5-HYDROXYTRYPTAMINE STIMULATES CYCLIC-AMP FORMATION IN THE TUNICA MUSCULARIS MUCOSAE OF THE RAT ESOPHAGUS VIA 5-HT(4) RECEPTORS

被引：41

作者：

FORD, APDW

BAXTER, GS

EGLEN, RM

CLARKE, DE

机构：

[1] Institute of Pharmacology, Syntex Research, Palo Alto, CA 94304

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1992年 / 211卷 / 01期

关键词：

ESOPHAGUS (RAT); 5-HT; (5-HYDROXYTRYPTAMINE; SEROTONIN); 5-HT(4) RECEPTORS; CAMP; BENZAMIDES (SUBSTITUTED); TROPISETRON;

D O I：

10.1016/0014-2999(92)90272-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The nature of 5-HT4 receptor coupling in the tunica muscularis mucosae of the rat oesophagus has been studied. 5-HT and renzapride stimulated cyclic AMP formation concentration dependently, with -log EC50 values of 7.1 and 6.8, respectively. Renzapride, relative to 5-HT, acted as a partial agonist. Tropisetron (ICS 205 930) and a novel 5-HT4 antagonist, SDZ 205 557, inhibited 5-HT-induced cyclic AMP production competitively, with pA2 estimates of 6.7 and 7.7, respectively. These data are consistent with the hypothesis that 5-HT4 receptors mediate relaxation of the smooth muscle cells of the tunica muscularis mucosae of rat oesophagus via activation of adenylyl cyclase.

引用

页码：117 / 120

页数：4

共 14 条

[1] A SINGLE COLUMN METHOD FOR THE ASSAY OF ADENYLATE-CYCLASE [J].