5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3′-bipyridine:: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity

被引：44

作者：

Roppe, JR

Wang, BW

Huang, DH

Tehrani, L

Kamenecka, T

Schweiger, EJ

Anderson, JJ

Brodkin, J

Jiang, XH

Cramer, M

Chung, J

Reyes-Manalo, G

Munoz, B

Cosford, NDP

机构：

[1] Merck Res Labs, Dept Med Chem, San Diego, CA 92121 USA

[2] Merck Res Labs, Dept Pharmacol, San Diego, CA 92121 USA

[3] Merck Res Labs, Dept Mol Profiling, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 15期

关键词：

metabotropic glutamate receptor; mGluR; mGluR5; MPEP; MTEP;

D O I：

10.1016/j.bmcl.2004.05.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo receptor occupancy, and is efficacious in the rat fear-potentiated startle model of anxiety following oral dosing. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：3993 / 3996

页数：4

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