A novel series of N-(hexahydro-1,4-diazepin-6-yl) and N-(hexahydroazepin-3-yl)benzamides with high affinity for 5-HT3 and dopamine D2 receptors

被引：18

作者：

Hirokawa, Y ^{[1
]}

Morie, T ^{[1
]}

Yamazaki, H ^{[1
]}

Yoshida, N ^{[1
]}

Kato, S ^{[1
]}

机构：

[1] Dainippon Pharmaceut Co Ltd, Discovery Res Labs 1, Suita, Osaka 564, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(98)00078-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of benzamides with a hexahydro-1,4-diazepine or hexahydroazepine ring in the amine moiety were prepared, and their binding affinities for 5-HT3 and dopamine D-2 receptors were evaluated. The R isomer of the 1-ethyl-4-methylhexahydro-1,4-diazepinylbenzamide (R)-22 had potent affinity for both receptors. The R-enantiomer of the corresponding 1-ethylhexahydroazepinylbenzamide 28 showed potent affinity for dopamine D, receptors with reduced affinity for 5-HT, receptors, while the S isomer was found to be a potent and selective 5-HT3 receptor antagonist. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：619 / 624

页数：6

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