Pubmed abstracts for Protein-Protein Interaction search result :

Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
This rotationally restricted phenolic analogue of RU 24 , 969 is a potent ( 15 nM ) and selective ( 200x vs the 5 HT1A receptor , 150x vs the 5HT1D receptor ) functional agonist for the 5 HT1B receptor . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These 5 HT 1 like receptors resemble both cloned 5 HT1D receptor subtypes , 5 HT1D alpha and 5 HT 1D beta . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Ketanserin at a concentration which should block the 5 HT 1D alpha but not the 5 HT 1D beta receptor failed to antagonize the inhibitory effect of 5 carboxamidotryptamine . ^^^ In contrast , the nonselective 5 HT 1D alpha / 1D beta receptor antagonist , methiothepin , at a concentration which should block both the 5 HT 1D alpha and the 5 HT 1D beta receptor abolished the effect of 5 carboxamidotryptamine . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
When given alone , neither the selective 5 HT 1B antagonist isamoltane ( 1 microM ) nor the 5 HT 1D / B antagonist GR 127935 ( 50 nM ) , affected 5 HT efflux or uptake under this stimulation paradigm . ^^^ Furthermore , these data show that 5 HT 1B and possibly 5 HT 1D antagonists block this inhibitory autoreceptor tone and may thus be a useful addition to SSRI treatment in the clinic . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
No significant binding ( Ki greater than 10 mumol / l ) of DAU 6285 to serotonergic 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , and 5 HT 2 receptors as well as to adrenergic alpha 1 , alpha 2 , dopaminergic D 1 , D 2 or muscarinic M 1 M3 receptor subtypes was found . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The effect of metergoline ( 1 mg . kg 1 ) , a substance with a very high affinity for the 5 HT1D receptor as well as for the 5 HT1A , 5 HT1B , 5 HT1C and 5 HT 2 receptors , was studied on the responses to 5 HT and sumatriptan . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
HT 1B / D receptor antagonists . 1 . 5 Hydroxytryptamine 1B ( 5 HT 1B , formerly designated 5 HT 1D beta ) and 5 hydroxy tryptamine 1D ( 5 HT 1D , formerly designated 5 HT 1D alpha ) receptors are distinct molecular entities that mediate serotonergic neurotransmission . ^^^ Few if any ligands show selectivity for 5 HT 1B or 5 HT 1D receptors or both . ^^^ To find out whether the available so called 5 HT 1B / D receptor antagonists are indeed antagonists and not partial agonists , efficacy was measured at recombinant human 5 HT 1B and 5 HT 1D receptor sites by using a [ 35S ] GTP gamma S binding assay to membrane preparations of stably transfected rat C 6 glial cell lines . ^^^ Metergoline and the selective 5 HT 1B / D receptor ligands GR 127935 as well as GR 125743 showed significant intrinsic activity ( 43 % to 69 % ) at the 5 HT 1D receptor subtype , whereas the nonselective ligand 1 naphthylpiperazine yielded less ( 15 % to 19 % ) intrinsic activity at both receptor subtypes . ^^^ Future work should be directed toward the identification of selective 5 HT 1B and 5 HT 1D receptor ligands that display either neutral antagonist or inverse agonist properties to evaluate the therapeutic potential of 5 HT 1B / D receptor blockade . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In the current study , we examined arterial smooth muscle for the presence of serotonin ( 5 hydroxytryptamine , 5 HT ) 5 HT 1B , 5 HT 1D , 5 HT 1F , 5 HT 2A , 5 HT 2B , and 5 HT 7 receptor mRNA and hypothesized that , if present , activation of these receptors would stimulate the extracellular signal regulated kinase ( Erk ) MAPK pathway and an Erk MAPK dependent contraction . ^^^ RT PCR analyses of rat aortic smooth muscle cells , cultured and fresh , indicated the presence of 5 HT 1B , 5 HT 1D , 5 HT 1F , 5 HT 2A , 5 HT 2B , and 5 HT 7 receptor mRNA . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In contrast , DV 7028 had no affinity for 5 HT1A , 5 HT1B and 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Molecular cloning and functional characterization of a human 5 HT1B serotonin receptor : a homologue of the rat 5 HT1B receptor with 5 HT1D like pharmacological specificity . ^^^ Instead , human 5 HT1B drug specificity is highly similar to that of the human 5 HT1D receptor , with which it shares 59 % amino acid sequence identity . ^^^ The human 5 HT1B receptor , like the 5 HT1D receptor , can couple to Gi proteins . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Radioligand binding studies were performed in membranes of rabbit whole brain and striatum using the novel iodinated radioligand for 5 hydroxytryptamine 5 HT1B and 5 HT1D sites , Serotonin 5 O Carboxymethyl Glycyl [ 125I ] Tyrosinamide ( [ 125I ] GTI ) . [ 125I ] GTI labelled a finite number of high affinity sites in rabbit brain membranes , Bmax = 191 + / 47 fmol / mg protein , pKD ( log mol / l ) = 8 . 50 + / 0 . 13 , n = 5 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The present study was aimed at characterizing this receptor with respect to the currently recognized 5 HT 1 receptor subtypes ( 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Competition binding experiments using compounds that are selective for various 5 HT receptor subtypes showed the highest correlation with a 5 HT1D like receptor ( r = 0 . 89 ) and a low correlation with 5 HT1B like receptors . ^^^ Therefore , despite the close genetic relationship between RH 2 and the rat 5 HT1B receptor , our results indicate that the receptor encoded by RH 2 2 is best classified as a human 5 HT1D receptor subtype and defines a second member of the human 5 HT1D receptor family . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT 2 receptor displayed a genomic organization quite different from the 5 HT1A , 5 HT1B and 5 HT1D receptor subtypes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These data were compared to those found under similar conditions in the brain of rats and guinea pigs , species which are known to possess 5 HT1B and 5 HT1D receptors , respectively . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Radioligand binding studies were performed in membranes of calf caudate , guinea pig cortex , dog caudate and whole brain , monkey caudate and whole brain , and human caudate using the novel iodinated radioligand , Serotonin 5 O Carboxymethyl Glycyl [ 125I ] Tyrosinamide ( abbreviated [ 125I ] GTI for the sake of simplicity ) , a ligand known to label 5 HT1B and 5 HT1D sites . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Recently a human receptor gene was isolated ( designated 5 HT1B receptor , 5 HT1D beta receptor , or S 12 receptor ) which shares 93 % identity of the deduced protein sequence with rodent 5 HT1B receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Conversion of the human 5 HT1D beta serotonin receptor to the rat 5 HT1B ligand binding phenotype by Thr355Asn site directed mutagenesis . ^^^ The human 5 HT1D beta serotonin receptor and its rat homolog ( also called the 5 HT1B receptor ) share 93 % amino acid identity , yet display markedly different pharmacological specificities . ^^^ We now report that Thr355Asn mutagenesis of the human 5 HT1D beta receptor alters the binding characteristics of the recombinant receptor in [ 3H ] 5 HT binding assays to a profile very similar to that of the rat 5 HT1B binding site . ^^^ These results confirm that this single amino acid difference is responsible for the majority of the known pharmacological discrepancies between human and rat observed for 5 HT1D beta ( 5 HT1B ) receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Furthermore , SR 46349B displayed moderate affinity for the 5 HT1C receptor and had no affinity for the other 5 HT 1 subclass ( 5 HT1A , 5 HT1B or 5 HT1D ) , dopamine ( D 1 or D 2 ) , `` alpha ' ' adrenergic ( alpha 1 or alpha 2 ) , sodium and calcium channel and histamine ( H 1 ) receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These data suggest that the 5 HT induced increase in intragastric pressure in the spinal and bilaterally vagotomized rat is mediated by an atypical 5 HT 1 like receptor , which , based on the low agonist potency of 5 carboxamidotryptamine and RU 24969 and the resistance to blockade by metergoline , does not seem to correspond to either the 5 HT1A , 5 HT1B , 5 HT1C or the 5 HT1D receptor subtypes . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
No 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 , or 5 HT uptake sites were found in any of the tumors , although all were detected in human or rat brain . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In addition , controversy has been raging for several years over the classification of 5 HT1B receptors ( found only in rat brain ) and 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The deduced amino acid sequence of HGCR 1 is 39 % , 55 % and 87 % identical to that for the human 5 HT1A , the human 5 HT1D and the rat 5 HT1B receptor , respectively . [ 3H ] 5 HT binding to transfected COS 7 cell membranes yields a pharmacological profile similar to that of 5 HT1B receptor . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
At least seven receptor subtypes ( 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 , 5 HT 3 , 5 HT 4 ) have been identified in brain . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Interaction of the alpha adrenoceptor agonist oxymetazoline with serotonin 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D receptors . ^^^ Oxymetazoline was recognized with nanomolar affinity by 5 HT1A , 5 HT1B and 5 HT1D binding sites and mimicked the effects of 5 hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests . ^^^ Thus , oxymetazoline is a full and potent agonist at 5 HT1A , 5 HT1B and 5 HT1D receptors and a partial agonist at 5 HT1C receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In addition , the drugs with antagonistic properties at the 5 HT1A , 5 HT1B , 5 HT1C , and 5 HT1D receptors block other 5 HT receptors or even entirely different receptors ( e . g . , beta adrenoceptors ) ; as a rule , they do not discriminate between the four 5 HT receptor subtypes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The relationship between the serotonin 5 hydroxytryptamine1B ( 5 HT1B ) and 5 HT1D receptors has been the topic of much investigation and speculation since their complementary species distribution was first appreciated . ^^^ The pharmacological profile of this binding site closely matched that of the native rat 5 HT1B receptor ( r = 0 . 95 ) but not the 5 HT1D receptor ( r = 0 . 07 ) . ^^^ These data indicate that , although the 5 HT1B and 5 HT1D receptors are pharmacologically distinct , they are species variants of the same receptor gene , the 5 HT1D beta gene . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Biochemical and pharmacological characterization of serotonin O carboxymethylglycyl [ 125I ] iodotyrosinamide , a new radioiodinated probe for 5 HT1B and 5 HT1D binding sites . ^^^ There is a lack of radioactive probes , particularly radioiodinated probes , for the direct labeling of serotonin 1B ( 5 HT1B ) and serotonin 1D ( 5 HT1D ) binding sites . ^^^ Binding is heterogeneous , paralleling the anatomical distribution of 5 HT1B sites in the rat and of 5 HT1D sites in the guinea pig . ^^^ S CM G [ 125I ] TNH 2 is then a useful new probe for the direct study of 5 HT1B and 5 HT1D binding sites . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
This new ligand is therefore highly specific for 5 HT1B and 5 HT1D binding sites and can be used to further characterize the involvement of these subtypes in physiological studies focusing particularly on behavioral effects . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
At this time , there is a general consensus that the 5 HT 1 family can be further subdivided into 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , and 5 HT1P subpopulations . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The inhibitory effect of TFMPP was mimicked by CGS 12066B ( 10 , 30 , and 100 microM ) , a 5 hydroxytryptamine1B ( 5 HT1B ) / 5 HT1D receptor agonist ; 1 ( m chlorophenyl ) piperazine ( 100 microM ) , a 5 HT1C / 5 HT1B receptor agonist ; and 5 carboxamidotryptamine ( 10 microM ) , a nonselective 5 HT 1 receptor agonist . 8 Hydroxy 2 ( di n propylamino ) tetralin ( 10 and 100 microM ) , a 5 HT1A receptor agonist , and quipazine ( 10 and 100 microM ) , a 5 HT 2 receptor agonist , did not have any significant effect . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Good correlations were found between species in the regional distribution of 5 HT 1 sites labelled with [ 3H ] 5 HT ( r = 0 . 73 ) , 5 HT1A sites labelled with [ 3H ] 8 OH DPAT ( r = 0 . 87 ) , and 5 HT1B versus 5 HT1D sites labelled with [ 3H ] 5 HT in the presence of ipsapirone and DOI ( r = 0 . 76 ) . ^^^ Areas almost exclusively containing 5 HT1B or 5 HT1D sites , such as the ventral pallidum , globus pallidus and substantia nigra , expressed markedly more [ 3H ] 5 HT binding in rat as compared to guinea pig , while the opposite occurred in claustrum , dorsal endopiriform nucleus , lateral geniculate nucleus , and superficial grey layer of the superior colliculus . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Species differences in presynaptic serotonin autoreceptors : mainly 5 HT1B but possibly in addition 5 HT1D in the rat , 5 HT1D in the rabbit and guinea pig brain cortex . ^^^ The serotonin axons of rat brain cortex may possess 5 HT1D in addition to 5 HT1B autoreceptors . ( ABSTRACT TRUNCATED AT 400 WORDS ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In the rat vena cava , they are of the 5 HT1B subtype , in the pig coronary artery they belong to a novel , so far unknown class of 5 HT receptors , and in the human saphenous vein they could be classified as 5 HT1D . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
A correlation analysis performed between the agonists vascular potency ( pD 2 values ) and their affinities ( pKD values ) published at various subtypes of 5 HT binding sites showed a positive significant correlation with rat cortical 5 HT1B ( r = 0 . 86 ; P less than 0 . 01 ) and human caudate 5 HT1D ( r = 0 . 98 ; P less than 0 . 005 ) subtypes . 4 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Constriction of porcine arteriovenous anastomoses by indorenate is unrelated to 5 HT1A , 5 HT1B , 5 HT1C or 5 HT1D receptor subtypes . ^^^ These effects of indorenate were not appreciably modified after treatment with the 5 HT 2 receptor antagonist ketanserin ( 0 . 5 mg . kg 1 i . a . ) , but were markedly reduced after treatment with methiothepin ( 1 . 0 mg . kg 1 i . a . ) , which antagonizes not only 5 HT 2 receptors , but also the putative 5 HT1A , 5 HT1B 5 HT1C and 5 HT1D subtypes of 5 HT 1 like receptors . ^^^ It is therefore concluded that , like 8 hydroxy 2 ( di n propylamino ) tetralin ( 8 OH DPAT ) and 5 methoxy 3 ( 1 , 2 , 3 , 6 tetrahydro 4 pyridinyl ) 1H indole ( RU 24969 ) , indorenate reduces both total common carotid and cephalic arteriovenous anastomotic blood flow in the pig by stimulating 5 HT 1 like receptors ; these receptors , however , do not seem to correspond to either 5 HT1A , 5 HT1B , 5 HT1C or 5 HT1D binding sites . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT 1 receptor family comprises five different pharmacologic subtypes , designated 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , and 5 HT1E , whose common property is to bind 5 HT with nanomolar affinity . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Calculated ID 50 values correlated significantly with reported affinities ( r = 0 . 81 , n = 10 , P less than 0 . 01 ) for 5 HT1C but not for 5 HT 2 , 5 HT1A , 5 HT1B or 5 HT1D receptors . 2 . ^^^ ID 50 values of the ten antagonists against 5 hydroxytryptophan ( 5 HTP ) + carbidopa induced head shakes ( a 5 HT 2 mediated response ) correlated significantly ( r = 0 . 81 , n = 10 , P less than 0 . 01 ) with their affinities for 5 HT 2 but not for 5 HT1A , 5 HT1B , 5 HT1C or 5 HT1D receptors . 3 . ^^^ These ratios correlated highly significantly ( r = 0 . 91 , n = 10 , P less than 0 . 001 ) with the ratios of the affinities of the drugs for 5 HT1C ( but not for 5 HT1A , 5 HT1B or 5 HT1B or 5 HT1D receptors ) and with their affinities for 5 HT 2 receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Synthesis and pharmacological study of radioiodinated serotonin derivative specific of 5 HT1B and 5 HT1D binding sites of the central nervous system ] . ^^^ Quantitative autoradiographic studies on rat and guinea pig brain sections incubated with 2 nM [ 3H ] 5 HT showed a preferential affinity of S CM GTNH 2 for 5 HT1B and 5 HT1D sites . ^^^ Autoradiograms from brain sections incubated with 0 . 02 nM S CM G [ 125I ] TNH 2 showed a heterogeneous anatomical distribution of the labelling with high densities in regions rich in 5 HT1B or 5 HT1D binding sites , and with no labelling of those rich in 5 HT1A or 5 HT1C sites . ^^^ The pharmacological profiles of the binding sites corresponded to those of 5 HT1B and 5 HT1D receptor subtypes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
They belong to the 5 HT1B receptor subclass in the rat and to the 5 HT1D subclass in the pig , guinea pig , and probably man . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT 1 sites have been further divided into 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D and 5 HT1E sites . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Whereas tryptamine derivatives generally display little selectivity for the various populations of 5 HT receptors , N 1 n propyl 5 methoxy alpha methyltryptamine ( 3h ) binds with significant affinity ( Ki = 12 nM ) and selectivity at 5 HT 2 receptors relative to 5 HT1A ( Ki = 7100 nM ) , 5 HT1B ( Ki = 5000 nM ) , 5 HT1C ( Ki = 120 nM ) , and 5 HT1D ( Ki greater than 10 , 000 nM ) receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Such data are still missing for 5 HT1D ( and 5 HT1B ) receptors , but will certainly be provided in the next few years . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Furthermore , 5 HT 1 receptors are not a homogeneous class , but are subdivided further into four subtypes : 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Among the most potent antagonists ( mean pKB value ) were the nonselective 5 HT receptor antagonists , methiothepin ( 7 . 30 ) and metergoline ( 6 . 86 ) , the 5 HT1A / 5 HT1D receptor ligand , 1 [ 2 ( 4 amino phenyl ) ethyl ] 4 ( 3 trifluoromethylphenyl ) piperazine ( 7 . 02 ) , the 5 HT1A / 5 HT1B / 5 HT1D receptor ligand , 7 trifluoromethyl 4 ( 4 methyl 1 piperazinyl ) pyrrolo [ 1 , 2 , a ] quinoxaline 1 ( 6 . 73 ) and yohimbine ( 6 . 37 ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Presently , 5 TH receptors have been divided into 5 HT 1 , 5 HT 2 and 5 HT 3 . 5 HT 1 receptors have been subdivided into 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The prejunctional inhibitory receptor has been the most studied ; depending on the tissue , these subtypes may resemble 5 HT1A , 5 HT1B , 5 HT1C or 5 HT1D binding sites , or the contractile receptor in dog saphenous vein . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Nevertheless many of these studies on the 5 HT1B receptor may aid the development of drugs acting at the 5 HT1D site since this receptor has been identified as being the equivalent of the 5 HT1B site in species other than the rat and mouse . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
This communication deals essentially with the biochemical approaches to characterize 5 HT1D receptors , and their comparison with 5 HT1B receptors . ^^^ The methods used include radioligand binding , in vitro autoradiography , and second messenger studies . 5 HT 1 receptor subtypes are labeled with [ 3H ] 5 HT and present a large heterogeneity : no less than 4 subtypes have been characterized : 5 HT1B and 5 HT1D are labeled respectively with [ 125I ] cyanopindolol , and [ 3H ] 5 HT under appropriate conditions . ^^^ In contrast , calf , pig or human 5 HT1D receptors show significantly lower affinities for these drugs . 5 HT1D receptors show high to intermediate affinities to compounds such as PAPP , DP 5 CT , 8 OH DPAT , yohimbine and rauwolscine , whereas 5 HT1B receptors have very low affinities for these compounds . ^^^ The presence of 5 HT1B receptors has been documented convincingly only in rat , mouse and hamster . 5 HT1D receptors have been demonstrated in pigeon , guinea pig , cat , dog , pig , calf , monkey , and man . ^^^ The distribution of 5 HT1B and 5 HT1D receptors in all species examined so far , is very similar : high concentrations of sites are found in the nigro striatal pathway , caudate putamen , globus pallidus and especially substantia nigra . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The potencies of these agonists in inhibiting overflow were significantly correlated with their affinities for 5 HT1B and 5 HT1D binding sites , but not with those for 5 HT1A or 5 HT1C binding sites . 5 Aminotryptamine , methysergide , ipsapirone , cyanopindolol , SDZ 21009 and metergoline dit not produce a significant inhibition . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In view of the appreciable affinity of DP 5 CT for the 5 HT1D receptor subtype , the effects of the mixed 5 HT1B / 5 HT1D receptor agonist 7 trifluoromethyl 4 ( 4 methyl 1 piperazinyl ) pyrrolo ( 1 , 2 a ) quinoxaline ( CGS 12066B ) , and the mixed 5 HT1A / 5 HT1B / 5 HT1D receptor agonist 5 methoxy 3 ( 1 , 2 , 3 , 6 tetrahydropyridine 4 yl ) 1H indole ( RU 24969 ) were also investigated . ^^^ The data suggest that central 5 HT1A receptors , but neither 5 HT1B nor 5 HT1D receptors , regulate plasma adrenaline and glucose levels . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
As previously reported , 2 Me 5 HT possesses a low affinity ( Ki greater than 500 nM ) for 5 HT1A , 5 HT1B , 5 HT1C , and 5 HT 2 sites ; this agent also displays a low affinity for 5 HT1D ( Ki = 1220 nM ) and 5 HT1E ( Ki greater than 10 , 000 nM ) sites . ^^^ However , alpha Me 5 HT displays little selectivity for 5 HT1A , 5 HT1B , 5 HT1C , and 5 HT1D sites ( Ki = 42 , 85 , 150 , and 150 nM , respectively ) and a very low affinity for 5 HT1E ( Ki greater than 10 , 000 nM ) sites . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
This binding , which is unlikely to be to the 5 HT1B type , could represent labelling to the 5 HT1D or 5 HT1E sites . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Hydroxytryptamine 5 HT1B and 5 HT1D receptors mediating inhibition of adenylate cyclase activity . ^^^ Pharmacological comparison with special reference to the effects of yohimbine , rauwolscine and some beta adrenoceptor antagonists . 5 Hydroxytryptamine1B ( 5 HT1B ) receptor mediated inhibition of forskolin stimulated adenylate cyclase activity in rat substantia nigra was characterized pharmacologically and compared to 5 HT1D receptor mediated inhibition of forskolin stimulated adenylate cyclase activity in calf substantia nigra . ^^^ Special attention was paid to the effects of drugs known to bind with high affinity to 5 HT1B ( pindolol , propranolol , cyanopindolol , SDZ 21 009 , isamoltane ) or 5 HT1D recognition sites ( yohimbine , rauwolscine ) . pEC 50 or pKB values of a variety of 5 HT receptor ligands ( 6 agonists including 5 HT , and 12 antagonists ) for the inhibition of adenylate cyclase activity in rat substantia nigra , correlated significantly to the corresponding pKD values at 5 HT1B binding sites ( r = 0 . 90 , P = 0 . 0001 ) . ^^^ The rank orders of potency of the tested compounds at 5 HT1B and 5 HT1D were markedly different . ^^^ The results strengthen the identity between 5 HT receptors mediating inhibition of adenylate cyclase activity in rat and calf substantia nigra and 5 HT1B and 5 HT1D binding sites , respectively . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These antagonists covered the whole range of currently defined serotonin receptor types and subtypes : 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 , and 5 HT 3 . 6 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Anorexia is probably induced by interaction with 5 HT1B receptors in the rat ; the human equivalent of this receptor is not known , but the 5 HT1D type is a likely candidate . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Interactions with functional 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D receptors . ^^^ The effects of the compound were investigated in radioligand binding studies and in functional models for 5 HT1A , 5 HT1B , and 5 HT1D receptors ( inhibition of forskolin stimulated adenylate cyclase activity in calf hippocampus , rat and calf substantia nigra , respectively ) and 5 HT1C receptors ( stimulation of inositol phosphate production in pig choroid plexus ) . ^^^ GR 43175 displayed the following order of affinity for 5 HT recognition sites ( pKD values , log mol / l , in parentheses ) : 5 HT1D ( 7 . 54 ) greater than 5 HT1B ( 6 . 35 ) greater than 5 HT1A ( 6 . 13 ) much greater than 5 HT1C ( 4 . 13 ) greater than 5 HT 2 ( 3 . 67 ) . ^^^ The same order of potency was observed at functional 5 HT 1 receptors , at which GR 43175 acted as a full agonist , with the exception of the 5 HT1C receptor , where the compound was a weak antagonist ( pEC 50 or pKB values , log mol / l , in parentheses ) : 5 HT1D ( 6 . 28 ) greater than 5 HT1B ( 6 . 03 ) greater than 5 HT1A ( 5 . 57 ) much greater than 5 HT1C ( 4 . 25 ) . ^^^ The present data show that GR 43175 interacts preferentially as an agonist with 5 HT1B and 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Moreover , 5 HT 1 is heterogenous and can be divided into 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D subtypes . 5 HT1B is probably related to the 5 HT autoreceptor controlling 5 HT release . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
As 5 HT 1 receptors were first described using radioligand binding studies , a brief description of 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D receptor binding is given . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Identification of 5 HT receptor subtypes 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 ( possibly A and B ) , 5 HT 3 subtypes , and possibly 5 HT 4 has encouraged the manufacture of 5 HT receptor inhibitors with greater subtype specificity . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
No significant correlations were found between drug affinities for 125I R ( ) DOI labeled sites in rat cortex and 5 HT1A , 5 HT1B , 5 HT1D , or 5 HT 3 sites , as determined by previous investigators . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The potencies of the serotonin receptor agonists and antagonists were compared with their affinities for 5 HT1A , 5 HT1B , 5 HT1C , and 5 HT1D binding sites in pig or rat tissue membranes ; in addition , the potencies of the agonists were compared to their potencies in inhibiting adenylate cyclase activity in membranes of calf substantia nigra . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Characterization of a [ 3H ] 5 hydroxytryptamine binding site in rabbit caudate nucleus that differs from the 5 HT1A , 5 HT1B , 5 HT1C and 5 HT1D subtypes . [ 3H ] 5 HT binding sites were analyzed in membranes prepared from the rabbit caudate nucleus ( CN ) . [ 3H ] 5 HT labeled both 5 HT1A and 5 HT1C recognition sites , defined by nanomolar affinity for 8 OH DPAT and mesulergine respectively ; however , these represented only a fraction of total specific [ 3H ] 5 HT binding . ^^^ The pharmacological profile of the non 5 HT1A / non 5 HT1C sites ( designated 5 HT1R ) also differed from that of 5 HT1B and 5 HT 2 sites , but was similar to that of the 5 HT1D site . ^^^ The present findings demonstrate the presence of a high affinity [ 3H ] 5 HT binding site in rabbit CN , designated 5 HT1R , that is different from previously defined 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , and 5 HT 2 sites . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Agonist binding to 5 HT1A , 5 HT1B , and 5 HT1D sites in rat brain and to 5 HT1A and 5 HT1D sites in bovine brain is sensitive to NEM . ^^^ These findings suggest that agonist binding to 5 HT1A , 5 HT1B , and 5 HT1D sites is sensitive to NEM alkylation . ^^^ These data suggest that NEM exerts its effects on 5 HT1A , 5 HT1B , and 5 HT1D binding sites by inactivating the G protein ( s ) associated with the 5 HT receptor subtypes . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Radioligand binding studies were performed to characterize serotonin 5 HT1D receptors in postmortem human prefrontal cortex and caudate homogenates . [ 3H ] 5 HT binding , in the presence of pindolol ( to block 5 HT1A and 5 HT1B receptors ) and mesulergine ( to block 5 HT1C receptors ) , was specific , saturable , reversible , and of high affinity . ^^^ In competition experiments , 8 hydroxydipropylaminotetralin , trifluoromethylphenylpiperazine , mesulergine , 4 bromo 2 , 5 dimethoxyphenylisopropylamine , and ICS 205 930 had low affinity for [ 3H ] 5 HT labeled 5 HT1D sites , indicating that the pharmacology of the 5 HT1D site is distinct from that of previously identified 5 HT1A , 5 HT1B , 5 HT1C , 5 HT 2 , and 5 HT 3 sites . 5 HT1D sites in human brain have a similar pharmacology to the 5 HT1D sites previously identified in rat , porcine and bovine brains . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The different subpopulations of 5 HT 1 sites were investigated by the use of unlabeled selective compounds . 8 OH DPAT ( 8 hydroxy 2 [ N , N di n propyl amino ] tetralin ) was used to block [ 3H ] 5 HT binding to 5 HT1A , the beta blocker ( ) 21 009 ( 4 [ 3 ter butyl amino 2 hydroxy propoxy ] indol 2 carbonic acid isopropyl ester ) to 5 HT1B and the ergoline mesulergine to 5 HT1C recognition sites . 5 HT1D sites were defined as the binding sites remaining when both 8 OH DPAT and mesulergine were added to the incubation medium . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Inhibition studies with [ 3H ] 5 HT plus 100 nM 8 OH DPAT ( which inhibits binding to 5 HT1A receptors only ) representing total binding , indicated that no further displacement occurred when ligands preferentially selective for 5 HT1B , 5 HT1D alpha , 1D beta , or 5 HT2C were tested . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT 1 subfamily of receptors contains subtypes 5 HT1A , 5 HT1B , 5 HT1D , 5 HT1E , and 5 HT1F ; activation of all of them results in the inhibition of adenylylcyclase . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In addition , these antibodies were successfully used in immunofluorescence experiments to detect the 5 HT1B / 1D beta , but not the 5 HT1D / 1D alpha , receptor in transiently transfected LLC PK 1 cells . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Evidence that 5 hydroxytryptamine release in rat dorsal raph nucleus is controlled by 5 HT1A , 5 HT1B and 5 HT1D autoreceptors . ^^^ These results suggest that 5 HT release in the rat DRN is under the control of 5 HT1A , 5 HT1B and 5 HT1D autoreceptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Mutual influences are seen particularly with 5 HT1A , 5 HT1C and 5 HT 2 , but not with 5 HT1B , 5 HT1D or 5 HT 3 receptor mediated effects . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Within these hydrophobic regions , this receptor was found to be 41 36 % identical to the following serotonin [ 5 hydroxytryptamine ( 5 HT ) ] receptors : 5 HT 2 > 5 HT1D > 5 HT1C > 5 HT1B > 5 HT1A > 5 HT1E . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Pharmacological differentiation of human 5 HT1B and 5 HT1D receptors . ^^^ Human 5 hydroxytryptamine1B ( 5 HT1B ; also designated 5 HT1D beta ) receptors and 5 HT1D ( also designated 5 HT1D alpha ) receptors are distinct molecular entities which mediate serotonergic neurotransmission . ^^^ The present study analyzed a series of 21 drugs , 8 of which were found to be at least an order of magnitude more potent at 5 HT1D than 5 HT1B receptors . ^^^ These data provide pharmacological evidence that human 5 HT1B and 5 HT1D receptors are distinct molecular entities which represent independent targets for future drug development . ^^^ Furthermore , these data indicate that a number of selective pharmacological agents already exist and can be used to analyze the functional roles of 5 HT1B and 5 HT1D receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The effects of intra collicular injections of 5 HT 1 drugs on distractibility were studied in hooded rats trained to run toward illuminated targets for a food reward in a 2 choice runway . 8 hydroxy 2 ( di n propylamino ) tetraline ( 8 OH DPAT ) , a 5 HT1A receptor agonist , RU 24969 , a mixed 5 HT1A and 5 HT1B agonist , serotonin O carboxymethylglycyltyrosinamide ( S CM GTNH 2 ) , a mixed 5 HT1B and 5 HT1D receptor agonist and saline ( control ) were alternately injected . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Serotonin ( 5 HT ) receptors have been classified into several categories , and they are termed as 5 HT 1 , 5 HT 2 , 5 HT 3 , 5 HT 4 , 5 HT 5 , 5 HT 6 and 5 HT 7 type receptors . 5 HT 1 receptors have been further subdivided into 5 HT1A , 5 HT1B , 5 HT1D , 5 HT1E and 5 HT1F . 5 HT 2 receptors have been divided into 5 HT2A , 5 HT2B and 5 HT2C receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT1A , 5 HT1B and beta adrenergic receptor antagonists pindolol and cyanopindolol ( 6 mg / kg SC ) did not affect punished responding either , nor did the 5 HT1D receptor partial agonist and alpha 2 adrenergic receptor antagonist yohimbine ( 2 . 5 mg / kg SC ) or the histamine H 1 receptor antagonist mepyramine ( 1 mg / kg SC ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The neuroendocrine effects of sumatriptan differ from those of previously described 5 HT receptor agonists , and may be a consequence of selective activation of 5 HT1D or 5 HT1B receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The aim of this study was to provide evidence that anpirtoline , which is an agonist at 5 HT1B and 5 HT1D receptors and also displays submicromolar affinity for 5 HT1A recognition sites , in addition , acts as an antagonist at 5 HT 3 receptors . 2 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These studies not only demonstrate the existence of several classes of serotonin receptors called 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 , 5 HT 3 and 5 HT 4 , but led also to the development of novel agonists and antagonists for the stimulation or blockade of each of them . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The functional activity of various 5 HT receptor agonists , including 5 CT , sumatriptan , CP 93 , 129 and 1 naphtylpiperazine , and of drugs known to bind with high affinity to 5 HT1B ( pindolol , propranolol , cyanopindolol , SDZ 21 , 009 and isamoltane ) or 5 HT1D binding sites ( yohimbine and rauwolscine ) was measured at 5 HT receptors that are negatively coupled to adenylate cyclase in cultures of the renal epithelial cell line OK . 5 HT receptor mediated inhibition of adenylate cyclase was studied by measuring inhibition of cAMP formation , induced by 100 microM forskolin . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The clinical effective dose of ergotamine , beginning from the minimal dose of 1 mg , correlates well with its affinity for 5 HT1B and 5 HT1D receptors , and the rank order of clinical potency of ergotamine is superior to sumatriptan . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Localization of 5 HT1B , 5 HT1D alpha , 5 HT1E and 5 HT1F receptor messenger RNA in rodent and primate brain . ^^^ Thus , 5 HT1B and 5 HT1D alpha mRNA were determined in rat and mouse brain , while 5 HT1E and 5 HT1F mRNA were studied in human ( and monkey ) and guinea pig brain , respectively . 5 HT1B and 5 HT1D alpha hybridization signals were predominantly present in caudate putamen and cortical areas ; in addition , 5 HT1B mRNA was also detected in hippocampus , cerebellum and cerebral arteries . ^^^ In general , the distribution of 5 HT1B mRNA was characterized by high densities , whereas 5 HT1D alpha mRNA was expressed at very low levels . ^^^ Comparison of the localization of the mRNAs to the regional distributions of the 5 HT1B and 5 HT1D binding sites in rat brain ( described in a previous study ) , revealed that both receptor subtypes could be putative presynaptic heteroreceptors , modulating the release of various neurotransmitters in the central nervous system . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Therefore , terminal 5 HT1D autoreceptors bear similarity to terminal 5 HT1B autoreceptors identified in rat brain in being devoid of a significant rhythm in their responsiveness . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT inhibition of SRC and SAT is predominant and is mediated by 5 HT 1 like receptors , which , however , do not seem to correspond to 5 HT1A , 5 HT1B , 5 HT1C , 5 HT1D , 5 HT1E , or 5 HT1F receptor subtypes . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We sought molecular evidence for the expression of an mRNA species encoding the 5 HT1D receptor subtype in guinea pig and human trigeminal ganglia , using the polymerase chain reaction with oligonucleotides uniquely homologous to the coding sequences of the 5 HT1B / D family ( human 5 HT1D alpha and 5 HT1D beta ; rat 5 HT1B ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The firing rate of dorsal raphe serotonergic neurons is under the control of somatodendritic 5 hydroxytryptamine 1A ( 5 HT1A ) autoreceptors , the release of serotonin from nerve terminals is under the control of 5 HT autoreceptors ( 5 HT1B subtype in rodents , 5 HT1D in other species ) , whereas the control of the activity of tryptophan hydroxylase , the rate limiting enzyme of serotonin synthesis , is complex , involving 5 HT1A but possibly other 5 HT receptors including the 5 HT1B / D subtype . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
L 694 , 247 had an affinity ( pIC 50 ) of 10 . 03 at the 5 HT1D binding site and 9 . 08 at the 5 HT1B binding site ( sumatriptan : pIC 50 values 8 . 22 and 5 . 94 respectively ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The affinities of S 14489 , S 15535 and S 15931 for other 5 HT receptor types ( 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 and 5 HT 3 ) were about 50 to 1000 fold lower . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
When OKc 1 is compared to the rat , mouse , and human 5 HT1B receptors , it has an amino acid sequence identity of 82 % , but it is only 54 % identical to the human 5 HT1D receptor . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Autoradiographic characterisation and localisation of 5 HT1D compared to 5 HT1B binding sites in rat brain . ^^^ The pharmacology of the [ 125I ] GTI binding sites was analysed using compounds known to display high affinity for and / or distinguish between 5 HT1B and 5 HT1D sites : 5 carboxamidotryptamine ( 5 CT ) , sumatriptan , CP 93129 ( 5 hydroxy 3 ( 4 1 , 2 , 5 , 6 tetrahydropyridyl ) 4 azaindole ) , ( ) pindolol , PAPP ( 4 [ 2 [ 4 [ 3 ( trifluoromethyl ) phenyl ] 1 piperazinyl ] ethyl ] benzeneamine ) , rauwolscine , and 8 OH DPAT . ^^^ By contrast , the selective 5 HT1B compound CP 93129 and ( ) pindolol produced biphasic curves showing a majority of high affinity sites in the globus pallidus and the substantia nigra , whereas PAPP and sumatriptan ( which are somewhat 5 HT1D selective ) produced biphasic curves indicating a minority of high affinity sites in these areas . ^^^ Low densities of the 5 HT1D recognition sites were found to be present in globus pallidus , ventral pallidum , caudate putamen , subthalamic nucleus , entopeduncular nucleus , substantia nigra ( reticular part ) , nuclei of the ( normal and accessory ) optic tract , different nuclei of the geniculate body and frontoparietal cortex , although higher densities of 5 HT1B sites were always observed in the same structures . ( ABSTRACT TRUNCATED AT 400 WORDS ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In radioligand binding studies , SDZ 216 525 showed high affinity and selectivity for 5 HT1A sites ( pKD = 9 . 2 ) as compared to 5 HT1B , 5 HT1C , 5 HT1D , 5 HT 2 and 5 HT 3 sites ( pKD = 6 . 0 , 7 . 2 , 7 . 5 , 5 . 2 and 5 . 4 , respectively ) . ^^^ The effects of SDZ 216 525 , MDL 73005 and NAN 190 on 5 HT 1 receptor linked second messengers were characterised in the following tests : inhibition of forskolin stimulated adenylate cyclase activity in calf hippocampus ( 5 HT1A ) , rat substantia nigra ( 5 HT1B ) and calf substantia nigra ( 5 HT1D ) and stimulation of inositol phosphate production in pig choroid plexus ( 5 HT1C ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Within the conserved transmembrane domains , the sequences exhibit approximately 52 % , 59 % , 65 % , and 68 % amino acid identity with the known rat 5 HT1A , rat 5 HT1B , rat 5 HT1D , and human 5 HT1E receptors , respectively . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
However , drug affinities for the human 5 HT1B and 5 HT1D receptors correlate most closely with the rank order of clinical dosages used to treat a migraine attack . ^^^ Therefore , these data indicate that human 5 HT1B and / or 5 HT1D receptors are likely to mediate the therapeutic efficacy of acute anti migraine drugs . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Carboxamidotryptamine insensitive 5 HT 1 like receptors are concentrated in guinea pig but not rat , claustrum . 5 CT ( 5 carboxamidotryptamine ) insensitive ( 5 HT1E / 5 HT1F ) 5 HT 1 like recognition sites have been mapped autoradiographically in rat and guinea pig brain using [ 3H ] 5 HT in the presence of 5 CT and mesulergine to mask 5 HT1A , 5 HT1B , 5 HT1D and 5 HT2C binding sites . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Since the 5 HT1B receptor is the rodent homologue of the 5 HT1D beta subtype , it might be anticipated that 5 HT1D beta receptors will be found to mediate vasoconstrictor responses in non rodent species . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Functional effects of the 5 HT1D receptor antagonist GR 127 , 935 at human 5 HT1D alpha , 5 HT1D beta , 5 HT1A and opossum 5 HT1B receptors . ^^^ GR 127 , 935 did not show 5 HT1D beta receptor mediated agonist activity in permanently transfected CHO K 1 cells , whereas at submicromolar and higher concentrations intrinsic agonist activity was observed in HeLa / 5 HT1A , OK / 5 HT1B and CHO K1 / 5 HT1D alpha cells . ^^^ The antagonist activity of 1 microM of GR 127 , 935 at CHO K1 / 5 HT1D alpha and OK / 5 HT1B receptor sites was only partial and less pronounced . ^^^ This contrasts with the silent antagonism of methiothepin at the 5 HT1D alpha ( KB value = 11 . 8 nM ) , 5 HT1D beta ( KB value = 6 . 9 nM ) and 5 HT1B ( KB value = 49 . 3 nM ) receptor subtypes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Hydroxytryptamine 5 HT1D receptors mediating inhibition of cyclic AMP accumulation in Madin Darby canine kidney ( MDCK ) cells . 5 Hydroxytryptamine 5 HT1B / 5 HT1D receptors are members of the same receptor subfamily , but display a different pharmacology ( Hartig et al . ( 1992 ) Trends Pharmacol Sci 13 : 152 159 ) . ^^^ Whereas several cell lines have been reported to contain 5 HT1B receptors , none has been described , however , that endogenously expresses well characterized 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The high affinity component ( pKD = 9 . 2 9 . 9 ) probably corresponded to 5 HT1B ( rat ) or 5 HT1D ( guinea pig ) receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We studied the dural plasma protein extravasation response after unilateral electrical stimulation of the trigeminal ganglion in mice lacking serotonin 5 HT1B ( 5 HT1D beta ) receptors by modifying a technique previously described in rats or guinea pigs . ^^^ These results suggest that CP 93 , 129 , sumatriptan , and GTI exert their effects via 5 HT1B ( 5 HT1D beta ) receptors in mice . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These results indicate that chicken ileum contains 5 HT 1 receptors similar to the 5 HT1D mammalian subtype but not the 5 HT1A , 5 HT1B , 5 HT1C or 5 HT 3 subtypes . 5 HT 2 receptors are also present and would appear to be located on smooth muscle . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These findings support the identification of the guinea pig 5 HT terminal autoreceptor as a 5 HT1D receptor and reinforce the species homology between the 5 HT1B and 5 HT1D receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT receptor identity of control and transfected C 6 glial / 5 HT1D beta cells was determined by reverse transcription polymerase chain reaction using primers specific for rat 5 HT1A , rat 5 HT1B , rat 5 HT1D alpha , human 5 HT1D beta , and rat 5 HT2A receptor genes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Although the beta adrenergic receptor antagonist ( ) propranolol binds with relatively low affinity at human 5 hydroxytryptamine1D beta receptors ( Ki = 10 , 200 nM ) , it displays significantly higher affinity ( Ki = 17 nM ) at its species homolog , 5 HT1B receptors , and at a mutant 5 HT1D beta receptor ( Ki = 16 nM ) , where the threonine residue at position 355 ( T 355 ) is replaced with an asparagine residue ( i . e . , a T355N mutant ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Selective antagonism of human 5 HT1D and 5 HT1B receptor mediated responses in stably transfected C 6 glial cells by ketanserin and GR 127 , 935 . ^^^ The antagonist effects of ketanserin and 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 ) oxadiazol 3 yl ) biphenyl [ 4 carboxyli c acid 4 methoxy 3 ( 4 methyl piperazin 1 yl ) phenyl ] amide ( GR 127 , 935 ) were compared to naratriptan induced inhibition of cAMP formation in C 6 glial cell lines stably expressing human 5 HT1D or 5 HT1B receptor sites . ^^^ The differential antagonist effects of ketanserin and GR 127 , 935 on naratriptan responses elicited in C 6 glial / 5 HT1D and C 6 glial / 5 HT1B cells demonstrate these compounds do selectively block human 5 HT1D and 5 HT1B receptors , respectively . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In mesencephalic raphe , hippocampus and frontal cortex slices , the 5 HT1D / 1B receptor agonist , sumatriptan and the 5 HT 1 receptor agonist , 5 methoxytryptamine ( 5 MeOT ) but not the 5 HT1B receptor agonist , CP 93129 , inhibited electrically the evoked release of [ 3H ] 5 HT in a concentration dependent manner . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In the rat and mouse , the terminal autoreceptor is known to be a 5 HT1B receptor , whereas in human , pig , rabbit , and guinea pig , the terminal autoreceptor is thought to belong to the 5 HT1D receptor subtype . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The rat 5 HT1B receptor ( also referred to as the 5 HT1D beta receptor ) is expressed in both serotonergic and nonserotonergic neurons in the rat brain , where it has been hypothesized to inhibit the release of neurotransmitters from axonal terminals . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The inhibitory potency of the drugs was significantly correlated with their affinity for 5 HTID receptors in human brain and for cloned human 5 HT1D alpha and 5 HT1D beta receptors , but not with their affinity for 5 HT1B , 5 HT1E , 5 HT1F , 5 HT2A , 5 HT2B , 5 HT2C , 5 HT 3 , 5 HT5A , 5 HT5B and 5 HT 7 receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In the present study , we measured the affinity of acetaminophen at 5 HT 3 , as well as 5 HT1A , 5 HT1B , 5 HT1D , 5 HT 2 , 5 HT2C , 5 HT 4 , 5 HT 6 , 5 HT 7 and eleven other receptor sites and at serotonin and norepinephrine reuptake sites . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Pharmacology of cloned human 5 HT1D receptor mediated functional responses in stably transfected rat C 6 glial cell lines : further evidence differentiating human 5 HT1D and 5 HT1B receptors . ^^^ Together with the 5 HT1D receptor binding selectivity and antagonist activity of ketanserin and ritanserin , the findings define important pharmacological differences between cloned human 5 HT1D and 5 HT1B receptor sites . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Micromolar concentrations of the 5 HT1B receptor agonist 3 ( 1 , 2 , 5 , 6 tetrahydro ) 4 pyridil 5 pyrrolo [ 3 , 2 b ] pyril 5 one ( CP 93 , 129 ) and of the 5 HT 2 receptor agonist 1 ( 2 , 5 dimethoxy 4 iodophenyl _ 2 aminopropane ( DOI ) induced cell growth with a potency that accorded with the affinity of these compounds for the human 5 HT1D receptor site . ^^^ The findings suggest that 5 HT1A , 5 HT1B and 5 HT 2 receptors are not implicated in 5 HT stimulated C 6 glial / 5 HT1D cell growth . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The interaction was shown in rat and guinea pig brain tissues and in cells transfected with either 5 HT1B or 5 HT1D beta receptor gene . [ 3H ] 5 HT moduline binds to a single population of sites in mammalian brain ( Kd = 0 . 4 nM in rat , Kd = 0 . 8 nM in guinea pig ) as well as in transfected cells expressing the 5 HT1B or the 5 HT1D beta receptors ( Kd = 0 . 2 and 0 . 6 nM , respectively ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Functional behavioral homology between rat 5 HT1B and guinea pig 5 HT1D receptors in the modulation of prepulse inhibition of startle . ^^^ The present series of experiments explored the functional similarity between the rat 5 HT1B receptor and the guinea pig 5 HT1D receptor on two behavioral measures known to be influenced by 5 HT1B receptor manipulations in rats : prepulse inhibition of the startle response ( PPI ) and locomotor activity . ^^^ Because the 5 HT1B agonist RU 24969 disrupts PPI and stimulates locomotor behavior in rats , it was predicted that the 5 HT1D agonist , SDZ 219 964 , would demonstrate a similar behavioral profile in guinea pigs . ^^^ It is concluded that a functional similarity exists between 5 HT1D and 5 HT1B receptors with regard to the modulation of sensorimotor inhibition and , to a lesser extent , locomotor activity . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The effect of TFMPP and RU 24969 on duration of suppression was blocked by ( + ) mianserin , a drug with high affinity for the rat 5 HT1D , but not 5 HT1B , receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Oligonucleotide primers were chosen based on unique regions of complementary DNA sequence for each of the 12 cloned rat serotonin receptor subtypes ( i . e . 5 HT1A , 5 HT1B , 5 HT1D , 5 HT1F , 5 HT2A , 5 HT2B , 5 HT2C , 5 HT 3 , 5 HT5A , 5 HT5B , 5 HT 6 and 5 HT 7 ) and high stringency conditions were used during polymerase chain reaction . ^^^ Within lumbar dorsal root ganglia , the presence of the 5 HT1B , 5 HT1D , 5 HT2A , 5 HT2C , 5 HT 3 and 5 HT 7 receptor subtype messenger RNAs was detected . ^^^ Within superior cervical ganglia , the presence of messenger RNA for 5 HT1A , 5 HT1B , 5 HT1D , 5 HT2A , 5 HT 3 , 5 HT 6 , and 5 HT 7 receptor subtypes was detected . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These data suggest that neither the 5 HT1A , 5 HT1B , 5 HT1D , 5 HT2A , 5 HT2B , 5 HT2C , 5 HT 3 , 5 HT 5 , 5 HT 6 , nor 5 HT 7 receptors are involved . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These data suggest that sumatriptan inhibits neurogenic inflammation via 5 HT1D alpha receptors in guinea pigs and 5 HT1D beta ( 5 HT1B ) receptors in rats . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Here , we also report the ability of a 5 HT1D receptor antagonist , GR 127935 , to antagonize 5 HT1B receptors in vivo . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In this review , the functional interactions between serotonin ( 5 HT ) and other neuronal systems are discussed with the focus on microdialysis studies in the mammalian brain ( mainly rats ) . 5 HT release is negatively regulated not only by somatodendritic 5 HT1A and terminal 5 HT1B ( 5 HT1D ) autoreceptors but also by alpha 2 adrenergic and mu opioid heteroreceptors that are located on serotonergic nerve terminals . 5 HT by itself is involved in the inhibitory effects of noradrenaline release and the facilitatory regulation of dopamine release via multiple 5 HT receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Alignment of receptor nomenclature with the human genome : classification of 5 HT1B and 5 HT1D receptor subtypes . ^^^ Based on these principles , the present classification of 5 HT1B and 5 HT1D receptors is reconsidered , and a revised nomenclature for 5 HT1B , 5 HT1D alpha and 5 HT1D beta receptor subtypes is suggested . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In conclusion , the pharmacology of the cloned 5 HT1D receptor subtype seems , unlike the 5 HT1B receptor subtype , conserved among various mammal species such as the human , guinea pig , and rat . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Both E and DHE are 5 HT1A , 5 HT1B , 5 HT1D , and 5 HT1F receptor agonists . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Serotonin efflux in the rat ventral lateral geniculate nucleus assessed by fast cyclic voltammetry is modulated by 5 HT1B and 5 HT1D autoreceptors . ^^^ CP 93129 ( 0 . 3 microM ) , the selective 5 HT1B agonist , decreased 5 HT efflux to 37 + / 4 % of control and was antagonised by the 5 HT1B blocker isamoltane ( 0 . 5 microM ) and by the 5 HT1D / B antagonist GR 127935 ( 50 nM ) . ^^^ Furthermore , released 5 HT is taken up by the 5 HT transporter and may be under the influence of 5 HT1B and 5 HT1D autoreceptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In both types of vessel , the inability of 5 HT1B / 1D agonists to achieve the same maximum as the endogenous agonist 5 HT is explained by the additional presence of 5 HT2A receptors . 4 . 311C90 displayed high affinity at human recombinant 5 HT1D ( formerly 5 HT1D alpha ) and 5 HT1B ( formerly 5 HT1D beta ) receptors in transfected CHO K 1 cell membranes ( pIC 50 values = 9 . 16 + / 0 . 12 and 8 . 32 + / 0 . 09 , respectively ) . ^^^ Its potent partial agonist action at `` 5 HT1B like ' receptors in intracranial arteries , coupled with potent agonism at 5 HT1D and 5 HT1B receptors and an ability to inhibit neurogenic plasma protein extravasation in the dura , are consistent with its utility as an effective acute treatment for migraine . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Ketanserin and ritanserin showed low affinity for [ 3H ] GR 125 , 743 binding to guinea pig striatal sites ( K ( 1 ) = 12600 and 369 nM ) , suggesting that 5 HT1B ( rather than 5 HT1D ) receptors are predominantly labelled in this tissue . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We have studied the effects of the purportedly selective 5 HT1A receptor antagonist ( + ) WAY 100135 on electrically stimulated 5 hydroxytryptamine ( 5 HT ) efflux in the ventrolateral geniculate nucleus ( vLGN ) , and its affinity at human 5 HT1B and 5 HT1D receptors stably expressed in Chinese hamster ovary ( CHO ) cells . 2 . ^^^ The affinity and intrinsic activity of ( + ) WAY 100135 were determined at recombinant human 5 HT1B and 5 HT1D receptors expressed in CHO cells , by use of radioligand binding and [ 35S ] GTP gamma S binding ( + ) WAY 100135 was a partial agonist at human 5 HT1B and 5 HT1D receptors with moderately high affinity for 5 HT1D receptors ( pEC 50 = 7 . 61 ) . 5 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Molecular cloning and pharmacological characterization of guinea pig 5 HT1B and 5 HT1D receptors . ^^^ Human 5 HT1B and 5 HT1D receptors have been implicated as molecular targets for the treatment of acute migraine based upon the pharmacological actions and clinical efficacy of sumatriptan , an agonist for human 5 HT1B / 1D receptors . ^^^ Since two distinct , but closely related receptors displaying `` 5 HT1D receptor pharmacology ' ' have been cloned previously from most mammalian species , the genes encoding these receptors were isolated from a guinea pig liver genomic DNA library using oligonucleotide probes targeted to nonconserved regions of recombinant human 5 HT1B and 5 HT1D receptors . ^^^ Sequence analysis indicates that guinea pig 5 HT1B and 5 HT1D receptors are comprised 390 and 378 amino acids , respectively . ^^^ Comparison of the deduced amino acid sequences of guinea pig 5 HT1B and 5 HT1D receptor subtypes show that they display overall and transmembrane ( TM ) identities of 63 % and 77 % , respectively . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Differential distribution of [ 3H ] sumatriptan binding sites ( 5 HT1B , 5 HT1D and 5 HT1F receptors ) in human brain : focus on brainstem and spinal cord . ^^^ We report on the autoradiographic distribution of 5 HT1B , 5 HT1D and 5 HT1F receptor subtypes in human brain , focusing on the brainstem and cervical spinal cord . ^^^ We have used [ 3H ] sumatriptan as a radioligand in the presence of suitable concentrations of 5 CT ( 5 carboxamidotryptamine ) to define 5 HT1F receptors , and ketanserin , to discriminate between 5 HT1B and 5 HT1D receptors . ^^^ Significant levels of 5 HT1B and 5 HT1D receptors found in migraine control pain areas suggest their involvement in antinociceptive mechanisms . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
By manipulating the activity of the oncogene ( ts SV40T ) product used to immortalize the serotoninergic precursors , it has been possible to compare the expression of the 5 HT receptors in either replicative or differentiating cells . 5 HT1B , 5 HT1D , 5 HT 3 , 5 HT 6 and 5 HT 7 receptor gene expression were all observed in the replicating cells . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The serotonin ( 5 HT ) receptor subtype mediating inhibition of neurogenic dural inflammation in guinea pigs was investigated using a series of serotonin agonists with differing affinities for the 5 HT1B , 5 HT1D and 5 HT1F receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The present study shows that the hypothermic response to SKF 99101H is dose dependently blocked by SB 224289G ( 1 ' methyl 5 ( 2 ' methyl 4 ' [ ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) bipheny l 4 yl ] carbonyl ) 2 , 3 , 6 , 7 tetrahydrospiro [ furo [ 2 , 3 f ] indole 3 , 4 ' pi peridone ] hemioxalate ) ( 0 . 3 10 . 0 mg / kg p . o . ) ( ED 50 3 . 62 mg / kg ) , which is the first compound to be described which is more than 60 fold selective for the 5 HT1B receptor over the 5 HT1D receptor . ^^^ SB 216641A ( N [ 3 ( 2 dimethylamino ) ethoxy 4 methoxy phenyl ] 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) ( 1 , 1 ' biphenyl ) 4 car boxamide hydrochloride ) ( 0 . 6 20 . 0 mg / kg i . p . ) , which is somewhat less selective ( 30 fold ) for the 5 HT1B receptor over the 5 HT1D receptor had a similar effect ( ED 50 4 . 43 mg / kg ) . ^^^ These data demonstrate that 5 HT1B ( formerly 5 HT ( 1D beta ) ) and not 5 HT1D ( formerly 5 HT ( 1D alpha ) ) receptors mediate the hypothermic response to SKF 99101H ( 30 mg / kg i . p . ) in guinea pigs . ^^^ The compounds described are useful pharmacological tools for distinguishing responses to 5 HT1B and 5 HT1D receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
SB 216641 and BRL 15572 compounds to pharmacologically discriminate h 5 HT1B and h 5 HT1D receptors . ^^^ Despite only modest homology between h 5 HT1B and h 5 HT1D receptor amino acid sequences , these receptors display a remarkably similar pharmacology . ^^^ We now report on two compounds , SB 216641 ( N [ 3 ( 2 dimethylamino ) ethoxy 4 methoxyphenyl ] 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) ( 1 , 1 ' biphenyl ) 4 carboxamide ) and BRL 15572 3 [ 4 ( 3 chlorophenyl ) piperazin 1 yl ] 1 , 1 diphenyl 2 propanol ) , which display high affinity and selectivity for h 5 HT1B and h 5 HT1D receptors , respectively . ^^^ In receptor binding studies on human receptors expressed in CHO cells , SB 216641 has high affinity ( pKi = 9 . 0 ) for h 5 HT1B receptors and has 25 fold lower affinity at h 5 HT1D receptors . ^^^ In contrast , BRL 15572 has 60 fold higher affinity for h 5 HT1D ( pKi = 7 . 9 ) than 5 HT1B receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Chronic paroxetine desensitises 5 HT1D but not 5 HT1B autoreceptors in rat lateral geniculate nucleus . ^^^ The present study examined the effect of chronic paroxetine ( 10 mg / kg p . o . , 21 days ) on the 5 HT1B and 5 HT1D autoreceptors controlling 5 HT efflux in slices of rat ventrolateral geniculate nucleus . ^^^ M . ) than water ( 15 . 8 + / 1 . 4 nM ) . 5 HT efflux was inhibited by CP 93129 ( 1 nM 10 microM ) and sumatriptan ( 1 nM 1 microM ) , agonists at 5 HT1B and 5 HT1D receptors , respectively . ^^^ This may be the result of desensitisation of 5 HT1D but not 5 HT1B autoreceptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Effects of selective h 5 HT1B ( SB 216641 ) and h 5 HT1D ( BRL 15572 ) receptor ligands on guinea pig and human 5 HT auto and heteroreceptors . ^^^ Human cerebral cortical slices and synaptosomes , guinea pig cerebral cortical slices and human right atrial appendages were used to study the effects of SB 216641 , a preferential h 5 HT1B receptor ligand , and of BRL 15572 , a preferential h 5 HT1D receptor ligand , on the presynaptic h 5 HT1B and h 5 HT1B like autoreceptors in the human and guinea pig brain preparations , respectively , and on the presynaptic h 5 HT1D heteroreceptors in the human atrium . ^^^ This effect was not modified by BRL 15572 ( 2 microM ; concentration 154 times higher than its Ki at h 5 HT1D receptors ) but was antagonized by SB 216641 ( 0 . 1 microM ; concentration 100 times higher than its Ki at h 5 HT1B receptors ; apparent pA 2 8 . 45 ) . ^^^ This response was unaffected by BRL 15572 ( 300 nM ) but antagonized by SB 216641 ( 15 nM ; drug concentrations 23 and 15 times higher than their Ki at h 5 HT1D and h 5 HT1B receptors , respectively ) . ^^^ In human atrial appendages , the electrically evoked tritium overflow was inhibited by 5 HT in a manner susceptible to antagonism by BRL 15572 ( 300 nM ; 23 times Ki at h 5 HT1D receptors ) but not by SB 216641 ( 30 nM ; 30 times Ki at h 5 HT1B receptors ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The G protein coupling behavior of four human 5 hydroxytryptamine receptor subtypes ( 5 HT1A , 5 HT1B , 5 HT1D , and 5 HT1E ) has been studied in membranes from Sf 9 cells expressing the individual receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In a similar manner , the mixed 5 HT1B 5 HT1D receptor agonist sumatriptan ( 800 nM ) decreased significantly K+ evoked 5 HT release in the frontal cortex ( by 46 % ) of wild type mice but had no effect in mutants . ^^^ These data provide in vivo evidence that , in mice , 5 HT1B , but not 5 HT1D , autoreceptors inhibit 5 HT release at nerve terminals located in the frontal cortex and ventral hippocampus . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Sumatriptan , a relatively pure 5 HT1D / 5 HT1B receptor agonist , also showed higher potency versus neurogenic inflammation . ^^^ MDL 74 , 721 demonstrated nanomolar affinity for 5 HT1A ( 12 . 7 + / 0 . 3 nM ) and 5 HT1D ( 41 . 3 + / 10 . 9 nM ) but considerably lower affinity for 5 HT1B receptors ( > 1000 nM ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These data suggest a possible involvement of 5 HT2A and 5 HT1B or 5 HT1D receptors in the response to 5 HT . 4 . ^^^ Contractions to ( + / ) alpha me 5 HT , which is selective for 5 HT2A over 5 HT1B and 5 HT1D receptors , were competitively antagonized by low concentrations of ketanserin . ^^^ These data appear to confirm the presence of 5 HT1B and / or 5 HT1D receptors in the tissue . 6 . ^^^ This reinforces the evidence that 5 HT1B and / or 5 HT1D receptors contribute to the effects of 5 HT in the tissue . 7 . ^^^ In conclusion , in endothelium denuded rabbit epicardial coronary arteries , 5 HT activates 5 HT2A and 5 HT1D and / or 5 HT1B receptors to cause contraction . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Binding experiments at cloned human 5 HT1A , 5 HT1B , and 5 HT1D receptors show that these derivatives are potent and selective ligands for 5 HT1B / 1D subtypes with increased binding selectivity versus the 5 HT1A receptor when compared to 1 naphthylpiperazine ( 1 NP ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Preferential expression of 5 HT1D over 5 HT1B receptors during early embryogenesis . ^^^ The cloning and pharmacological characterization of mouse 5 HT1D receptors as well as the comparative analysis of its embryonic expression vs that of 5 HT1B receptors are reported . ^^^ In contrast , no specific 5 HT1B binding sites could be detected until 13 . 5 days of development , when they were present at lower levels than 5 HT1D receptors . ^^^ This differs markedly from the situation in the adult brain , in which 5 HT1B receptors are present at a much higher density than the 5 HT1D subtype . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Naphthyloxy ) ethylamines with enhanced affinity for human 5 HT1D beta ( h 5 HT1B ) serotonin receptors . ^^^ Although the beta adrenergic antagonist propranolol ( 1 ) binds at rodent 5 HT1B serotonin receptors , it displays low affinity ( Ki > 10 , 000 nM ) for its species homologue 5 HT1D beta ( i . e . , h 5 HT1B ) receptors . ^^^ Compound 11 was shown to bind equally well at human 5 HT1D alpha ( h 5 HT1D ) receptors ( Ki = 34 nM ) and was further demonstrated to possess h 5 HT1B agonist character in an adenylate cyclase assay . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Detailed mapping of serotonin 5 HT1B and 5 HT1D receptor messenger RNA and ligand binding sites in guinea pig brain and trigeminal ganglion : clues for function . ^^^ The similar pharmacology of the 5 HT1B and 5 HT1D receptors , and the lack of selective compounds sufficiently distinguishing between the two receptor subtypes , have hampered functional studies on these receptors . ^^^ The anatomical patterns of 5 HT1B and 5 HT1D receptor messenger RNA were quite different . ^^^ While 5 HT1B receptor messenger RNA was abundant throughout the brain ( with highest levels in the striatum , nucleus accumbens , olfactory tubercle , cortex , hypothalamus , hippocampal formation , amygdala , thalamus , dorsal raphe and cerebellum ) , 5 HT1D receptor messenger RNA exhibited a more restricted pattern ; it was found mainly in the olfactory tubercle , entorhinal cortex , dorsal raphe , cerebellum , mesencephalic trigeminal nucleus and in the trigeminal ganglion . ^^^ This distribution pattern was indistinguishable from specific 5 HT1B receptor labelling in the presence of ketanserin under conditions to occlude 5 HT1D receptor labelling ; hence the latter were below detection level . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT1B / 5 HT1D receptor agonist sumatriptan mimicked 5 HT ( EC 50 = 6 . 4 nM ; maximal effect approximately 50 % ) ; the effect of sumatriptan was also methiothepin sensitive . ^^^ The 5 HT1B / 5 HT1D receptor ligand GR 127935 and the 5 HT2C / 5 HT1B / 5 HT1D receptor ligand metergoline were unable to prevent the 5 HT effect ; instead they inhibited glutamate release , their effects being abolished by methiothepin . ^^^ The effect of sumatriptan was prevented by ketanserin , a drug known to display much higher affinity for recombinant h 5 HT1D than for h 5 HT1B receptors . 5 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The selective 5 HT1B / D receptor antagonist , GR 127935 ( 100 1000 nM ) , and the 5 HT1D receptor antagonist , ketanserin ( 300 1000 nM ) , had no significant effect on this release in either of these regions . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The human 5 HT1B and 5 HT1D receptors ( previously known as 5 HT1Dbeta and 5 HT1Dalpha , respectively ) , although encoded by two distinct genes , are structurally very similar . ^^^ Pharmacologically , these two receptors have been differentiated using nonselective chemical tools such as ketanserin and ritanserin , but the absence of truly selective agents has meant that the precise function of the 5 HT1B and 5 HT1D receptors has not been defined . ^^^ In this paper we describe how , using computational chemistry models as a guide , the nonselective 5 HT1B / 5 HT1D receptor antagonist 4 was structurally modified to produce the selective 5 HT1B receptor inverse agonist 5 , 1 ' methyl 5 [ [ 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) biphenyl 4 yl ] carbonyl ] 2 , 3 , 6 , 7 tetrahydrospiro [ furo [ 2 , 3 f ] indole 3 , 4 ' piperidine ] ( SB 224289 ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Agonistic properties of alniditan , sumatriptan and dihydroergotamine on human 5 HT1B and 5 HT1D receptors expressed in various mammalian cell lines . 1 . ^^^ Alniditan , a novel migraine abortive agent , is a potent 5 HT1B / 5 HT1D receptor agonist of nM affinity . ^^^ We compared the agonistic properties of alniditan , sumatriptan and dihydroergotamine on the cloned human 5 HT1B receptor expressed at 200 fmol mg ( 1 ) protein ( Bmax ) in non induced L929sA cells , at 740 fmol mg ( 1 ) protein in HEK 293 and at 2300 fmol mg ( 1 ) protein in mIFNbeta induced L929sA cells , and on the human cloned 5 HT1D receptor expressed in C 6 glioma cells ( Bmax 780 fmol mg ( 1 ) protein ) . 2 . ^^^ Sodium butyrate treatment increased the expression level of human ( h ) 5 HT1B receptors in HEK 293 cells and h 5 HT1D receptors in C 6 glioma cells approximately 3 fold , the binding affinities of [ 3H ] 5 HT and [ 3H ] alniditan were unaffected . 3 . ^^^ This comparative study demonstrated that alniditan was 10 times more potent than sumatriptan at the h 5 HT1B receptor , and twice as potent at the h 5 HT1D receptor . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Autoradiographic mapping of 5 HT1B and 5 HT1D receptors in human brain using [ 3H ] alniditan , a new radioligand . [ 3H ] alniditan , a new potent non indole serotonin 5 HT1B / 1D agonist , was used as a radioligand to characterize 5 HT1B and 5 HT1D receptor ( previously termed 5 HT1D beta and 5 HT1D alpha ) in various regions of the human brain . ^^^ Selective 5 HT1B receptor labeling was achieved using [ 3H ] alniditan in the presence of 300 nM of ketanserin ( sufficient to block 5 HT1D receptor labeling ) . ^^^ Surprisingly , the distribution of selective 5 HT1B receptor labeling was completely identical to the distribution of labeling of 5 HT1B + 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The 5 HT 1 like receptors mediating inhibition of sympathetic vasopressor outflow in the pithed rat : operational correlation with the 5 HT1A , 5 HT1B and 5 HT1D subtypes . 1 . ^^^ The above results suggest that the 5 HT 1 like receptors , which inhibit the sympathetic vasopressor outflow in pithed rats , display the pharmacological profile of the 5 HT1A , 5 HT1B and 5 HT1D , but not that of 5 HT 7 , receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In the human temporal artery both 5 HT 1 like and 5 HT2A receptors mediate the contractile effects of 5 hydroxytryptamine ( 5 HT ) and we have suggested that the 5 HT 1 like receptors resemble more closely recombinant 5 HT1B than 5 HT1D receptors . ^^^ To investigate further which subtype is involved , we investigated the blockade of 5 HT induced contractions by the 5 HT1B selective antagonist SB 224289 ( 2 , 3 , 6 , 7 tetrahydro 1 ' methyl 5 [ 2 methyl 4 ' [ ( 5 methyl 1 , 2 , 4 oxadiazole 3 yl ) biphenyl 4 yl ] carbonyl ] furo [ 2 , 3 f ] indole 3 spiro 4 ' piperidine oxalate ) and the 5 HT1D selective antagonist BRL 15572 ( 1 phenyl 3 [ 4 3 chlorophenyl piperazin 1 yl ] phenylpropan 2 ol ) . ^^^ We also used RT PCR to search for the mRNA of 5 HT1B , 5 HT1D and other 5 HT receptors . 2 . ^^^ We detected arterial receptor mRNA for the following receptors ( incidence ) : 5 HT1B ( 8 / 8 ) , 5 HT1D ( 2 / 8 ) , 5 HT1F ( 0 / 4 ) , 5 HT2A ( 0 / 8 ) 5 HT2B ( 0 / 8 ) , 5 HT2C ( 0 / 8 ) , 5 HT 4 ( 4 / 8 ) and 5 HT 7 ( 4 / 8 ) . 6 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In doing so , they advocate that the so called ' 5 HT 1 like ' receptors , having been shown to be a heterogeneous population of 5 HT1B , 5 HT1D and 5 HT 7 receptors , are now redundant . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Human 5 HT1B ( h 5 HT1B ) and human 5 HT1D ( h 5 HT1D ) receptors show remarkably similar pharmacology with few compounds discriminating the receptors . ^^^ We report here on a novel compound , SB 224289 ( 1 ' Methyl 5 [ [ 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) biphenyl 4 yl ] carbonyl ] 2 , 3 , 6 , 7 tetrahydro spiro [ furo [ 2 , 3 f ] indole 3 , 4 ' piperidine ] oxalate ) , which has high affinity for h 5 HT1B receptors ( pK1=8 . 16+ / 0 . 06 ) and displays over 75 fold selectivity for the h 5 HT1B receptor over all other 5 HT receptors including the h 5 HT1D receptor and all other receptors tested thus far . 2 . ^^^ Functional activity of SB 224289 was measured in a [ 15S ] GTPgammaS binding assay on recombinant h 5 HT1B and h 5 HT1D receptors expressed in Chinese Hamster Ovary ( CHO ) cells . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Specific interaction of 5 HT moduline with human 5 HT1b as well as 5 HT1d receptors expressed in transfected cultured cells . 5 HT1B receptors are the predominant auto and heteroreceptors located on serotonergic and non serotonergic terminals where they regulate the neuronal release of neurotransmitters . 5 HT moduline ( Leu Ser Ala Leu ) has been shown to specifically interact with a very high apparent affinity and in a non competitive manner with 5 HT1B receptors ( Massot et al . 1996 ; Rousselle et al . 1996 ) . ^^^ Using transfected cells expressing either 5 HT1B or 5 HT1D receptors , it was shown that 5 HT moduline prevents the binding of [ 3H ] 5 HT to 5 HT1B as well as to 5 HT1D receptors with similar biochemical characteristics : the IC 50 of the peptide was 1 . 2x10 ( 12 ) M for 5 HT1B and 9x10 ( 13 ) M for 5 HT1D receptors . ^^^ The observed effect corresponds to a marked decrease of the maximal binding for [ 3H ] 5 HT on 5 HT1B ( 51 . 2 + / 1 % ) as well as 5 HT1D binding ( 47 . 2 + / 7 . 7 % of the control binding ) whereas the affinity of 5 HT is increased by a factor close to 3 . ^^^ The interaction of the peptide was also studied on the functional activity related to the stimulation of the receptors as measured by the increase in [ 35S ] GTPgammaS binding reflecting the coupling of the receptor to the G protein . 5 HT moduline yields an antagonistic effect on the 5 HT induced coupling with a corresponding IC 50 = 1 . 2 + / 0 . 7x10 ( 12 ) M for 5 HT1B and 9 . 8 + / 4 . 0x10 ( 12 ) M for 5 HT1D receptors , respectively . ^^^ The present results demonstrate that 5 HT moduline interacts with 5 HT1D as well as 5 HT1B receptors and possesses a non competitive antagonistic activity , likely corresponding to its role of endogenous allosteric modulator , specific for both 5 HT1B and 5 HT1D receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The results suggest that 5 HT2A receptors mediate vasoconstriction in perinatal vessels whilst the 5 HT1D or 5 HT1B receptor contributes in adult rabbit vessels . ^^^ The 5 HT1D or 5 HT1B receptor mediates NO dependent vasodilation in vessels from rabbits at 4 days of age whilst 5 HT 7 receptors mediate NO independent vasodilation by 7 days . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Co localization of 5 HT1B and 5 HT1D receptor mRNA in serotonergic cell bodies in guinea pig dorsal raph nucleus : a double labeling in situ hybridization histochemistry study . ^^^ In order to provide further details on the cellular localization of 5 HT1B and 5 HT1D receptor mRNA in the dorsal raph nucleus , we performed , in the same sections of guinea pig dorsal raph nucleus , double labeling in situ hybridization histochemistry for : ( 1 ) 5 HT1B receptor mRNA and 5 HT1D receptor mRNA , ( 2 ) 5 HT1B receptor mRNA and 5 HT transporter ( 5 HTT ) mRNA as marker for serotonergic neurons and ( 3 ) 5 HT1D receptor mRNA and 5 HTT mRNA . ^^^ The 5 HT1B receptor mRNA was present in all cells containing 5 HT1D receptor mRNA . ^^^ Similarly , both 5 HT1B and 5 HT1D receptor mRNA was present in all 5 HTT mRNA positive cells . ^^^ The present study demonstrates that 5 HT1B and 5 HT1D receptor mRNA is co localized in serotonergic cell bodies of the guinea pig dorsal raph nucleus . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Reverse transcriptase polymerase chain reaction ( RT PCR ) revealed expression of 5 HT1A , 5 HT1B , 5 HT1D , 5 HT1F , 5 HT2A , 5 HT2B , 5 HT2C , 5 HT5B , 5 HT 6 and 5 HT 7 receptor mRNAs in astrocytes derived from 2 day old rats and cultured for 10 12 days . ^^^ The functional expression of 5 HT 1 receptor subtypes was investigated by measuring the ability of 5 HT 1 receptor agonists : 8 OH DPAT ( 5 HT1A receptors ) , RU 24969 ( 5 HT1A , 5 HT1B , 5 HT1D , and 5 HT1F receptors ) or sumatriptan ( 5 HT1B , 5 HT1D , and 5 HT1F receptors ) to modulate forskolin or isoproterenol stimulated cAMP production . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Zolmitriptan is a selective agonist of 5 HT1B / D receptors . 5 HT1B receptors are concentrated in the wall of the cranial extracerebral arteries . 5 HT1D receptors are located on the trigeminal terminals which receive pain from the leptomeningeal vessels . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
RT PCR analysis of RNA isolated from embryonic sensory neurons in culture confirmed the expression of 5 HT1B , 5 HT1D and 5 HT2A receptor mRNA . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The effects of 5 HT1A , 5 HT1B and 5 HT1D receptor agonists on trigeminal nociceptive neurotransmission in anaesthetized rats . ^^^ Brain penetrant , triptan 5 HT1B / 1D receptor agonists may therefore mediate their central trigeminal anti nociceptive action in the rat via 5 HT1D , but not 5 HT1B or 5 HT1A , receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The canine external carotid vasoconstrictor 5 HT 1 receptor : blockade by 5 HT1B ( SB 224289 ) , but not by 5 HT1D ( BRL 15572 ) receptor antagonists . ^^^ Treatment with the selective 5 HT1B receptor antagonist SB 224289 ( 2 , 3 , 6 , 7 tetrahydro 1 ' methyl 5 [ 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazo l 3 yl ) biphenyl 4 carbonyl ] furo [ 2 , 3f ] indole 3 spiro 4 ' piperidine hydrochloride ; 30 300 microg / kg , i . v . ) produced a potent , specific and dose dependent blockade of this response , whereas the selective 5 HT1D receptor antagonist BRL 15572 ( 1 ( 3 chlorophenyl ) 4 [ 3 , 3 diphenyl ( 2 ( S , R ) hydroxypropanyl ) piperazine ] hydrochloride ; 30 300 microg / kg , i . v . ) was ineffective . ^^^ It is concluded that mainly 5 HT1B , but not 5 HT1D receptors mediate the canine external carotid vasoconstriction by 5 HT and sumatriptan . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Activation of recombinant h 5 HT1B and h 5 HT1D receptors stably expressed in C 6 glioma cells produces increases in Ca2+ dependent K+ current . ^^^ The putative coupling between stably expressed recombinant h 5 HT1B or h 5 HT1D receptors and K+ channels which regulate excitability was investigated in C 6 glioma cells . ^^^ Outward K+ currents ( IK ) were examined in nontransfected C 6 glioma cells and in cells expressing cloned h 5 HT1B or h 5 HT1D receptors using the patch clamp technique in the whole cell configuration . ^^^ In C 6 glioma cells expressing either recombinant h 5 HT1B or h 5 HT1D receptors , sumatriptan similarly increased IK in a concentration dependent manner ( maximum increase 19 . 4+ / 7 . 2 % , n=8 , P < 0 . 05 and 25 . 1+ / 3 . 9 % , n=6 , P < 0 . 001 , respectively ) with EC 50 values ( geometric mean with 95 % confidence intervals in parentheses ) of 56 . 3 nM ( 7 . 9 140 nM ) and 68 . 7 nM ( 16 120 nM ) , respectively . ^^^ Sumatriptan failed to elicit increases in IK in non transfected cells , confirming a specific involvement of the respective membrane h 5 HT1B and h 5 HT1D receptors in transfected C 6 cells . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Using a blinded methodology , animals were injected with normal saline , vehicle , or one of seven serotonin antagonists given at a dose that maintains serotonin receptor subtype specificity : WAY 100135 ( 5 HT1A ) , methiothepin mesylate ( 5 HT1B / 1D / 2 ) , mesulergine hydrochloride ( 5 HT2A / 2B ) , GR 127935 ( 5 HT1D ) , SR 46349 ( 5 HT 2 ) , ondansetron ( 5 HT 3 ) , or GR 125487 ( 5 HT 4 ) . ^^^ CONCLUSIONS : 5 HT1B , 5 HT2A / 2B , and possibly 5 HT1D receptor subtypes likely play a role in posthypoxic myoclonus . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Preferential expression of 5 HT1D over 5 HT1B receptors during murine embryonic development . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
H ] 5 HT binding to cloned human , dog , and rat 5 HT1D and 5 HT1B receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Sumatriptan is an agonist at 5 HT1D and 5 HT1B receptor subtypes , and effective in treating migraine pain and associated symptoms . ^^^ Recently , selective 5 HT1F agonists have been proposed for the treatment of migraine , without the side effects associated with the present 5 HT1D and 5 HT1B receptor agonists . ^^^ Thus , agents that modulate 5 HT1B , 5 HT1D , 5 HT1F and 5 HT2B receptors either have or may have clinical utility in the therapy of migraine headache . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Using a series of 5 HT1B / 1D receptor agonists ( sumatriptan , zolmitriptan , CP 122 , 288 , L 741 , 519 and L 741 , 604 ) , some with high affinity for 5 HTIF receptors and the non selective 5 HT receptor agonists 5 HT and 5 CT , we compared the vasoconstrictor potency of these drugs in human isolated middle meningeal artery with their affinities at cloned human 5 HT1B , 5 HT1D and 5 HT1F receptors expressed in CHO cell lines . ^^^ There was a significant correlation between vasoconstrictor potency and 5 HT1B receptor affinity ( r=0 . 93 , P=0 . 002 ) but not with 5 HT1D or 5 HT1F receptor affinity ( r=0 . 74 , P=0 . 06 ; r= 0 . 31 , P= 0 . 49 , respectively ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Dimerization of sumatriptan increased the binding affinity for h 5 HT1B ( pKi : 9 . 22 vs . 7 . 79 for sumatriptan ) , h 5 HT1D ( 9 . 07 vs . 8 . 08 ) and also h 5 HT1A receptors ( 7 . 80 vs . 6 . 40 ) , while the binding affinity for h 5 ht1E ( 6 . 67 vs . 6 . 19 ) and h 5 ht1F ( 7 . 37 vs . 7 . 78 ) receptors was not affected . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Pharmacological diversity between native human 5 HT1B and 5 HT1D receptors sited on different neurons and involved in different functions . ^^^ The releases of [ 3H ] 5 hydroxytryptamine ( [ 3H ] 5 HT ) and of endogenous glutamic acid and their modulation through presynaptic h 5 HT1B autoreceptors and h 5 HT1D heteroreceptors have been investigated in synaptosomal preparations from fresh neocortical samples obtained from patients undergoing neurosurgery . ^^^ The inhibition by 5 HT of the K+ ( 15 mM ) evoked overflow of [ 3H ] 5 HT was antagonized by the 5 HT1B / 5 HT1D receptor ligand GR 127935 , which was ineffective on its own ; this drug was previously found to behave as a full agonist at the h 5 HT1D heteroreceptor regulating glutamate release . ^^^ The recently proposed selective h 5 HT1B receptor ligand SB 224289 also prevented the effect of 5 HT at the autoreceptor , being inactive on its own ; in contrast , SB 224289 , at 1 microM , was unable to interact with the h 5 HT1D heteroreceptor . ^^^ The selective 5 HT1A receptor antagonist ( + ) WAY 100135 , previously found to be an agonist at the h 5 HT1D heteroreceptor regulating glutamate release , could not interact with the h 5 HT1B autoreceptor when added at 1 microM . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Sumatriptan ' s effects might be mediated by 5 HT1B , 5 HT1D or 5 HT1F receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Naratriptan , launched by Glaxo Wellcome under the trade name Naramig , is a potent and selective agonist of 5 HT1B and 5 HT1D vascular receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The involvement of phospholipase D ( PLD ) in the 5 hydroxytryptamine 5 HT1B / 5 HT1D signalling pathway was assessed in the rabbit isolated mesenteric artery . 2 . ^^^ These characteristics are identical to the profile for 5 HT1B / 5 HT1D receptor evoked contraction in vascular smooth muscle cells , suggesting a role for PLD in this response to 5 HT . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
RESULTS : By RT PCR , 5 HT1b , 5 HT2A and 5 HT2B mRNAs were detected in all of the 14 patients . 5 HT1A , 5 HT1D , and 5 HT1E mRNAs were detected in only some patients . ^^^ By ribonuclease protection assay , 5 HT1B and 5 HT2A signals were detected in all patients examined , but neither 5 HT1A , 5 HT1D nor 5 HT2B signal was detected in any patient . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Characterisation of the 5 HT receptor binding profile of eletriptan and kinetics of [ 3H ] eletriptan binding at human 5 HT1B and 5 HT1D receptors . ^^^ Eletriptan , like sumatriptan , zolmitriptan , naratriptan and rizatriptan had highest affinity for the human 5 HT1B , 5 HT1D and putative 5 ht1f receptor . ^^^ Kinetic studies comparing the binding of [ 3H ] eletriptan and [ 3H ] sumatriptan to the human recombinant 5 HT1B and 5 HT1D receptors expressed in HeLa cells revealed that both radioligands bound with high specificity ( > 90 % ) and reached equilibrium within 10 15 min . ^^^ However , [ 3H ] eletriptan had over 6 fold higher affinity than [ 3H ] sumatriptan at the 5 HT1D receptor ( K ( D ) ) : 0 . 92 and 6 . 58 nM , respectively ) and over 3 fold higher affinity than [ 3H ] sumatriptan at the 5 HT1B receptor ( K ( D ) : 3 . 14 and 11 . 07 nM , respectively ) . ^^^ These data indicate that eletriptan is a potent ligand at the human 5 HT1B , 5 HT1D , and 5 ht1f receptors and are consistent with its potent vasoconstrictor activity and use as a drug for the acute treatment of migraine headache . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The expression of 5 HT1B or 5 HT1D receptor protein was studied using subtype selective antibodies and standard immunocytochemical techniques . ^^^ RT PCR products corresponding to the human 5 HT2A , 5 HT1B and 5 HT1F receptors were expressed in high levels , mRNAs coding for 5 HT 7 , 5 HT1A and 5 HT1D receptors were only weakly expressed . ^^^ In coronary arteries there was a differential expression of 5 HT1B versus 5 HT1D receptor mRNAs , with 5 HT1B mRNAs being found in greater abundance . ^^^ Dense 5 HT1B immunoreactivity was detected on smooth muscle layer within coronary artery , however , 5 HT1D immunoreactivity was not detected . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Investigation of the role of 5 HT1B and 5 HT1D receptors in the sumatriptan induced constriction of porcine carotid arteriovenous anastomoses . 1 . ^^^ The recent availability of silent antagonists selective for the 5 HT1B ( SB 224289 ) and 5 HT1D ( BRL 15572 ) receptor led us to further analyse the nature of receptors involved . 2 . ^^^ The results indicate that sumatriptan constricts porcine carotid arteriovenous anastomoses primarily via 5 HT1B , but not via 5 HT1D receptors . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Both the 5 HT1D and 5 HT1B receptors are implicated in migraine pathophysiology . ^^^ Recently isochromans have been discovered to bind primate 5 HT1D receptors with much higher affinity than 5 HT1B receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We studied the effects of PNU 109291 [ ( S ) ( ) 1 [ 2 [ 4 ( 4 methoxyphenyl ) 1 piperazinyl ] ethyl ] N methyl isoc hroman 6 carboxamide ] , a receptor agonist showing 5000 fold selectivity for primate 5 HT1D versus 5 HT1B receptors ( Ennis et al . , J . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Actions of roxindole at recombinant human dopamine D 2 , D 3 and D 4 and serotonin 5 HT1A , 5 HT1B and 5 HT1D receptors . ^^^ The present study determined its affinity and agonist efficacy at recombinant human ( h ) dopamine hD 2 , hD 3 and hD 4 and serotonin ( 5 HT ) h 5 HT1A , h 5 HT1B and h 5 HT1D receptors . ^^^ Further , it displayed high affinity at hS HT1A receptors ( pKi = 9 . 42 ) but modest affinity at 5 HT1B and 5 HT1D receptors ( pKi values 6 . 00 and 7 . 05 , respectively ) . ^^^ Roxindole only weakly stimulated [ 35S ] GTPgammaS binding at 5 HT1B and 5 HT1D receptors ( Emax = 27 . 1 % and 13 . 7 % ) . ^^^ D 2 or D 4 receptors and 5 HT1A vs . 5 HT1B or 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
A novel compound , SB 236057 ( 1 ' ethyl 5 ( 2 ' methyl 4 ' ( 5 methyl 1 , 3 , 4 oxadiazol 2 yl ) biphenyl 4 carbonyl ) 2 , 3 , 6 , 7 tetrahydrospiro [ furo [ 2 , 3 f ] indole 3 , 4 ' piperid ine ] ) has been shown to have high affinity for human 5 hydroxytryptamine1B ( 5 HT1B ) receptors ( pKi = 8 . 2 ) and displays over 75 or more fold selectivity for the human 5 HT1B receptor over other 5 HT receptors , including the human 5 HT1D receptor , and a range of other receptors , ion channels and enzymes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Serotonin 5 HT1B and 5 HT1D receptors form homodimers when expressed alone and heterodimers when co expressed . ^^^ Gene expression studies have shown that there are brain regions where the 5 HT1B and 5 HT1D receptors are co localized and where heterodimerization may occur physiologically . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
F 11356 has subnanomolar affinity for cloned human and nonhuman 5 HT1B and 5 HT1D receptors , and its affinity for 5 HT1A and other 5 HT receptors , including the 5 ht1F subtype , is 50 fold lower and micromolar , respectively . ^^^ In C 6 cells expressing human 5 HT1B or human 5 HT1D receptors , F 11356 was the most potent compound in inhibiting forskolin induced cyclic AMP formation ( pD 2 = 8 . 9 and 9 . 6 ) , and in contrast to tryptamine and derivatives , it produced maximal enhancement of [ 35S ] guanosine 5 ' O ( 3 thio ) triphosphate specific binding equivalent to 5 HT . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Enhancement of 5 HT1B and 5 HT1D receptor antagonist effects on extracellular 5 HT levels in the guinea pig brain following concurrent 5 HT1A or 5 HT re uptake site blockade . ^^^ The aim of the study was to further investigate the autoreceptor roles of the 5 HT1A , 5 HT1B and 5 HT1D receptors in the median vs dorsal raphe nuclei . ^^^ These data demonstrate that to simultaneously increase extracellular 5 HT in both frontal cortex and dorsal hippocampus of the guinea pig brain concurrent 5 HTA1A , 5 HT1B and 5 HT1D receptor blockade is required . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
SB 224289 ( 5 HT1B selective antagonist , 0 . 2 microM ) inhibited sumatriptan induced contractions ( estimated pKB=8 . 4+ / 0 . 1 ) whilst these were unaffected by the 5 HT1D selective antagonist BRL 15572 ( 0 . 5 microM ) suggesting that the 5 HT1B receptor mediates vasoconstriction in this vessel . 4 . ^^^ RT PCR confirmed the presence of substantial amounts of mRNA for the 5 HT2A and 5 HT1B receptor subtypes in these arteries whilst only trace amounts of 5 HT1D receptor message were evident . 5 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The ' triptan ' anti migraine agents ( e . g . sumatriptan , rizatriptan , zolmitriptan naratriptan ) are serotonergic agonists that have been shown to act selectively by causing vasoconstriction through 5 HT1B receptors that are expressed in human intracranial arteries and by inhibiting nociceptive transmission through an action at 5 HT1D receptors on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brain stem sensory nuclei . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Using specific primers for human 5 HT1B , 5 HT1D and 5 HT2A receptor genes , the reverse transcriptase polymerase chain reaction revealed mRNA expression of 5 HT1B and 5 HT2A receptors in the HUA . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Consequently , the present study using in vivo microdialysis was undertaken to ( 1 ) characterize the effects of alpha2D , 5 HT1B and 5 HT1D receptor stimulation or blockade on 5 HT efflux in the FC given the purported regulatory role of these sites on 5 HT release , and ( 2 ) to investigate the ability of risperidone to interfere with these receptors in order to examine their putative role in the facilitatory action or risperidone on cortical 5 HT output . ^^^ The present in vivo biochemical data indicate that the output of 5 HT in the FC is negatively regulated via alpha2D , 5 HT1B and tentatively also via 5 HT1D receptors located in the nerve terminal area . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
RATIONALE : Effective neuroendocrine probes of 5 HT1B and 5 HT1D receptor function may facilitate investigation of the role of these receptor subtypes in the pathophysiology of depression and the mode of action of antidepressant medication . ^^^ A further six healthy men were recruited to an equivalent study to examine the effect of ketanserin ( a 5 HT receptor antagonist with some preference for 5 HT1D over 5 HT1B receptors ) on the growth hormone response to zolmitriptan . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The first of the class , sumatriptan , and the newer triptans ( zolmitriptan , naratriptan , rizatriptan , eletriptan , almotriptan and frovatriptan ) display high agonist activity at mainly the serotonin 5 HT1B and 5 HT1D receptor subtypes . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We have examined 5 HT receptor subtype distribution in cerebral blood vessels by immunocytochemistry with antibodies selective for human 5 HT1B and human 5 HT1D receptors and also studied the contractile effects of a range of 5 HT receptor agonists and antagonists in HCA . 2 Immunocytochemistry of cerebral arteries showed dense 5 HT1B receptor immunoreactivity ( but no 5 HT1D receptor immunoreactivity ) within the smooth muscle wall of the HCA . ^^^ There was a significant correlation between vasoconstrictor potency and 5 HT1B and 5 HT1D receptor affinity , but not with 5 HT1A , 5 ht1F or 5 HT 2 receptor affinity . 4 The 5 HT1B / 1D receptor antagonist GR 55562 ( 10 7 10 6 M ) inhibited the contractile responses to sumatriptan and 5 CT in a competitive manner with a pKB value for GR 55562 of 7 . 4 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Effect of chronic paroxetine treatment on 5 HT1B and 5 HT1D autoreceptors in rat dorsal raphe nucleus . ^^^ This study reports the effect of chronic paroxetine ( 10 mg / kg p . o . , 21 days ) on 5 HT1B and 5 HT1D autoreceptors controlling stimulated 5 HT efflux in slices of rat dorsal raphe nucleus . ^^^ Electrically evoked 5 HT ( 10 pulses , 200 Hz , 0 . 1 ms , 10 mA ) was measured using fast cyclic voltammetry . 5 HT efflux was inhibited by CP 93129 ( 10 nM 10 microM ) and by sumatriptan ( 1 nM 1 microM ) agonists at 5 HT1B and 5 HT1D receptors , respectively . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
A series of 5 ( 2 or 3 thienyl ) tryptamine derivatives ( 9 ) has been synthesized and shown to be potent and selective 5 HT1D versus 5 HT1B receptor agonists and , therefore , potential treatments for migraine . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In this context , two discoveries have been especially important : 1 ) these anti migraine drugs are specifically recognized by three main types of serotonin receptors ( 5 HT1B , 5 HT1D , and 5 HT1F ) ; and 2 ) these receptors are present in the meninges , where they are expressed by both smooth muscle cells and / or endothelial cells of the vascular wall and / or the perivascular trigeminal to be deleted axon terminals . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Within this framework , it has been shown that the external carotid vasoconstrictor response to 5 HT in the dog is mediated by ' 5 HT 1 like ' receptors , which being blocked by the 5 HT1B / 1D receptor antagonist GR 127935 , resemble 5 HT1B / 1D ( previously called 5 HT1D beta / 1D alpha ) receptors . ^^^ It was proposed that these receptors could belong to the 5 HT1B , rather than the 5 HT1D , subtype on the basis of their resistance to blockade by a high dose of ritanserin ( a potential 5 HT1D receptor antagonist ) and the presence of mRNA for 5 HT1B ( 5 HT1D beta ) receptors , but not for 5 HT1D ( 5 HT1D alpha ) receptors , in vascular smooth muscle . ^^^ With the advent of subtype selective antagonists it was subsequently shown that external carotid vasoconstriction to 5 HT and sumatriptan is dose dependently antagonized by the selective 5 HT1B receptor antagonist SB 224289 ( 2 , 3 , 6 , 7 tetrahydro 1 ' methyl 5 [ 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) biphenyl 4 carbonyl ] furo [ 2 , 3 f ] indole 3 spiro 4 ' piperidine hydrochloride ) , whereas the selective 5 HT1D receptor antagonist BRL 15572 ( 1 ( 3 chlorophenyl ) 4 [ 3 , 3 diphenyl ( 2 ( S , R ) hydroxypropanyl ) piperazine ] hydrochloride ) was ineffective . ^^^ These findings represent the first in vivo evidence showing that vascular constriction induced by 5 HT and sumatriptan is mediated primarily via 5 HT1B , but not 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Central penetration and increased receptor affinity and selectivity for the neuronal ( 5 HT1D ) receptor also combine to allow for lower total oral dosing ( i . e . , unit doses of 15 mg or less compared with 50 300 mg doses of sumatriptan ) and reduced peripheral exposure to the coronary vasoconstrictor ( 5 HT1B ) receptor . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The involvement of 5 HT1B and 5 HT1D receptors seems highly unlikely since antagonists at 5 HT1B ( SB 224289 ) and 5 HT1D ( BRL 15572 ) receptors ( both at 300 microg / kg ) were ineffective . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
AIM : To study the relationship between the vasoconstrictor effect to 5 hydroxytryptamine ( 5 HT ) and the expression of 5 HT1B and 5 HT1D ) receptors in pulmonary arteries ( PA ) from normal and pulmonary hypertensive ( PHT ) rats . ^^^ Concentration response curves of 5 HT induced pulmonary vasoconstriction were established and semiquantitative RT PCR was performed to identify mRNA expression of 5 HT1B and 5 HT1D receptors in rat PA . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In addition , it was not associated with changes in the function of 5 HT1D and 5 HT1B autoreceptors and of alpha 2 adrenergic heteroreceptors on 5 HT neurons , nor of that of alpha 2 adrenoceptors on norepinephrine terminals . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The role of 5 HT1B and 5 HT1D receptors in the selective inhibitory effect of naratriptan on trigeminovascular neurons . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In resistance arteries from Sprague Dawley rats , the 5 HT2A receptor mediated contraction ; agonists of the 5 HT1B , 5 HT1D , 5 HT1F , and 5 HT2B receptor were inactive . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Involvement of 5 HT1B and 5 HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery . 1 . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
An immunocytochemical investigation of human trigeminal nucleus caudalis : CGRP , substance P and 5 HT1D receptor immunoreactivities are expressed by trigeminal sensory fibres . 5 HT1D ( but not 5 HT1B ) receptor immunoreactivity ( i . r . ) can be detected on trigeminal fibres within the spinal trigeminal tract of the human brainstem . ^^^ This suggests that 5 HT1D receptors can regulate the release of CGRP and substance P and may be relevant to the clinical effectiveness of 5 HT1B / 1D receptor agonists in the treatment of migraine and other cranial pain syndromes . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The action of 5 hydroxytryptamine ( 5 HT1B / 1D ) agonists so called triptans on receptors located in meningeal arteries ( 5 HT1B ) and trigeminovascular fiber endings ( 5 HT1D ) has an inhibitory effect on this neurogenic inflammation . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In line with the vascular and neurogenic theories of migraine , all triptans produce selective carotid vasoconstriction ( via 5 HT1B receptors ) and presynaptic inhibition of the trigeminovascular inflammatory responses implicated in migraine ( via 5 HT1D / 5 ht1F receptors ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
PNU 142633 binds with a Ki of 6 nm at the human 5 HT1D receptor and a Ki of > 18 000 nm at the human 5 HT1B receptor . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Eletriptan has 6 fold greater affinity for the 5 HT1D receptor than sumatriptan , and a 3 fold greater affinity for the 5 HT1B receptor [ 249570 ] . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Within DRG neurons , mRNAs for 5 HT1B , 5 HT1D , 5 HT2A , 5 HT2B , 5 HT3B and 5 HT 4 receptors were readily detected in small ( < 25 microm ) , medium ( 25 45 microm ) and large ( > 45 microm ) diameter neurons . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Ergotamine and dihydroergotamine are highly potent at the 5 HT1B and 5 HT1D antimigraine receptors and , as a consequence , the plasma concentrations that are necessary to produce the appropriate therapeutic and physiologic effects are very low . ^^^ In acute migraine treatment , their mechanisms of action involve constricting the pain producing intracranial extracerebral blood vessels at the 5 HT1B receptors and inhibiting the trigeminal neurotransmission at the peripheral and central 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We analyzed the expression of three types of serotonin receptors : 5 HT1B , 5 HT2C and 5 HT1D by reverse transcription polymerase chain reaction in mouse unfertilized oocytes and preimplantation embryos from zygotes to the blastocyst stage in vivo . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
I . v . continuous infusions of the agonists 5 carboxamidotryptamine ( 5 CT ; 5 HT1 / 7 and recombinant 5 ht5A / 5B ) , CP 93129 ( r 5 HT1B ) , sumatriptan ( 5 HT1B / 1D ) , PNU 142633 ( 5 HT1D ) and ergotamine ( 5 HT1B / 1D and recombinant 5 ht5A / 5B ) mimicked the above sympatho inhibition to 5 HT . ^^^ Interestingly , 5 CT induced cardiac sympatho inhibition was abolished by methiothepin , the cocktail of antagonists / inhibitors , GR 127935 or the combination of SB 224289 ( 5 HT1B ) plus BRL 15572 ( 5 HT1D ) , but remained unchanged when SB 224289 or BRL 15572 were given separately . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
These factors were 5 HT1B and 5 HT1D receptor activities , the pharmacokinetic elimination half life of each triptan , and the clinical efficacy of each compound , determined by the proportion of patients with headache relief and the therapeutic gain over placebo . ^^^ There was also a significant inverse correlation between 5 HT1B receptor potency and recurrence ( r = 0 . 68 , P = . 034 ) , but 5 HT1D receptor potency was not correlated with recurrence ( r = 0 . 20 , P = . 54 ) . ^^^ In addition , the binding affinities for the 5 HT1B and 5 HT1D receptors were not correlated to headache recurrence . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Further characterization of the 5 HT 1 receptors mediating cardiac sympatho inhibition in pithed rats : pharmacological correlation with the 5 HT1B and 5 HT1D subtypes . ^^^ More recently , it has been shown that this cardiac sympatho inhibitory response to 5 HT , mediated by prejunctional 5 HT 1 receptors as well as putative 5 ht5A / 5B receptors , is mimicked dose dependently by the agonists CP 93 , 129 ( r 5 HT1B ) , sumatriptan ( 5 HT1B / 1D ) and PNU 142633 ( 5 HT1D ) . ^^^ The 5 HT 1 receptors producing cardiac sympatho inhibition in pithed rats thus display the pharmacological profile of the 5 HT1B and 5 HT1D receptor subtypes . . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
We also investigated GR 46611 ( 3 [ 3 ( 2 dimethylaminoethyl ) 1H indol 5 yl ] N ( 4 methoxybenzyl ) acrylamide ) , which has agonist activity predominantly at 5 HT1B and 5 HT1D receptors but also at the 5 HT1A receptor . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
RT PCR studies in guinea pig iliac arteries showed a strong signal for the 5 HT1B receptor while expression of 5 HT1D and 5 HT1F receptors was not detected in any sample . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In line with the vascular and neurogenic theories of migraine , all triptans produce selective carotid vasoconstriction ( via 5 HT1B receptors ) and presynaptic inhibition of the trigeminovascular inflammatory responses implicated in migraine ( via 5 HT1D / 5 ht1F receptors ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The depression of the monosynaptic reflex was antagonized by GR 127935 ( N [ methoxy 3 ( 4 methyl l piperazinyl ) phenyl ] 2 ' methyl 4 ' ( 5 methyl 1 , 2 , 4 oxadiazol 3 yl ) [ 1 , 1 biphenyl ] 4 carboxamide ; 5 HT1B / 1D receptor antagonist ) and BRL 15572 ( 3 [ 4 ( 4 chlorophenyl ) piperazin 1 yl ] 1 , 1 diphenyl 2 propanol ; 5 HT1D receptor antagonist ) but not by isamoltane ( 5 HT ( 1B ) receptor antagonist ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The selective 5 HT1B antagonist SB 224289 inhibited GTI and CP 93129 stimulated [ 35S ] GTPgammaS binding in basal ganglia and substantia nigra , while coincubation with BRL 15572 ( selective 5 HT1D antagonist ) did not result in any significant change . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Triptans are agonists at 5 HT1B and 5 HT1D ( where 5 HT is 5 hydroxytryptamine ; serotonin ) receptors and cause vasoconstriction of isolated blood vessels . ^^^ The ratio of Cmax / EC50 was calculated . 5 HT1B and 5 HT1D receptors were visualized by immunohistochemical techniques in coronary arteries . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The template was N substituted to give a series of compounds showing binding to human cloned 5 HT1A , 5 HT1B and 5 HT1D receptors with pKi ' s greater than 9 and selectivities up to 1000 fold against other serotonin , dopamine and adrenergic receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The effects of 5 HT were mimicked by 5 carboxamidotryptamine ( a 5 HT 1 receptor agonist ) and L 694 247 ( a selective 5 HT1D receptor agonist ) , but not by 8 hydroxy 2 dipropylaminotetralin ( a 5 HT1A receptor agonist ) , CGS 12066B ( a 5 HT1B receptor agonist ) , alpha methyl 5 HT ( a 5 HT 2 receptor agonist ) , 1 ( 3 chlorophenyl ) piperazine ( a 5 HT2C receptor agonist ) or 1 phenylbiguanide ( a 5 HT 3 receptor agonist ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
PROCEDURE : Amounts of mRNA coding for 7 subtypes of 5 HTRs ( 5 HT1A , 5 HT1B , 5 HT1D , 5 HT1F , 5 HT2A , 5 HT2B , and 5 HT 4 ) were measured by quantitative real time reverse transcriptase PCR assay . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
At one end of a spectrum is combination therapies that maintain the benefits associated with SSRIs but attempt to either improve efficacy or reduce side effects by adding additional mechanisms ( 5 HT1A , 5 HT1B , 5 HT1D , 5 HT2C , alpha 2A ) . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
The current studies describe the in vitro profile of SB 649915 ( 6 [ ( 1 { 2 [ ( 2 methylquinolin 5 yl ) oxy ] ethyl } piperidin 4 yl ) methyl ] 2H 1 , 4 benzoxazin 3 ( 4H ) one ) , a novel compound which has high affinity for human recombinant 5 HT1A , 5 HT1B and 5 HT1D receptors ( pKi values of 8 . 6 , 8 . 0 , 8 . 8 , respectively ) and the human recombinant 5 HT transporter ( pKi value of 9 . 3 ) . ^^^ SB 649915 also displays high affinity for rat , guinea pig , mouse and marmoset native tissue 5 HT1A , 5 HT1B and 5 HT1D receptors and rat native tissue 5 HT transporters ( pKi values > or=7 . 5 ) . ^^^ In functional [ 35S ] GTPgammaS binding studies , SB 649915 ( up to 1 microM ) does not display intrinsic activity in HEK 293 cells expressing human recombinant 5 HT1A receptors but acts as a partial agonist at human recombinant 5 HT1B and 5 HT1D receptors with intrinsic activity values of 0 . 3 and 0 . 7 , respectively , as compared to the full agonist 5 HT . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
In vitro pharmacology experiments showed that the 5 hydroxytryptamine ( 5 HT ) type 1B and 1D receptor agonists , eletriptan , naratriptan , rizatriptan , sumatriptan , and zolmitriptan , induced vasoconstriction in the thoracic blood vessels from 38 % to 57 % of the patients . 5 carboxamidotryptamine ( 5 CT ) and sumatriptan elicited a vasoconstriction that was antagonized by the 5 HT1B receptor antagonist SB 224289 , whereas the 5 HT1D receptor antagonist BRL 115572 had no effect . 5 HT induced a contraction that was inhibited by the 5 HT2A receptor antagonist ketanserin . 5 HT2A , 5 HT1B , and 5 HT1D receptor mRNA levels were detected by real time PCR in all blood vessels studied . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
PCR with cDNAs derived from reverse transcribed blood vessel mRNA suggested the expression of the 5 HT1B , 5 HT1D and 5 HT 4 receptors , the latter being highly homologous to the human one . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Donitriptan , but not sumatriptan , inhibits capsaicin induced canine external carotid vasodilatation via 5 HT1B rather than 5 HT1D receptors . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
Double immunostaining of rat cerebral arteries with endothelial cell or smooth muscle cell specific antibodies verified that an increase in ETB , 5 hydrotryptamine ( 5 HT1B ) , and 5 HT1D receptor expression occurs in smooth muscle cells . ^^^
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA
Interacting proteins: P28221 and P28222	Pubmed	SVM Score :0.0
NA