5-phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition

被引：193

作者：

Auberson, YP ^{[1
]}

Allgeier, H ^{[1
]}

Bischoff, S ^{[1
]}

Lingenhoehl, K ^{[1
]}

Moretti, R ^{[1
]}

Schmutz, M ^{[1
]}

机构：

[1] Novartis Pharma AG, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(02)00074-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

NMDA antagonists derived from 5-phosphonomethyl-1,4-dihydroquinoxaline-2,3-dione (3a) are potent anticonvulsant agents, and display strong protective effects in the electroshock-induced convulsion assay in mice. Their preference for the human NMDAR 1A/2A over 1A/2B subunit composition was optimized, leading to (1RS, 1'S)-PEAQX (9r), which shows a > 100-fold selectivity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1099 / 1102

页数：4

共 15 条

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