(2S,4S)-2-amino-4-(2,2-diphenylethyl) pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist

被引：33

作者：

Escribano, A

Ezquerra, J

Pedregal, C

Rubio, A

Yruretagoyena, B

Baker, SR

Wright, RA

Johnson, BG

Schoepp, DD

机构：

[1] Ctr Invest Lilly, Valdeolmos 28130, Madrid, Spain

[2] Lilly Res Ctr Ltd, Windlesham GU20 6PH, Surrey, England

[3] Eli Lilly & Co, Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(98)00091-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(2S,4S)-2-Amino-4-(4,4-diphenylbut-1-yl)-pentane-1,5-dioic acid 1m, is a novel metabotropic glutamate receptor (mGluR) antagonist with insignificant ionotropic affinity. It is a selective antagonist of negatively-coupled cAMP-linked mGluRs with no effect on phosphoinositide coupled mGluRs. A series of 4-substituted glutamic acid analogues were prepared and it was found that compound 1k is tenfold more potent than 1m. Compound 1k has neither significant affinity for ionotropic glutamate receptors nor group 1 and 3 metabotropic receptors. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：765 / 770

页数：6

共 12 条

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