Substituted 2-(R)-methyl piperazines as muscarinic M2 selective ligands

被引：22

作者：

Kozlowski, JA ^{[1
]}

Zhou, GW ^{[1
]}

Tagat, JR ^{[1
]}

Lin, SI ^{[1
]}

McCombie, SW ^{[1
]}

Ruperto, VB ^{[1
]}

Duffy, RA ^{[1
]}

McQuade, RA ^{[1
]}

Crosby, G ^{[1
]}

Taylor, LA ^{[1
]}

Billard, W ^{[1
]}

Binch, H ^{[1
]}

Lachowicz, JE ^{[1
]}

机构：

[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(02)00023-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 2-(R)-methyl-substituted piperazines (e.g.. 2) is described. They are potent M-2 selective ligands that have > 100-fold selectivity versus the M-1 receptor. In the rat microdialysis assay. compound 14 showed significantly enhanced levels of acetylcholine after oral administration. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：791 / 794

页数：4

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