . 5 . ^^^ L 365 , 260 behaves in a manner consistent with that of a competitive antagonist and both L 740 , 093 and YM 022 behave as insurmountable CCK B receptor antagonists in vitro . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| These effects were reversed by PD 135 , 158 , a selective CCK B receptor antagonist ( 0 . 1 mg / kg , s . c . ) , administered 5 min prior to ceruletide . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In contrast , mouse NIH3T3 fibroblasts transfected with human CCK B receptor ( NIH3T3CCK BR ) showed increased proliferation and phosphorylation to the peptides . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| An increased expression of cholecystokinin ( CCK ) messenger RNA ( mRNA ) as well as CCK B receptor mRNA in dorsal root ganglion ( DRG ) cells following peripheral axotomy has previously been demonstrated . ^^^ We also compared the effects of the CCK B receptor antagonist CI 988 on basal and potassium stimulated CCK LI release in intact animals and in chronically axotomized rats . ^^^ The present data suggest that axotomy reduces the release of CCK like immunoreactivity in the spinal cord by a mechanism involving the CCK B receptor binding site . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Furthermore , infusion of the CCK B receptor antagonist L 365 , 260 significantly blocked the increase of RMCP 2 concentration after OVH . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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 . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| However , sciatic nerve section was associated with a marked ipsilateral increase in both CCK B receptor mRNA levels in these ganglia ( +70 % ) and the autoradiographic labeling of CCK B receptors by [ 3H ] pBC 264 ( +160 % ) in the superficial layers of the lumbar dorsal horn . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor mRNA was expressed in the pancreas , but not in gallbladder and duodenum . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Furthermore , CI 988 , an antagonist of the CCK B receptor , chronically coadministered with morphine , reduces autotomy , a behavior that may be a sign of neuropathic pain following peripheral nerve section . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Expression of the CCK B receptor gene was observed in the stomach , pancreas , and brain in both OLETF and LETO rats by the RT PCR method , with expression of the CCK B receptor gene markedly enhanced in OLETF rats compared with that in LETO rats . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| GV 150013 , a selective CCK B receptor antagonist , was found to increase REM sleep , as well as non REM sleep , and therefore total sleep ( non REM + REM ) mainly in aged rats . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor : chemistry , molecular biology , biochemistry and pharmacology . ^^^ The physiological and pathological implication of CCK B receptor will be confirmed in CCK B receptor deficient mice obtained by gene targeting ( Nagata el al . , 1996 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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 . ^^^ RT PCR / Southern blot analysis also showed CCK A and CCK B receptor mRNA expression in fetal and infant pancreas . ^^^ These results show that the both CCK receptor types are expressed in human pancreas at stages of early gestation , but there is predominant expression of CCK B receptor in adult pancreas . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Disruption of cholecystokinin ( CCK ) B receptor gene did not modify bile or pancreatic secretion or pancreatic growth : a study in CCK B receptor gene knockout mice . ^^^ Pancreatic exocrine function and bile secretion were examined in cholecystokinin ( CCK ) B receptor gene targeted mice and compared among different genotypes [ i . e . , CCK B receptor gene : ( + / + ) , wild type ; ( + / ) , heterozygous ; and ( / ) , homozygous deficient ] . ^^^ These results indicated that the CCK B receptor has no role in pancreatic growth , exocrine secretion , or bile secretion in adult mice . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In accordance with their comparably low affinity , nonsulfated members of the CCK family showed fairly low uptake in the tumor and other CCK B receptor expressing tissues . ^^^ Best tumor uptake and tumor to nontumor ratios were obtained with members of the gastrin family because of their selectivity and affinity for the CCK B receptor subtype . ^^^ In a pilot clinical study , radioiodinated and 111In labeled derivatives showed excellent targeting of physiological CCK B receptor expressing organs , as well as all known tumor sites . ^^^ CONCLUSION : CCK / gastrin analogs may be a useful new class of receptor binding peptides for diagnosis and therapy of CCK B receptor expressing tumors , such as MTC or small cell lung cancer . ^^^ 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In a pilot study , we have demonstrated the feasibility of radiolabeled gastrin 1 to target CCK B receptor expressing tissues in vivo in animals and patients ( T . ^^^ In accordance to their comparably low affinity , nonsulfated members of the CCK family showed fairly low uptake in the tumor and other CCK B receptor expressing tissues ( e . g . , the stomach ) . ^^^ Best tumor uptake and tumor : nontumor ratios were obtained with members of the gastrin family , probably because of their selectivity and affinity for the CCK B receptor subtype . ^^^ Pilot therapy experiments in MTC bearing animals showed significant antitumor efficacy as compared with untreated controls . ( 111 ) In Labeled diethylene triamine pentaacetate derivatives of minigastrin showed excellent targeting of CCK B receptor expressing tissues in animals and a normal human volunteer . ^^^ These data suggest that CCK / gastrin analogues may be a useful new class of receptor binding peptides for diagnosis and therapy of CCK B receptor expressing tumors , such as MTC or small cell lung cancer . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Indeed , 111In labeled DTPA derivatives of gastrin showed excellent targeting of CCK B receptor expressing tissues in animals and patients . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Preclinical and initial clinical evaluation of 111In labeled nonsulfated CCK 8 analog : a peptide for CCK B receptor targeted scintigraphy and radionuclide therapy . ^^^ METHODS : The aim of this study was to evaluate in vitro and in vivo whether 111In labeled CCK B receptor specific CCK 8 analog [ D Asp 26 , Nle 28 , 31 ] CCK 26 33 ( D Asp Tyr Nle Gly Trp Nle Asp Phe NH 2 ) is suitable for CCK B receptor scintigraphy based on the finding that unlabeled nonsulfated diethylenetriamine pentaacidic acid [ DTPA 0 ] CCK 8 and tetraazacyclododecanetetraacetic acid [ DOTA 0 ] CCK 8 analogs show high and specific binding for CCK B receptors in human tumors . ^^^ RESULTS : In vitro , [ 111In DOTA 0 ] CCK 8 showed specific internalization in CCK B receptor positive rat pancreatic tumor cells AR42J . ^^^ From the data obtained with [ 111In DOTA 0 ] CCK 8 and ( 125I ) 1 gastrin , the latter being a specific ligand for the CCK B receptor , the rat pancreatic cell line CA 20948 also appeared to be CCK B receptor positive . ^^^ In vivo biodistribution experiments in CA 20948 tumor bearing Lewis rats showed rapid clearance of [ 111In DOTA 0 ] CCK 8 , and specific uptake was found in the CCK B receptor expressing stomach and tumor . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| RESULTS : The cell line LN 36 responded with increased cell number to stimulation by gastrin 17 and decreased cell number to inhibition by the CCK B receptor antagonist L 365 , 260 . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK A receptor antagonist L 364 , 718 was 300 fold more potent than the CCK B receptor antagonist L 365 , 260 at inhibiting CCK 8 induced contraction . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Using reverse transcription polymerase chain reactions , CCK B receptor mRNA was expressed in all specimens of normal fetal and postnatal human pancreas , adult pancreas , and pancreatic adenocarcinomas . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| These findings suggest that CCK B receptor antagonists might be of some value in the treatment and prevention the relapse of opiate addicts . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Structure and developmental expression of the mouse CCK B receptor gene . ^^^ We have cloned the mouse CCK B receptor gene ( Cckbr ) and determined its complete genomic structure , nucleotide sequence , and tissue specific expression pattern . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ Gastrin / CCK B receptor mRNA was present in all carcinomas , resection margins , and normal pancreatic tissue . ^^^ |
|
| Interacting proteins: P32239 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 ) . ^^^ The CCK B receptor antagonist was not more effective at blocking . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We injected the CCK B receptor antagonist PD 135 , 158 into the PVTh before restraint in control and chronically cold stressed rats . ^^^ In addition , CCK B receptor mRNA expression in the pPVTh was not altered by chronic cold stress . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In all patients there was visualization of the CCK B receptor positive stomach . ^^^ In conclusion : ( 1 ) the CCK B receptor positive gastric mucosa and presumed MTC lesions could be visualized in patients using an octapeptide [ 111In DTPA ] CCK analogue that is probably internalized , proving the feasibility of CCK B receptor imaging in vivo ; ( 2 ) there was a relatively low uptake of the CCK analogue in the strongly CCK receptor positive stomach , and rapid degradation of the peptide in serum . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| These results show the CCK B receptor blockade mediated antinociceptive effects and reveals the antinociceptive action of morphine in diabetic rats after CCKergic system inhibition . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| To explore relationships between CCK B receptor activation , the HPA axis response , and AVP release , a dose response study using the CCK B receptor agonist pentagastrin was conducted . ^^^ These findings suggest a possible role for the CCK B receptor in AVP release , which may be at least partially separate from its role in modulation of the HPA axis . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B receptor antagonist CI 988 ( 2 mg / kg , i . p . ) reduced the anxiety like behavior without affecting the increase in CCKLM outflow . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Indeed , 111In labeled DTPA derivatives of gastrin showed excellent targeting of CCK B receptor expressing tissues in animals and patients . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Mitogenic effects of gastrin 1 on ductal complexes in vivo and of tetragastrin , pentagastrin , and gastrin 1 and 2 , with or without the CCK B receptor antagonist L 365 , 260 , on duct like cells in vitro were analyzed by 5 bromo 2 ' deoxyuridine labeling . ^^^ Immunocytochemistry , Western blotting , and reverse transcription polymerase chain reaction were applied for detection of the CCK B receptor . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| As a proof of concept , it could be demonstrated that a majority of medullary thyroid cancer primary tumors and metastases are visualized in vivo with CCK B receptor scintigraphy using these radioligands . ^^^ More recently , radiotherapy of CCK B receptor expressing medullary thyroid cancers with radiolabeled minigastrin has been successfully reported in a small number of patients , giving support to the proposal that CCK B receptors overexpressed in tumors represent a useful target for clinical application . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In this study , we have investigated the CCK B receptor ( CCKBR ) gene , which is the main constituent of the CCK receptor in the CNS . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The aim of our work was to develop and systematically optimize suitable radioligands for targeting CCK B receptors in vivo and to investigate their role in the staging and therapy of MTC and other CCK B receptor expressing malignancies . ^^^ Best tumor uptake and tumor to nontumor ratios were obtained with members of the gastrin family , because of their superior selectivity and affinity for the CCK B receptor subtype . ^^^ Radiometal labeled derivates of minigastrin showed excellent targeting of CCK B receptor expressing tissues in animals and healthy human volunteers . ^^^ CCK B receptor scintigraphy was performed with ( 111 ) In diethylenetriamine pentaacetic acid d Glu ( 1 ) minigastrin . ^^^ The normal organ uptake was essentially confined to the stomach ( and , to a lesser extent , to the gallbladder and , in premenopausal women , to normal breast tissue ) as a result of CCK B receptor specific binding and to the kidneys , as excretory organs . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Neither CCK A nor CCK B receptor mediates amylase release from human pancreatic acini in vitro . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ CCK B receptor antagonists might be of some value in the treatment and prevention of relapse to stress induced to drug craving following long term detoxification . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| A spliced variant of the CCK B receptor was identified which differed from the CCK B receptor by the presence of intron 4 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| These data support the hypothesis that CCK B receptor mediated activation of the HPA axis is relatively resistant to cortisol feedback inhibition . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This cell line was used to characterize the agonist dependent regulation of CCK A and CCK B receptor gene expression . ^^^ In contrast , the level of CCK B receptor gene expression was upregulated to 157 % and 153 % , respectively . ^^^ These effects are most probably linked to the CCK B receptor in AR42J cells . ^^^ The phorbolester PMA ( 100 nM ) , a protein kinase C activator , downregulated CCK A receptor expression but did not affect CCK B receptor gene transcription . ^^^ CONCLUSION : These results demonstrate that CCK A and CCK B receptor mRNA levels are differentially regulated by their agonists via distinct signal transduction mechanisms in AR42J cells . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin B ( CCK B ) / gastrin receptor targeting peptides for staging and therapy of medullary thyroid cancer and other CCK B receptor expressing malignancies . ^^^ The aim of our recent work was to develop and systematically optimize suitable radioligands for targeting CCK B receptors in vivo and to investigate their role in the staging and therapy of MTC and other CCK B receptor expressing malignancies . ^^^ Best tumor uptake and tumor to nontumor ratios were obtained with members of the gastrin family , due to their superior selectivity and affinity for the CCK B receptor subtype . ^^^ Radiometal labeled derivatives of minigastrin showed excellent targeting of CCK B receptor expressing tissues in animals and healthy human volunteers . ^^^ CCK B receptor scintigraphy was performed with ( 111 ) In DTPA D Glu ( 1 ) minigastrin . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Chronic anxiolytic treatment with the selective CCK B ( CCK ( 2 ) ) receptor antagonist , Ci 988 ( 0 . 3 mg / kg / day ip ) or diazepam ( 2 mg / kg / day ip ) , induced numerous effects throughout the central nervous system ( CNS ) , with Ci 988 inducing significant changes in the density of dopamine D ( 2 ) receptors , and diazepam producing marked changes in both dopamine D ( 2 ) and CCK B receptor binding density as well as preproCCK mRNA expression . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ 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: P32239 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: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Central microinjection of CCK in rats induces a thermogenic response that can be attenuated by CCK B receptor antagonists , but some authors observed a hypothermia . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We therefore determined the allele and genotype frequencies of a single nucleotide polymorphism in the CCK gene ( 36C > T ) and one CT repeat polymorphism in the CCK B receptor gene in a German panic disorder sample ( n = 115 for CCK gene polymorphism , n = 111 for CCK B receptor polymorphism ) and compared them with gender and age matched controls . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptor antagonist YF 476 inhibits pancreatic enzyme secretion at a duodenal level in pigs . ^^^ BACKGROUND : To evaluate the mechanisms by which cholecystokinin ( CCK ) regulates the exocrine pancreas , the role and location of CCK receptors in the pig were investigated using the CCK B receptor antagonist YF 476 and different administration routes of CCK . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Similarly , pretreatment with the CCK B receptor antagonist , triglumide ( 1 microM ) , did not prevent the actions of CCK 8s . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Colorectal and pancreatic cancers , but not the nonmalignant tissue , express a splice variant of the cholecystokinin 2 receptor ( CCK2R ) called CCK ( 2i4sv ) R that , because of intron 4 retention , contains an additional 69 amino acids within its third intracellular loop domain . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This was blockaded by the cholecystokinin 2 receptor ( CCK 2R ) antagonists JB 95008 and JMV 1155 and by antiserum to gastrin and HB EGF . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This is the case of BUBU , Tyr D Ser ( OtBu ) Gly Phe Leu Thr ( OtBu ) and BUBUC , Tyr D Cys ( OtBu ) Gly Phe Leu Thr ( OtBu ) for the opioid delta receptors and of BC 254 , Boc gamma D Glu Tyr ( SO3H ) Nle D Lys Trp Nle Asp PheNH 2 and of BC 264 , Boc Tyr ( SO3H ) gNle mGly Trp MeNle Asp PheNH 2 for central CCK B receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This was quantified by measuring the effects of both inhibitors on the in vivo binding of [ 3H ] propionyl Tyr ( SO3H ) gNle mGly Trp ( N Me ) Nle Asp Phe NH 2 ( [ 3H ] pBC 264 ) , a selective and highly potent CCK B agonist . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Both CCK A and CCK B / gastrin receptors are present on rabbit vagus nerve . ^^^ Competitive binding studies using A 63387 , a selective CCK B / gastrin receptor agonist , also showed biphasic displacement curves , with the high affinity portion ( less than 30 nM ) at approximately 40 % and the low affinity portion at approximately 60 % . ^^^ 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 ) . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The new compounds were assayed in CCK binding assays using homogenated rat pancreatic membranes and bovine striatum as a source of CCK A and CCK B receptors respectively and in vivo in rats for anorectic activity . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| To this end , we tested the effects of both unselective CCK agonists CCK 8 and caerulein , and CCK B selective agonists CCK 4 and pentagastrin as well as the selective CCK antagonists ( devazepide and L 365 , 260 ) at wide dose ranges on the cold stimulated and TRH induced TSH and PRL secretion . ^^^ 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
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| Interacting proteins: P32239 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 B antagonist CI 988 ( 20 ng ) blocked CCK inhibition of dopamine induced hyperlocomotion in the anterior nucleus accumbens . ^^^ The CCK B antagonists CI 988 ( 20 ng ) and L 365 , 260 ( 10 ng ) blocked CCK potentiation of dopamine induced hypolocomotion in the ventral tegmental area . ^^^ 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The selective CCK B agonist , BC 264 injected in the antero lateral part of the nucleus accumbens , reduces the spontaneous alternation behaviour of rats . ^^^ The aim of this study was to examine the behavioural effects induced by stimulation of CCK receptors in the nucleus accumbens of the rat , which contains a high density of heterogenously distributed CCK B receptors . ^^^ The drug BC 264 ( Boc Tyr ( SO3H ) gNle mGly Trp ( NMe ) Nle Asp Phe NH 2 ) , a highly potent and selective CCK B agonist , injected into the postero median or antero median n . accumbens did not modify the spontaneous alternation and exploratory behaviour observed in a Y maze . ^^^ This effect was suppressed by the selective CCK B antagonist : L 365 , 260 , but not by the selective CCK A antagonist : MK 329 . ^^^ These results emphasize the functional heterogeneity of the CCK network in the n . accumbens of the rat and the participation of the peptide in the expression of alternation behaviour , through stimulation of CCK B receptors . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ However , the effect of CCK on cortisol secretion does not appear to involve either CCK A or CCK B receptors . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Four analogues of cholecystokinin ( CCK ) octapeptide having analgesic activity after i . c . v . administration and high affinity for CCK B receptors were studied for their ability to displace specific ligands , [ 3H ] D Phe Cys Tyr D Trp Orn Thr Pen Thr NH 2 . [ 3H ] [ D Pen 2 , 4 ' Cl Phe 4 , D Pen 5 ] enkephalin and [ 3H ] U 69 , 593 , for mu , delta and kappa opioid receptors , respectively . ^^^ The results suggest a relationship between the ligand requirements of CCK B and delta opioid receptors which further implies a possible structural relationship between these receptors . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Rationally designed `` dipeptoid ' ' analogues of CCK . alpha Methyltryptophan derivatives as highly selective and orally active gastrin and CCK B antagonists with potent anxiolytic properties . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Neurochemical actions of CCK underlying the therapeutic potential of CCK B antagonists . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In an effort to evaluate CCK antagonists as potential antipsychotic drugs , we have examined the effects of a selective CCK B antagonist , LY 262691 , on the number of spontaneously active midbrain dopamine neurons using extracellular , single unit recordings in anesthetized rats . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ They were , however , weak and behaved as partial agonists in calcium studies in NCI H 345 cells , which possess CCK B / gastrin receptors . ^^^ In guinea pig gastric glands , the affinities of A 71623 and A 70874 for the CCK B / gastrin receptor were 11 and 1 . 6 microM , respectively . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B ( gastrin ) receptor regulates gastric histamine release and acid secretion . ^^^ 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 . ^^^ We conclude that G ( 1 17 ) and CCK ( 1 33 ) stimulate histamine and acid secretion by a CCK B ( gastrin ) receptor . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ L 365 , 260 is the more potent , suggesting a role for central CCK B type receptors in satiety . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ Chemical manipulations of the structure of lorglumide led to the discovery of selective antagonists of the CCK B / gastrin receptors . ^^^ Some of these new derivatives exhibit different affinities with rabbit gastric gland cells and rat cortex membranes , suggesting that the stomach gastrin receptor ( arbitrarily termed CCK B 1 receptor ) is not as closely related to the CCK central receptor ( termed CCK B 2 ) as previously hypothesized . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Development of CCK B antagonists . ^^^ Our approach to design small molecule non peptide analogues of the neuropeptide cholecystokinin ( CCK ) has led to the discovery of the CCK B antagonist ' dipeptoids ' . ^^^ This dipeptide has been systematically chemically modified at the N and C terminal to increase CCK B binding affinity 10 , 000 fold . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| PD 134308 and PD 135158 are potent and selective antagonists at the cholecystokinin type B ( CCK B ) receptors with IC 50 values of 1 . 6 nM and 3 . 5 nM , respectively , in the radioligand binding assay and Ke values of 7 . 82 and 12 . 9 nM , respectively , in their blocking action on CCK responses in the rat lateral hypothalamic slice . ^^^ Both CCK B antagonists were able to suppress the withdrawal anxiogenesis and produce an anxiolytic effect in mice previously made tolerant to diazepam . ^^^ The CCK B antagonists also showed powerful anxiolytic activity in the `` marmoset human threat test . ' ' These results provide evidence of a selective role for CCK B receptors in the control of anxiety . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 ) . ^^^ L 365 , 260 was more potent , suggesting that central CCK B type receptors may mediate the satiety effects of endogenously released CCK . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We showed that : 1 ) Suppression of the C terminal phenylalanine residue leads to peripheral as well as central cholecystokinin receptor antagonists ; 2 ) Suppression of the C terminal amide function produces `` partial agonists ' ' exhibiting interesting biological and pharmacological activities ; 3 ) Replacement of L tryptophan residue by D tryptophan in such `` partial agonist analogues ' ' resulted in potent CCK receptor antagonists ; 4 ) The peptide bond between methionine 28 and glycine 29 , as well as the glycine residue are quite significant for the central biological activity ; 5 ) It is possible to obtain highly potent and selective CCK analogues for the central receptor ( CCK B ) by cyclization including the C terminal tetrapeptide . ^^^ 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 . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The results suggest that the exploratory behaviour of rats can be altered by pharmacological manipulations at CCK B receptors . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Proglumide does not discriminate between CCK A and CCK B ( central type ) receptors . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK antagonists interact with CCK B receptors on human small cell lung cancer cells . ^^^ |
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| Interacting proteins: P32239 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 ) . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ 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 . ^^^ In contrast , A 71378 was relatively weak ( EC 50 = 600 nM ) in mobilizing intracellular calcium from NCI H 345 cells , which express CCK B / gastrin receptors . ^^^ The high potency and selectivity of A 71378 for the CCK A over CCK B and gastrin receptors is unprecedented among CCK peptides . ^^^ |
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| Interacting proteins: P32239 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 ) . ^^^ We describe here the properties of tert butyloxycarbonyl Trp Leu Asp Phe NHNH 2 ( A 57696 ) , a C terminal hydrazide analogue of tert butyloxycarbonyl CCK 4 ( Boc Trp Met Asp Phe NH 2 ) , at four cholecystokinin ( CCK ) receptor bearing tissues , the guinea pig pancreas and gall bladder ( Type A ) , guinea pig cortex ( Type B ) , and NCI H 345 cells , a human small cell lung cancer cell line that expresses CCK B / gastrin receptors . ^^^ 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 ) . ^^^ In contrast , A 57696 behaved as a partial agonist ( 80 % of maximal CCK 8 response ) in stimulating calcium mobilization at CCK B / gastrin receptors on NCI H 345 cells . ^^^ 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 . ^^^ |
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| Interacting proteins: P32239 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 B receptors are found ubiquitously throughout other regions of the neuraxis . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Postponement of satiety by blockade of brain cholecystokinin ( CCK B ) receptors . ^^^ 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 . ^^^ These results suggest that endogenous CCK causes satiety by an agonist action on CCK B receptors in the brain . . ^^^ |
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| Interacting proteins: P32239 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 . . ^^^ |
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| Interacting proteins: P32239 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 . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Binding of raclopride to dopamine D 2 , SCH 23390 to dopamine D 1 , ketanserin to serotonin 5 HT 2 , 8 hydroxy 2 ( di n propylamino ) tetralin to serotonin 5 HT1A , and cholecystokinin ( CCK ) 8 to CCK B sites was measured in tissue homogenates from the striatum or fronto parietal cortex . ^^^ Binding to striatal D 1 and frontoparietal cortex CCK B sites was reduced over the course of a 27 h postmortem delay . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK B selective antagonist L 365 , 260 ( ( 3R ( + ) 2 , 3 dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepine 3yl ) N ( 3 methylphenyl ) urea ) was inactive up to a concentration of 30 nM . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ In contrast , selective and biologically active CCK B agonist had no effect . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Gastrin ( 2 17 ds ) increased cell proliferation by 2 fold with an IC 50 of 150 pM , corresponding to the occupancy of the CCK B receptors . ^^^ CR 1409 , at concentrations that fully occupied CCK B receptors , inhibited the gastrin ( 2 17 ds ) effects . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Derived by chemical modification of the benzodiazepine ring system embedded within the CCK B antagonist L 365 , 260 , these compounds display CCK B / CCK A selectivity and some analogs have receptor binding affinities in the subnanomolar range . ^^^ This group of novel imidazobenzodiazepines , among which N [ ( 2S , 4R ) methyl 6 phenyl 2 , 4 dihydro 1H imidazo [ 1 , 2 alpha ] [ 1 , 4 ] benzodiazepin 4 yl ] N ' [ 3 methylphenyl ] urea ( 12 ) is the principal compound , expands the structural diversity of the collection of non peptide CCK B antagonists and will be useful in further delineating the function of CCK in the central nervous system . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Conformationally readdressed CCK B / delta opioid peptide ligands . ^^^ The sequence of a cholecystokinin ( CCK ) related peptide was modified to obtain analogues , which interact selectively either with CCK B , or with delta opioid receptors . ^^^ 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 . ^^^ The results of this study demonstrate a possibility to redirect a peptide sequence that interacts with one type of receptors ( CCK B receptors ) toward interaction with another type ( delta opioid receptors ) belonging to a different physiological system . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Exogenously applied CCK depolarizes supraoptic neurons , acting at postsynaptic CCK B type receptors . ^^^ |
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| Interacting proteins: P32239 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 . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| All had essentially the same sequence contained within 2 of these clones consisted of 427 amino acids and was 92 % homologous ( 87 % identity ) to the known rat pancreatic CCK A sequence but only 43 % homologous to the gastric CCK B sequence . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ These results demonstrate directly for the first time that guinea pig chief cells possess CCK A R and CCK B R . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| RESULTS : In the cardiac and fundic stomach , CCK B / gastrin receptors were found in the mucosa and in a subpopulation of neuronal elements in the circular muscle . ^^^ The antrum expressed CCK B / gastrin receptors in a few neurons in the circular muscle and in the entire myenteric plexus ; no receptors were observed in the antral mucosa or esophagus . ^^^ The duodenum showed a high concentration of CCK B / gastrin receptors in the myenteric plexus . ^^^ CCK B / gastrin receptor expression in a subset of neurons in gastric circular muscle suggests a novel site of action for CCK and / or gastrin . . ^^^ 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 . ^^^ |
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| Interacting proteins: P32239 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 . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In this review , the studies evaluating the putative involvement of CCK , and especially CCK B receptors , in panic disorder will be discussed . . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ) . ^^^ In contrast , the selective CCK B agonist BC 264 ( 62 micrograms / kg i . v . ) produced a hyperalgesic effect that was antagonized by 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 ) . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The present findings demonstrate an opposing physiological role of endogenous CCK , acting on CCK B receptors , and opioid peptides in the control of pain perception at both spinal and supraspinal levels . ^^^ These results could have important clinical applications because a combination of a CCK B antagonist and RB 101 , which has been showed to be almost devoid of morphine side effects , would increase the overall antinociceptive efficacy into a range that will be more clinically useful . . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Effects induced by BC 264 , a selective agonist of CCK B receptors , on morphine dependent rats . ^^^ Rats were made dependent to morphine and the ability of cholecystokinin octapeptide ( CCK 8 ) and Tyr ( SO3H ) gNle mGly Trp ( NMe ) Nle Asp Phe NH 2 ( BC 264 ) , a selective agonist of CCK B receptors , to induce signs of morphine withdrawal after ICV injection was tested . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| L 365 , 260 ( [ 3R ( + ) 2 , 3 dihydro 1 methyl 2 oxo 5 phenyl 1H 1 , 4 benzodiazepine 3 yl ] N ' [ 3 methyl phenyl ] urea ) , a CCK B antagonist , also decreased ceruletide induced protection . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B antagonists inhibit the activity of brain dopamine neurons . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The effects of intracerebroventricular administration of the cholecystokinin ( CCK ) analogue , BDNL , and the selective CCK B agonist , BC 264 , were determined using the hot plate test in mice . ^^^ In contrast , the selective CCK B agonist BC 264 produced , at one dose ( 2 . 5 nmol ) , a slight decrease in the lick latency that was only antagonized by the CCK B antagonist . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Temporal expression of the gastrin ( CCK B ) receptor during azaserine induced pancreatic carcinogenesis . ^^^ Cholecystokinin ( CCK A ) and gastrin ( CCK B ) receptors have been demonstrated in the azaserine induced rat pancreatic carcinoma DSL 6 . ^^^ In order to determine at what stage in azaserine induced pancreatic carcinogenesis gastrin ( CCK B ) receptors are first expressed , we examined the binding of [ 125I ] gastrin 1 to normal rat pancreas , azaserine induced premalignant pancreatic nodules , grossly normal internodular pancreas , and DSL 6 carcinoma . ^^^ We observed that specific gastrin binding was absent in normal pancreas , premalignant nodules , and internodular pancreas , and also reconfirmed our previous report of marked overexpression of gastrin ( CCK B ) receptors in the DSL 6 carcinoma . ^^^ Therefore , we conclude that the presence of gastrin ( CCK B ) receptors in the azaserine induced pancreatic carcinoma DSL 6 , in contrast to their absence in premalignant nodules , suggests that the expression of the gastrin ( CCK B ) receptor may be important in the transformation from premalignant nodules to pancreatic cancer . . ^^^ |
|
| Interacting proteins: P32239 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 ) . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ In contrast , the selective CCK B agonist [ ( 2R , 3S ) beta MePhe 28 , N MeNle 31 ] CCK 26 33 had no effect . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Association of the peptidase inhibitor RB 101 and a CCK B antagonist strongly enhances antinociceptive responses . ^^^ This has been definitely demonstrated in this study by co administration of the CCK B selective antagonist L 365 , 260 with RB 101 , a systemically active inhibitor of peptidases , which fully protects the endogenous opioids , the enkephalins , from their inactivation . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ These data suggest that in the substantia nigra there may be a tonic level of CCK release that , through actions on CCK B receptors , may modulate DA agonist induced inhibition of DA neuronal activity . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In the present study , three structural analogs of LY 262691 with high selectivity for CCK B receptors , LY 262684 , LY 191009 and LY 242040 , also decreased the number of spontaneously active A 10 DA cells . ^^^ L 365 , 260 , a benzodiazepine CCK B antagonist , also decreased 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 . ^^^ CCK B antagonists may therefore represent a novel class of antipsychotic drugs . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B agonists stimulated calcium mobilization in a dose dependent manner in T cells . ^^^ CCK B antagonists suppressed CCK 4 induced calcium mobilization more potently than CCK A antagonist . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Recently , we have demonstrated that the human brain CCK B receptors are identical to the gastrin receptors derived from the stomach mucosa , and that the brain gut peptides , CCK 8 and gastrin 1 are mitogenic for mouse NIH 3T3 fibroblasts expressing human CCK B / gastrin receptors ( N hCCKBR ) . ^^^ In this report , we evaluated the antiproliferative potency of CCK B / gastrin receptor antagonists by using N hCCKBR cells . ^^^ Interestingly , a potent antagonist for rat CCK B / gastrin receptors did not have such activities in N hCCKBR cells . ^^^ These results suggest that YM 022 could intervene in the autocrine stimulation of human tumor cell lines through CCK B / gastrin receptors . ^^^ N hCCKBR cells are an excellent tool to screen for novel human CCK B / gastrin receptor antagonists possessing antiproliferative activity for human cancer cells . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| In morphine tolerant rats , addition of the CCK B receptors antagonist CI 988 or the NMDA receptor blocker dextromethorphan enhanced the antinociceptive effect of morphine on the hot plate test . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| It has recently been demonstrated that L 365 , 260 , a CCK B antagonist in mammals , causes an increase in food intake in chickens . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The influence of guanyl nucleotide on agonist and antagonist affinity at guinea pig CCK B / gastrin receptors : binding studies using [ 3H ] PD 140376 . ^^^ These data are consistent with the notion that the receptor sites in brain and gastric glands , which recognise CCK and gastrin related compounds , are the same and of the CCK B / gastrin subtype . ^^^ These findings may explain previously reported differences between gastrin and CCK B receptors that were based upon binding studies using agonist ligands . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The in vivo release of the selective CCK B agonist pBC 264 ( associated with a tracer dose of [ 3H ] pBC 264 ) from microspheres prepared with OVA was very fast ( 92 % after 6 h ) , whereas only 26 % ( 88 pmol ) of pBC 264 was released from the formulation with Pluronic F 68 after 24 h . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Association of enkephalin catabolism inhibitors and CCK B antagonists : a potential use in the management of pain and opioid addiction . ^^^ 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 . ^^^ Recently the existence of regulatory mechanisms between both systems have been proposed , and the physiological antagonism between CCK and endogenous opioid systems has been definitely demonstrated by coadministration of CCK B selective antagonists with RB 101 , a systemically active inhibitor , which fully protects enkephalins from their degradation . ^^^ This article will review the experimental pharmacology of association of enkephalin degrading enzyme inhibitors and CCK B antagonists to demonstrate the interest of these molecules in the management of both pain and opioid addiction . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| These results suggest that the disruption of the MMC mediated by CCK is due to stimulation of peripheral CCK B receptors located in vagal afferent fibers . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Upregulation of ECL function is determined by activation of CCK B receptors , by gastrin , and by activation of beta adrenergic receptors , as well as by acetylcholine in some ( 10 29 % ) of the cells . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ RESULTS : High concentrations of CCK B gastrin receptors were detected in the midglandular region of the human 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) A and CCK B / gastrin receptors in human tumors . ^^^ Cholecystokinin ( CCK ) A and CCK B / gastrin receptors were evaluated with in vitro receptor autoradiography in 406 human tumors of various origins using a sulfated 125I labeled CCK decapeptide analogue 125I ( D Tyr Gly , Nle 28 , 3l ) CCK 26 33 and 125I labeled Leu 15 gastrin as radioligands . ^^^ CCK B / gastrin receptors were found frequently in medullary thyroid carcinomas ( 92 % ) , in small cell lung cancers ( 57 % ) , in astrocytomas ( 65 % ) , and in stromal ovarian cancers ( 100 % ) . ^^^ 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The results confirmed and extended previous behavioural data indicating that blockade of CCK B receptors potentiated antinociception elicited by endogenous opioids protected from enzymatic degradation . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Subcutaneous injection of the CCK agonist caerulein dose dependently decreased food intake in Zucker obese and lean rats whereas the CCK B agonist gastrin 17 did not . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The novel atypical antipsychotic olanzapine , but not the CCK B antagonist LY 288513 , blocks apomorphine induced disruption of pre pulse inhibition . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptors , present in control pancreata , were not detected in any of the pancreatic cancers . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Role of gastrin / CCK B receptors in meal stimulated acid secretion in rats . ^^^ Basal and stimulated acid outputs and portal venous plasma gastrin , histamine , and somatostatin concentrations were measured before and after close arterial injection of a new , relatively selective , gastrin / CCK B receptor antagonist GR143330X . ^^^ Furthermore , we show for the first time in an intact , in vivo , anesthetized rat model that meal stimulated activation of gastrin / CCK B receptors stimulates acid secretion in part by regulating the release of histamine and somatostatin . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Selective activation of CCK B receptors does not induce sleep and does not affect EEG slow wave activity and brain temperature in rats . ^^^ 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 . ^^^ In the present experiments , we studied the effects of the selective activation of CCK B receptors by CCK tetrapeptide ( CCK 4 ) or nonsulfated CCK 8 ( CCK 8 NS ) on sleep and brain temperature ( Tbr ) . ^^^ These results suggest that the activation of CCK B receptors by systemic injection of CCK 4 or CCK 8 NS is not sufficient to elicit increased NREMS and hypothermia in rats . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK induced depolarization was significantly reduced by a CCK A , but not a CCK B , receptor antagonist . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Expression of CCK B receptors was detected in all tissues arising from pancreas and in most extrapancreatic tissues and tumors . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ 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 . . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CCK B receptors in the limbic system modulate the antidepressant like effects induced by endogenous enkephalins . ^^^ Systemic administration of RB 101 , a complete inhibitor of enkephalin catabolism , has been reported to induce antidepressant like responses in mice which were potentiated by an ineffective dose of a CCK B antagonist . ^^^ The aim of this study was to investigate the neuroanatomical substrate involved in the facilitatory effects induced by CCK B antagonists on RB 101 behavioural responses . ^^^ Thus , the CCK B antagonist PD 134 , 308 was locally administered into different brain structures ( anterior nucleus accumbens , central amygdala and caudate nucleus ) and its effects on the antidepressant like response induced by systemic administration of RB 101 were evaluated in the conditioned suppression of motility ( CSM ) test in rats . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 ) . ^^^ 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 . ^^^ |
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| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Furthermore , antagonists of CCK B receptors , which are found most frequently in the brain , inhibit the activity of brain dopamine neurons . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| All the compounds were evaluated in vitro towards both CCK B and CCK A receptors . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK B antagonists L 365 , 260 and PD 134 , 308 decreased and completely blocked ( respectively ) the place aversion induced by naloxone in morphine dependent animals whereas BC 264 and devazepide were inactive in this model . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ Biodistribution studies in mice showed very low brain uptakes ( < 0 . 8 % dose / gram ) of the radioactivities after intravenous injections of these compounds , although that of brain CCK B receptor selective [ 11C ] L 365 , 260 was 2 fold that of [ 11C ] L 365 , 346 . ^^^ Owing to the very low brain permeability , however , [ 11C ] L 365 , 260 may have no potential as a PET tracer for probing brain CCK B receptors . . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ Furthermore , several selective CCK B agonists produce anxiogenic like effects , while CCK B antagonists induce anxiolytic like responses in several models of anxiety . ^^^ However , BC 264 a highly selective CCK B agonist , does not produce anxiogenic like effects but increases attention and / or memory . ^^^ Together with biochemical data , this led to the hypothesis of the existence of two CCK B binding sites , CCK B 1 and CCK B 2 , which could correspond to different activation states of a single molecular entity . ^^^ Investigations into CCK B 1 and CCK B 2 systems might be of critical interest , since only one site , CCK B 1 , appears to be responsible for the effects of anxiety . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 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 . ^^^ 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
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| Interacting proteins: P32239 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 . ^^^ |
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| Interacting proteins: P32239 and P06307 |
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 . ^^^ |
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| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Dai , Novel gastrin receptors mediate mitogenic effects of gastrin and processing intermediates of gastrin on Swiss 3T3 fibroblasts : Absence of detectable cholecystokinin ( CCK ) A and CCK B receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Excitatory responses to CCK 8 are due to stimulation of preganglionic receptors while inhibitory responses are NO mediated through stimulation of postganglionic CCK B receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The involvement in memory processes of the neuropeptide cholecystokinin ( CCK ) through its interaction with the CCK B receptors was studied . ^^^ The improving effect of a selective CCK B agonist , BC 264 , intraperitoneally administered ( 0 . 3 microgram / kg ) in the retrieval phase of the task ( 6 hr time interval ) , was also observed after its injection ( 1 pmol / 0 . 5 microliter ) in the dorsal subiculum / CA1 of the hippocampus but not in the caudate / putamen nucleus or in the prefrontal cortex of rats . ^^^ The CCK B antagonist L 365 , 260 injected ( 10 ng / 0 . 5 microliter ) into this region of the hippocampus abolished the improving effect of BC 264 injected intraperitoneally . ^^^ Finally , CCK B receptor deficient mice have an impairment of performance in the memory task ( 2 hr time interval ) . ^^^ Together , these results support the physiological involvement of the CCKergic system through its interaction with CCK B receptors in the hippocampus to improve performance of rodents in the spatial recognition memory test . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Also , CCK B receptors have been found in some human pancreatic cancers . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Dose response of adrenocorticotropin and cortisol to the CCK B agonist pentagastrin . ^^^ To explore this hypothesis , we examined the effects of varying doses ( 0 to 0 . 8 microgram / kg ) of the CCK B agonist pentagastrin on adrenocorticotropin ( ACTH ) and cortisol release in healthy human subjects . ^^^ The HPA axis response to the CCK B agonist pentagastrin may be a direct pharmacological effect . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Placebo controlled trial of the CCK B antagonist , CI 988 , in panic disorder . ^^^ Selective antagonists of CCK B receptors can block the challenge induced symptoms in a dose dependent manner , leading to the hypothesis that these compounds may have anxiolytic effects . ^^^ METHODS : A randomized , double blind study was carried out to compare the effects of placebo with CI 988 , a selective antagonist of the CCK B receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| BACKGROUND & AIMS : Two distinct receptors , cholecystokinin ( CCK ) A and CCK B , mediate CCK effects in the digestive system . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The serendipitously discovered panicogenic effect of the cholecystokinin fragment , the C terminal tetrapeptide amide ( CCK 4 ) , has suggested that the widespread network of CCK neurons and corresponding CCK B receptors in the brain are in some way involved in pathogenesis panic disorders in man . ^^^ This review focuses on three immediate questions . ( 1 ) Does endogenous CCK 4 exist . ( 2 ) Is the panicogenic effect mediated only through CCK B receptors . ( 3 ) Are measurements of CCK peptides in cerebrospinal fluid of use in elucidating the pathogenesis and / or diagnosis . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ In bovine species , as in human , the pancreas predominantly expresses cholecystokinin B ( CCK B ) / gastrin receptors . ^^^ 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 participation of CCK B / gastrin receptors in this regulation was not demonstrated . . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We have previously shown in a rat model of central neuropathic pain after spinal cord injury that blockade of CCK B receptors lead to marked pain relief . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
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 . ^^^ CCK B / gastrin receptor mRNA and protein were detected in parietal cells ( 57 . 4+ / 11 . 1 % ) and in neuroendocrine cells ( 33 . 2+ / 4 . 4 % ) expressing chromogranin A . ^^^ Furthermore , epithelial cells within the neck of the gastric gland were found to express the CCK B / gastrin receptor . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ QSAR studies verify that CCK B receptors are closely related structurally to gastrin receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The CCK receptors can be pharmacologically subdivided into two subtypes : CCK A and CCK B . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| This effect is mediated by postsynaptic CCK B receptors and is attributable to potentiation of the A current . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The substituents of the 1 , 4 benzodiazepine scaffold have been varied in the 3 , 5 , 7 , and 8 positions and the combinatorial library was evaluated in a chole cys to kinin ( CCK ) radioligand binding assay . 3 Alkylated 1 , 4 benzodiazepines with selectivity towards the CCK B ( CCK 2 ) receptor have been optimized on the lipophilic side chain , the ketone moiety , and the stereochemistry at the 3 position . ^^^ Various novel 3 alkylated compounds were synthesized and [ S ] 3 propyl 5 phenyl 1 , 4 benzodiazepin 2 one , [ S ] NV A , has shown a CCK B selective binding at about 180 nM . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| We hypothesized that circulating concentrations of endogenous CCK 4 and / or CCK 8 are increased in later life , possibly due to decreased enzymatic degradation , and that this is associated with desensitization of CCK B receptors . ^^^ The two groups were compared on fasting basal plasma concentrations of CCK 4 , sulfated CCK 8 ( CCK 8s ) and nonsulfated CCK 8 ( CCK 8 ns ) , and on binding capacity of lymphocyte CCK B receptors . ^^^ Compared with younger subjects , older subjects had a significantly higher basal plasma concentration of CCK 8s and significantly diminished binding capacity of CCK B receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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 . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| BACKGROUND AND AIMS : Both cholecystokinin ( CCK ) A and CCK B receptors are expressed in the pancreas , and exogenous gastrin administration stimulates glucagon secretion from human islets . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Thus , bi daily antalarmin treatment ( 20 mg / kg ip ) induced a significant increase in CCK B receptor binding density throughout the neuraxis , indicative of either a global increase in receptor number or an increase in receptor affinity . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Two distinct activity labels can have a significant similarity for a number of reasons : two activities can be nearly synonymous ( e . g . , CCK B antagonist vs Gastrin antagonist ) , one activity may be a subset of another ( e . g . , Dopamine ( D 2 ) agonist vs Dopamine agonist ) , or an activity can be the mechanism by which another activity works ( e . g . , ACE inhibitor vs Antihypertensive ) , etc . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Quantitative RT PCR was used to validate the results and demonstrated that there were predictable increases of three GPCRs selected for this analysis , including the dopamine D 4 , alpha 1b , and CCK B receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| CONCLUSIONS : Pancreatic enzyme secretion due to CCK 33 stimulation depends on the presence of short duodenal pancreatic peptidergic reflexes evoked mainly via low sensitive , probably CCK B , receptors located in the duodenum / stomach . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Conversely , higher levels of stress can inhibit motivated behaviour , and evidence is presented that this may occur in part through the effects of the neuropeptide cholecystokinin ( CCK ) , acting through CCK B receptors in the nucleus accumbens . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Blockade of CCK B receptors with intraperitoneal L 365 , 260 ( 25 mg / kg ) reversed bombesin induced gastroprotection . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Cholecystokinin ( CCK ) has been shown to be implicated in panic attacks which can be induced by agonists at the CCK B subtype . ^^^ CCK B antagonists are thus potential antipanic agents although this has not yet been confirmed by clinical trials . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| METHODS : Receptors of bombesin 3 , cholecystokinin ( CCK ) A , CCK B , glucagon like peptide ( GLP ) 1 , melanin concentrating hormone ( MCH ) 1 , orexin 1 , orexin 2 , neuromedin B , neuropeptide Y ( NPY ) 1 and NPY 5 , neurotensin ( NT ) 1 , NT 2 , NT 3 , and leptin receptor long form mRNA in GT 1 7 cells were detected by reversed transcriptase polymerase chain reaction . ^^^ RESULTS : Receptors of bombesin 3 , CCK B , GLP 1 , MCH 1 , orexin 1 , neuromedin B , NPY 1 , NPY 5 , NT 1 , NT 3 , and leptin receptor long form mRNA were expressed in GT 1 7 cells , of which , receptors of GLP 1 , neuromedin B , NPY 1 , and NT 3 were highly expressed . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The respective receptors of these peptides , NK 3 , CCK B , and CRF 1 , were essentially expressed in pyramidal cells . ^^^ Neuropeptide effects were prevented by selective antagonists of NK 3 , CCK B , and CRF 1 receptors . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Conversely , pretreatment with the selective CCK B antagonist triglumide did not attenuate the CCK8s induced inward current ; pretreatment with triglumide ( 3 microM ) and lorglumide ( 1 microM ) attenuated the CCK8s induced current to the same extent as pretreatment with lorglumide alone . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The stimulatory effect of CCK on meningioma cell growth was completely abolished by a CCK B specific receptor antagonist , L 365 , 260 . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Since CCK can function as a satiety factor when administered to rodents , localization of Cckbr near the tub mutation identifies this receptor as a possible candidate gene for this obesity mutation . . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 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 . ^^^ Using site directed mutagenesis in this segment of the CCKBR , we identified a sequence of 5 amino acids in the second extracellular loop responsible for this 100 fold selective loss in gastrin affinity . 125I labeled Bolton Hunter CCK 8 binding displacement by L 365 , 260 ( a CCKBR selective antagonist ) was unaffected by the changes in these 5 amino acids . ^^^ |
|
| Interacting proteins: P32239 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 . ^^^ Both CCK and CCK B receptors are widely distributed in the hippocampal formation , but the functions of CCK there have been poorly understood . ^^^ Our results indicate that activation of CCK B receptors initially and transiently increased spontaneous IPSC ( sIPSC ) frequency , followed by a persistent reduction . ^^^ The effects of CCK were independent of the functions of phospholipase C , intracellular Ca ( 2+ ) release , protein kinase C or phospholipase A ( 2 ) , suggesting a direct coupling between the G proteins of CCK B receptors and 1 ( K ( Ca ) ) . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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 . ^^^ CCK 8 stimulated total inositol phosphate accumulation in COS 1 cells transiently expressing the CCKBR H207F with full efficacy and a 3044 fold reduced potency , which suggests that the loss of radioligand binding was caused by a loss in affinity . ^^^ 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Displacement experiments using [ 125I ] BH CCK and various agonists and antagonists identified binding sites with typical CCKBR pharmacology . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The mutated receptor displayed similar expression levels and high affinity CCK binding compared with the wild type CCKBR . ^^^ |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| The results suggest that CCK 45C > T and CCKBR Val125Ile polymorphisms do not have a major role in alcohol dependence in the population studied . ^^^ |
|
| Interacting proteins: P32239 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: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| Genomic DNA was analyzed for CCK , CCKAR , and CCKBR ( cholecystokinin B receptor ) polymorphisms by polymerase chain reaction . ^^^ |
|
| Interacting proteins: P32239 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: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P32239 and P06307 |
Pubmed |
SVM Score :0.0 |
| NA |
|