5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition |
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| Authors: | Auberson Yves P Allgeier Hans Bischoff Serge Lingenhoehl Kurt Moretti Robert Schmutz Markus |
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| Affiliation: | Novartis Pharma AG, Klybeckstrasse 141, 4002 Basel, Switzerland. yves.auberson@pharma.novartis.com |
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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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