Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

被引：20

作者：

Bennett, Chad E. ^{[1
]}

Burnett, Duane A. ^{[1
]}

Greenlee, William J. ^{[1
]}

Knutson, Chad E. ^{[1
]}

Korakas, Peter ^{[1
]}

Li, Cheng ^{[1
]}

Tulshian, Deen ^{[1
]}

Wu, Wen-Lian ^{[1
]}

Bertorelli, Rosalia ^{[2
]}

Fredduzzi, Silva ^{[2
]}

Grilli, Mariagrazia ^{[2
]}

Lozza, Gianluca ^{[2
]}

Reggiani, Angelo ^{[2
]}

Veltri, Alessio ^{[2
]}

机构：

[1] Merck Res Labs, Kenilworth, NJ 07033 USA

[2] Schering Plough Res Inst, I-20132 Milan, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 04期

关键词：

mGluR1 (metabotropic glutamate receptor 1); Neuropathic pain; Spinal nerve ligation (SNL); Fused tricyclic pyridones; GPCR; METABOTROPIC GLUTAMATE RECEPTORS; MODULATORS;

D O I：

10.1016/j.bmcl.2011.12.131

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test. (C) 2012 Elsevier Ltd. All rights reserved.

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收藏

页码：1575 / 1578

页数：4

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