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Titolo:
SELECTIVE ANTAGONISM OF HUMAN 5-HT1D AND 5-HT1B RECEPTOR-MEDIATED RESPONSES IN STABLY TRANSFECTED C6-GLIAL CELLS BY KETANSERIN AND GR-127,935
Autore:
PAUWELS PJ; COLPAERT FC;
Indirizzi:
CTR RECH PIERRE FABRE,CELLULAR & MOLEC NEUROBIOL LAB,17 AVE JEAN MOULIN F-81106 CASTRES FRANCE
Titolo Testata:
European journal of pharmacology
fascicolo: 1-2, volume: 300, anno: 1996,
pagine: 141 - 145
SICI:
0014-2999(1996)300:1-2<141:SAOH5A>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
ARTERY;
Keywords:
5-HT1D RECEPTOR ANTAGONIST; KETANSERIN; 5-HT1B RECEPTOR ANTAGONIST; GR 127,935; 5-HT1D RECEPTOR, HUMAN, CLONED; 5-HT1B RECEPTOR, HUMAN, CLONED; CAMP FORMATION; (TRANSFECTED RAT C6-GLIAL CELL LINE);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
15
Recensione:
Indirizzi per estratti:
Citazione:
P.J. Pauwels e F.C. Colpaert, "SELECTIVE ANTAGONISM OF HUMAN 5-HT1D AND 5-HT1B RECEPTOR-MEDIATED RESPONSES IN STABLY TRANSFECTED C6-GLIAL CELLS BY KETANSERIN AND GR-127,935", European journal of pharmacology, 300(1-2), 1996, pp. 141-145

Abstract

The antagonist effects of ketanserin and yl-4'-(5-methyl-1,2,4)oxadiazol-3-yl)-biphenyl-[4- carboxylic acid 4-methoxy-3-(4-methyl-piperazin- 1-yl)-phenyl]-amide (GR 127,935) were compared on naratriptan-induced inhibition of cAMP formation in C6-glial cell lines stably expressing human 5-HT1D or 5-HT1B receptor sites. Ketanserin demonstrated potent (pA(2) : 7.76), competitive antagonism of naratriptan-induced inhibition of forskolin (100 mu M)-stimulated cAMP formation in C6-glial/5-HT1D cells. Whereas GR 127,935 was ineffective as an antagonist in these cells, it produced an intrinsic activity (pEC(50) : 6.98) that was sensitive to ketanserin (10 mu M) blockade. Unlike ketanserin, GR 127,935 potently antagonised the naratriptan response in C6-glial/S-HT1B cells while also depressing the maximum response. The differential antagonist effects of ketanserin and GR 127,935 on naratriptan responses elicited in C6-glial/S-HT1D and C6-glial/5-HT1B cells demonstrate these compounds do selectively block human 5-HT1D and 5-HT1B receptors, respectively.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 04:18:38