BLOCKADE OF HUMAN ATRIAL 5-HT(4) RECEPTORS BY GR-113808

被引：44

作者：

KAUMANN, AJ ^{[1
]}

机构：

[1] AFRC,BABRAHAM INST HUMAN PHARMACOL,CAMBRIDGE CB2 4AT,ENGLAND

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1993年 / 110卷 / 03期

关键词：

HUMAN ATRIUM; 5-HT(4) RECEPTORS; 5-HYDROXYTRYPTAMINE; GR-113808;

D O I：

10.1111/j.1476-5381.1993.tb13937.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1 The mode of antagonism of 5-hydroxytryptamine (5-HT)-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist GR 113808 ({1-[2-methlylsulphonylamino ethyl]-4-piperidinyl}methyl 1-methyl-1H-indole-3-carboxylate) was investigated on isolated preparations of human right atrium. 2 GR 113808 caused concentration-dependent (2-100 nM) surmountable antagonism of the effects of 5-HT with a pK(B) (M) of 8.8. 3 The affinity of GR 113808 for human atrial 5-HT4 receptors, together with its high selectivity for 5-HT4 receptors comprise useful properties for investigating the question of 5-HT4 receptor subtypes.

引用

页码：1172 / 1174

页数：3

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