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5-Phosphonomethylquinoxalinediones As Competitive NMDA Receptor Antagonists with a Preference for the Human 1A/2A, Rather Than 1A/2B Receptor Composition

Overview
Specialty Biochemistry
Date 2002 Mar 23
PMID 11909726
Citations 119
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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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