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Bioorg Med Chem Lett. 2002 Apr 8;12(7):1099-102.

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

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  • 1Novartis Pharma AG, Klybeckstrasse 141, 4002 Basel, Switzerland. yves.auberson@pharma.novartis.com

Abstract

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.

PMID:
11909726
[PubMed - indexed for MEDLINE]
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