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
收藏
页码：415 / 420
页数：6
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