A potent antagonist of the strychnine insensitive glycine receptor has anticonvulsant properties
摘要：
5,7-Dinitro-quinoxaline-2,3-dione (MNQX) displaced [ 3H]glycine binding to cortical membranes but had no effect on [ 3 H]3-((±)-2- carboxypiperazin-4- ly)- propyl-1- phosphonic acid ([ 3 H] CPPP) binding. MNQX potently antagonized N-methyl-D-aspartate (NMDA)-evoked release of [ 3H]GABA from cultured cortical neurones, NMDA evoked spreading depression and NMDA depolarizations in the rat neo-cortex. All of these responses were reversed by addition of glycine to the perfusion media. These results suggested that MNQX is an antagonist at the strychnine-in-sensitive glycine receptor associated with the NMDA receptor/ionophore complex. Furthermore the compound was found to antagonise audiogenic seizures in DBA-2 mice indicating the potential of glycine antagonists of this type in anticonvulsant therapy.
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DOI：
10.1016/0014-2999(89)90312-9
被引量：
年份：
1989
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