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Titolo:
RECOMBINANT SAPHENOUS-VEIN 5-HT1B RECEPTORS OF THE RABBIT - COMPARATIVE PHARMACOLOGY WITH HUMAN 5-HT1B RECEPTORS
Autore:
WURCH T; PALMIER C; COLPAERT FC; PAUWELS PJ;
Indirizzi:
CTR RECH PIERRE FABRE,CELLULAR & MOL NEUROBIOL LAB,17 AVE JEAN MOULINF-81106 CASTRES FRANCE CTR RECH PIERRE FABRE,CELLULAR & MOL NEUROBIOL LAB F-81106 CASTRES FRANCE
Titolo Testata:
British Journal of Pharmacology
fascicolo: 1, volume: 120, anno: 1997,
pagine: 153 - 159
SICI:
0007-1188(1997)120:1<153:RS5ROT>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN 5-HT1D-ALPHA; SEROTONIN; IDENTIFICATION; 5-HT1D-BETA; ANTAGONISTS; KETANSERIN; BINDING;
Keywords:
RABBIT RECOMBINANT SAPHENOUS VEIN 5-HT1B RECEPTOR; HUMAN 5-HT1B RECEPTOR; CYCLIC AMP; KETANSERIN; RAT C6-GLIAL CELL LINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
T. Wurch et al., "RECOMBINANT SAPHENOUS-VEIN 5-HT1B RECEPTORS OF THE RABBIT - COMPARATIVE PHARMACOLOGY WITH HUMAN 5-HT1B RECEPTORS", British Journal of Pharmacology, 120(1), 1997, pp. 153-159

Abstract

1 The rabbit recombinant saphenous vein 5-hydroxytryptamine,B (rb 5-HT1B) receptor stably transfected in rat C6-glial cells was characterized by measuring adenosine 3':5'-cyclic monophosphate (cyclic AMP) formation upon exposure to various 5-HT receptor ligands. The effects of agonists and antagonists were compared with their effects determined previously at the human cloned 5-HT1B (h 5- HT1B) receptor under similarexperimental conditions. 2 Intact C6-glial cells expressing rb 5-HT1Breceptors exhibited [H-3]-5-carboxamidotryptamine (5-CT) binding sites with a K-d of 0.80 +/- 0.13 nM and a B-max between 225 to 570 fmol mg(-1) protein. The binding affinities of a series of 5-HT receptor ligands determined in a membrane preparation with [H-3]-5-CT or razin-1-yl)phenyl]-3-methyl-4-(4-pyridyl)benzamide (GR 125,743) were similar. With the exception of ketanserin, ligand affinities were comparable to those determined at the cloned h 5-HT1B receptor site. 3 rb 5-HT1B receptors were negatively coupled to cyclic AMP formation upon stimulation with 5-HT agonists. Of the several 5-HT agonists tested, 5-CT was the most potent, the potency rank order being: 5-CT > 5-HT > zolmitriptan > naratriptan > rizatriptan > sumatriptan > R(+)-8-(hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). The maximal responses of these agonists were similar to those induced by 5-HT. The potency of these agonists showed a positive correlation (r(2)=0.87; P<0.002) with their potency at the cloned h 5-HT1B receptor subtype. 4 ethyl-[1,2,4]oxadiazol-3-yl)-biphenyl-4-carboxylic acid -methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide (GR 127,935), methiothepin and ketanserin each behaved assilent, competitive antagonists at rb 5-HT1B receptors; pK(B) values were 8.41, 8.32 and 7.05, respectively when naratriptan was used as anagonist. These estimates accorded with their binding affinities and the potencies found on 5-HT and/or sumatriptan-mediated contraction of isolated rabbit saphenous vein segments. 5 In conclusion, the recombinant saphenous vein 5-HT1B receptor of the rabbit shares important pharmacological similarities with the cloned h 5-HT1B receptor. However, ketanserin is a more potent antagonist of rb 5-HT1B receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/06/20 alle ore 21:37:55