LABELING WITH [I-125]-SB-207710 OF A SMALL 5-HT4 RECEPTOR POPULATION IN PIGLET RIGHT ATRIUM - FUNCTIONAL RELEVANCE

被引：30

作者：

KAUMANN, AJ ^{[1
]}

LYNHAM, JA ^{[1
]}

BROWN, AM ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT PSYCHIAT RES,HARLOW CM19 5AW,ESSEX,ENGLAND

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1995年 / 115卷 / 06期

关键词：

PIGLET RIGHT ATRIUM; 5-HT4 RECEPTOR DENSITY; I-125] SB 207710; TACHYCARDIA; BETA(1) AND BETA(2)-ADRENOCEPTOR DENSITIES;

D O I：

10.1111/j.1476-5381.1995.tb15900.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1 We investigated the affinity of SE 207710 for sinoatrial 5-HT4 receptors and the density of right atrial 5-HT4 receptors with [I-125]-SB 207710 in right atria of new-born piglets. 2 SE 207710 (1-100 nM) antagonized the 5-HT-evoked tachycardia surmountably with a pK(B) of 9.8. 3 [I-125]-SB 207710 (5-1500 pM) labelled a small population of saturable binding sites with a pK(D) of 10.1 and with 5-HT4 receptor characteristics. The density of atrial binding sites with 5-HT4 receptor characteristics was 174 and 22 times lower respectively than those of atrial beta(1)- and beta(2)-adrenoceptors, labelled with (-)-[I-125]-cyanopindolol. 4 We suggest that the small 5-HT4 receptor population may in part explain why the maximal tachycardia caused by 5-HT is smaller than that caused by catecholamines.

引用

页码：933 / 936

页数：4

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