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CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) antagonizes NMDA-evoked [3H]GABA release from cultured cortical neurons via an inhibitory action at the strychnine-insensitive glycine site

Harris, K.M.; Miller, R.J.

Brain Research 489(1): 185-189

1989

ISSN/ISBN: 0006-8993
PMID: 2568152
DOI: 10.1016/0006-8993(89)90023-1
Accession: 039434975
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The novel glutamate antagonist 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) inhibited glutamate stimulated [3H]GABA release from cortical neurons in vitro. Kainate-induced release was blocked in a competitive fashion but N-methyl-D-aspartate (NMDA)-induced release was blocked non-competitively by CNQX. 7-Chlorokynurenate (7-CK) also inhibited NMDA evoked [3H]GABA release non-competitively, but had no effect on kainate induced release. The effects of both CNQX and 7-CK on NMDA-induced release were reversed by addition of exogenous glycine but the effects of CNQX on kainate-induced release were not altered by glycine. This suggests that both CNQX and 7-CK may interact with the glycine regulatory site of the NMDA receptor.

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Related References

Reynolds, I.J.; Harris, K.M.; Miller, R.J. 1989: NMDA receptor antagonists that bind to the strychnine-insensitive glycine site and inhibit NMDA-induced Ca2+ fluxes and [3H]GABA release European Journal of Pharmacology 172(1): 9-17
Reynolds, I.J.; Harris, K.M.; Miller, R.J. 1989: Nmda receptor antagonists that bind to the strychnine insensitive glycine site and inhibit nmda induced calcium ion fluxes and tritiated gaba release European Journal of Pharmacology Molecular Pharmacology Section 1(1): 9-18
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