4-alkylidenyl glutamic acids, potent and selective GluR5 agonists

被引：24

作者：

Baker, SR

Bleakman, D

Ezquerra, J

Ballyk, BA

Deverill, M

Ho, K

Kamboj, RK

Collado, I

Domínguez, C

Escribano, A

Mateo, AI

Pedregal, C

Rubio, A

机构：

[1] Eli Lilly & Co, Lilly Res Ctr Ltd, Windlesham GU20 6PH, Surrey, England

[2] Lilly Res Labs, Indianapolis, IN 46285 USA

[3] Lilly SA, Alcobendas 28108, Spain

[4] Allelix Biopharmaceut Inc, Mississauga, ON L4V 1V7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(00)00346-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Twenty-four 4-alkylidene glutamic acids were synthesised and tested as potential subtype selective GluR5 and 6 ligands. It was found that a critical size of alkylidene group gave potent and selective GluR5 receptor agonists. LY339624 had K(i)s of 0.0326 and >100 mu M on GluR5 and 6 receptors, respectively. (C) 2000 Published by Elsevier Science Ltd. All rights reserved.

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页码：1807 / 1810

页数：4

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