当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Selective antagonism of human 5-HT1D and 5-HT1B receptor-mediated responses in stably transfected C6-glial cells by ketanserin and GR 127,935.

Selective antagonism of human 5-HT1D and 5-HT1B receptor-mediated responses in stably transfected C6-glial cells by ketanserin and GR 127,935.

Abstract：

: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 C6-glial cell lines stably expressing human 5-HT1D or 5-HT1B receptor sites. Ketanserin demonstrated potent (pA2: 7.76), competitive antagonism of naratriptan-induced inhibition of forskolin (100 microM)-stimulated cAMP formation in C6-glial/5-HT1D cells. Whereas GR 127,935 was ineffective as an antagonist in these cells, it produced and intrinsic activity (pEC50: 6.98) that was sensitive to ketanserin (10 microM) blockade. Unlike ketanserin, GR 127,935 potently antagonised the naratriptan response in C6-glial/5-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/5-HT1D and C6-glial/5-HT1B cells demonstrate these compounds do selectively block human 5-HT1D and 5-HT1B receptors, respectively.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Pauwels PJ,Colpaert FC

doi

10.1016/0014-2999(96)00011-8

subject

Has Abstract

pub_date

1996-04-04 00:00:00

pages

141-5

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(96)00011-8

journal_volume

300

pub_type

杂志文章

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