1,1-DIPHENYL-3-DIALKYLAMINO-1-SILACYCLOPENTANE DERIVATIVES - A NEW CLASS OF POTENT AND SELECTIVE 5-HT2A ANTAGONISTS

被引：14

作者：

DAMOUR, D

BARREAU, FM

DUTRUCROSSET, G

DOBLE, A

PIOT, O

MIGNANI, S

机构：

[1] RHONE-POULENC RORER S.A. Centre de Recherches de Vitry-Alfortville, 94403 Vitry-sur-Seine Cedex

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 03期

关键词：

D O I：

10.1016/0960-894X(94)80007-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 1,1-diphenyl-3-dialkylamino-1-silacyclopentanes was synthesized, and most compounds demonstrated moderate to high affinity for the 5-HT2A receptor. A member of this series, compound 1p displays potent antagonist activity after oral administration against both mescaline and DOI-induced head-twitches in mice and rats, with a long duration of action. The dextrorotatory isomer (+)-1p is highly more potent than the levorotatory isomer (-)-1p in in vitro and in in vivo assays.

引用

页码：415 / 420

页数：6

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