Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators

被引：40

作者：

Pinkerton, AB ^{[1
]}

Cube, RV ^{[1
]}

Hutchinson, JH ^{[1
]}

James, JK ^{[1
]}

Gardner, MF ^{[1
]}

Rowe, BA ^{[1
]}

Schaffhauser, H ^{[1
]}

Rodriguez, DE ^{[1
]}

Campbell, UC ^{[1
]}

Daggett, LP ^{[1
]}

Vernier, JM ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 06期

关键词：

GPCRs; glutamate; mGlu receptors; allosteric; schizophrenia;

D O I：

10.1016/j.bmcl.2005.01.077

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have identified and synthesized a series of phenyl-tetrazolyl and 4-thiopyridyl indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50 = 186 nM), which displayed activity in a rodent model for schizophrenia. © 2005 Elsevier Ltd. All rights reserved.

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页码：1565 / 1571

页数：7

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