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ID: ALA1135273
Journal: Bioorg Med Chem Lett
Title: 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.
Authors: Auberson YP, Allgeier H, Bischoff S, Lingenhoehl K, Moretti R, Schmutz M.
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.
CiteXplore: 11909726