New probes of the agonist binding site of metabotropic glutamate receptors

被引：12

作者：

Bessis, AS

Bolte, J

Pin, JP

Acher, F

机构：

[1] Univ Paris 05, Chim & Biochim Pharmacol & Toxicol Lab, CNRS, UMR8601, F-75270 Paris 06, France

[2] Univ Blaise Pascal, Lab Synth Electrosynth & Etud Syst Interet Biol, CNRS, UMR6504, F-63177 Aubiere, France

[3] Ctr INSERM CNRS Pharmacol Endocrinol, CNRS, UPR9023, F-34094 Montpellier 5, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)00158-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The (2S,4R)- and (2S,4S)-4-hydroxyglutamates activate cloned mGlu(1a), mGlu(2), and mGlu(Sa) receptors with different potencies. Best results were obtained with the (2S,4S) isomer being almost as potent as glutamate on mGlu(1a)R and mGlu(Sa)R. Data are interpreted on the basis of the binding site model and X-ray structure. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1569 / 1572

页数：4

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