BLOCKADE OF HUMAN ATRIAL 5-HT4 RECEPTORS BY SB-207710, A SELECTIVE AND HIGH-AFFINITY 5-HT4 RECEPTOR ANTAGONIST

被引：27

作者：

KAUMANN, AJ

GASTER, LM

KING, FD

BROWN, AM

机构：

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

[2] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,HARLOW CM19 5AD,ESSEX,ENGLAND

[3] SMITHKLINE BEECHAM PHARMACEUT,DEPT PSYCHIAT RES,HARLOW CM19 5AD,ESSEX,ENGLAND

来源：

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY | 1994年 / 349卷 / 05期

关键词：

HUMAN ATRIUM; 5-HT4; RECEPTORS; 5-HYDROXYTRYPTAMINE; SB; 207710; 5-HT4 RECEPTOR ANTAGONIST;

D O I：

10.1007/BF00169146

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The mode of antagonism of 5-hydroxytryptamine-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist SB 207710 (1-butyl-4-piperidinyl) methyl 8-amino-7-iodo-1,4-benzodioxan-5-carboxylate) was investigated on isolated preparations of human right atrial appendage. SB 207710 caused concentration-dependent (0.1-10 nmol/l) surmountable antagonism of the effects of 5-hydroxytryptamine with a pK(B) (mol/l) of 10.1. Due to its high selectivity and affinity, SB 207710 could be a powerful tool for the comparison of human atrial 5-HT4 receptors with 5-HT4 receptors of other organs of man and other species.

引用

收藏

页码：546 / 548

页数：3

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