STEREOSELECTIVE INTERACTION OF MIANSERIN WITH 5-HT3 RECEPTORS

被引：24

作者：

WOOD, MD ^{[1
]}

THOMAS, DR ^{[1
]}

WATKINS, CJ ^{[1
]}

NEWBERRY, NR ^{[1
]}

机构：

[1] UNIV OXFORD,RADCLIFFE INFIRM,SMITHKLINE BEECHAM CTR APPL NEUROPSYCHOBIOL,DEPT CLIN PHARMACOL,OXFORD OX2 6HE,ENGLAND

来源：

JOURNAL OF PHARMACY AND PHARMACOLOGY | 1993年 / 45卷 / 08期

关键词：

D O I：

10.1111/j.2042-7158.1993.tb07094.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The interaction of the enantiomers of mianserin with the 5-HT3 receptor was determined. Using [H-3]granisetron binding, (-)-mianserin was more potent than (+)-mianserin (pK(i) 8.46 and 6.95, respectively). The enantiomers competitively antagonized the depolarizing effect of 5-hydroxytryptamine in the rat vagus nerve preparation (pK(app): (-)-mianserin 8.13, (+)-mianserin 6.58). This stereoselectivity was maintained in-vivo as determined using ex-vivo inhibition of [H-3]granisetron binding. Therefore, in contrast to its enantiomeric selectivity for the 5-HT1C and 5-HT2 receptors, where the (+)-isomer is more potent, the enantiomeric selectivity of mianserin for the 5-HT3 receptor was reversed. This differential selectivity of the enantiomers of mianserin may be useful in elucidating its utility in anxiety states.

引用

页码：711 / 714

页数：4

共 27 条

[1] STEREOSELECTIVE BLOCKADE OF CENTRAL [H-3] 5-HYDROXYTRYPTAMINE BINDING TO MULTIPLE SITES (5-HT1A, 5-HT1B AND 5-HT1C) BY MIANSERIN AND PROPRANOLOL [J].