Agonists and antagonists for group III metabotropic glutamate receptors 6, 7 and 8

被引：16

作者：

Yang, ZQ ^{[1
]}

机构：

[1] Merck & Co Inc, Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2005年 / 5卷 / 09期

关键词：

glutamate; metabotropic glutamate receptors; agonists; antagonists;

D O I：

10.2174/1568026054750272

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Metabotropic glutamate receptors (mGluRs) have been implicated in a variety of neurological and psychiatric disorders. This article describes recent progress in the development of agonists and antagonists for mGluR 6, 7, and 8. All of them are conformationally constrained or substituted amino acids, and they act at N-terminal extracellular glutamate binding site. These ligands serve as valuable tools for studying physiological and pathological roles of mGluRs. However, their therapeutic potential may be restricted by their poor CNS penetration and lack of selectivity for individual receptors.

引用

页码：913 / 918

页数：6

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