2. Academic Validation
  3. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition

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

  • Bioorg Med Chem Lett. 2002 Apr 8;12(7):1099-102. doi: 10.1016/s0960-894x(02)00074-4.
Yves P Auberson 1,  Hans Allgeier,  Serge Bischoff,  Kurt Lingenhoehl,  Robert Moretti,  Markus Schmutz
Affiliations

Affiliation

  • 1 Novartis Pharma AG, Klybeckstrasse 141, 4002 Basel, Switzerland. yves.auberson@pharma.novartis.com
PMID: 11909726 DOI: 10.1016/s0960-894x(02)00074-4
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.

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