New quinoxalinediones show potent antagonism of quisqualate responses in cultured mouse cortical neurons.
Two new quinoxalines, DNQX (6,7-dinitro-quinoxaline-2,3-dion = FG 9041) and CNQX (6-nitro-7-cyano-quinoxaline-2,3-dion = FG 9065), were tested as antagonists of excitatory amino acid responses in cultured neurons and brain slices. DNQX and CNQX showed potent competitive antagonism of quisqualate and kainate induced [3H]GABA release from cultured mouse cortical neurons with weaker effects on NMDA responses (Schild values for DNQX were 6.2, 5.9 and 5.4, respectively). Also in a model of excitatory amino acid induced 22Na efflux from striatal slices DNQX blocked responses to quisqualate and kainate more effectively than responses to NMDA.
Drejer
J
J
Ferrosan Research Division, Department of Biochemistry, Soeborg, Denmark.
Honoré
T
T
D000818:Animals; D001224:Aspartic Acid / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D007608:Kainic Acid / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D016202:N-Methylaspartate; D010069:Oxadiazoles / Q000378:metabolism / Q000494:pharmacology*; D011810:Quinoxalines / Q000378:metabolism / Q000494:pharmacology*; D016318:Quisqualic Acid; D018091:Receptors, AMPA; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism; D012964:Sodium / Q000493:pharmacokinetics; D005680:gamma-Aminobutyric Acid / Q000493:pharmacokinetics*
D010069:Oxadiazoles; D011810:Quinoxalines; D018091:Receptors, AMPA; D011955:Receptors, Drug; D001224:Aspartic Acid; D005680:gamma-Aminobutyric Acid; D016202:N-Methylaspartate; D016318:Quisqualic Acid; D012964:Sodium; D007608:Kainic Acid