5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.
作者： Yves P Auberson , Hans Allgeier , Serge Bischoff , Kurt Lingenhoehl , Robert Moretti
DOI: 10.1016/S0960-894X(02)00074-4
关键词:
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 mice. Their preference for 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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