Alkyl diphenylacetyl, 9H-xanthene- and 9H-thioxanthene-carbonyl carbamates as positive allosteric modulators of mGlu1 receptors

被引：30

作者：

Wichmann, J ^{[1
]}

Bleicher, K ^{[1
]}

Vieira, E ^{[1
]}

Woltering, T ^{[1
]}

Knoflach, F ^{[1
]}

Mutel, V ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Preclin CNS Res, CH-4070 Basel, Switzerland

来源：

FARMACO | 2002年 / 57卷 / 12期

关键词：

metabotropic glutamate receptors; positive allosteric modulators; carbamates;

D O I：

10.1016/S0014-827X(02)01283-1

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Starting from the random-screening hit la, a series of alkyl diphenylacetyl, 9H-xanthene- and 9H-thioxanthene-carbonyl carbamates 1 has been prepared. These derivatives turned out to be selective positive allosteric modulators of mGlu1 receptors. These compounds do not directly activate mGlu1 receptors but markedly potentiate agonist stimulated responses, increasing potency and maximum efficacy. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.

引用

页码：989 / 992

页数：4

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