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.
MeSH terms
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Animals
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Anticonvulsants / pharmacology*
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Binding, Competitive
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Electric Stimulation
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Humans
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Mice
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Molecular Structure
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Quinoxalines / chemical synthesis
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Quinoxalines / chemistry*
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Quinoxalines / pharmacology*
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
Substances
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Anticonvulsants
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NMDA receptor A1
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NR2B NMDA receptor
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Quinoxalines
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Receptors, N-Methyl-D-Aspartate
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N-methyl D-aspartate receptor subtype 2A