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PMID: 2899909 Published · ppublish English Comparative Study Journal Article

Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists.

Science (New York, N.Y.) ·Vol. 241 ·No. 4866 ·1988-08-05 ·Pages 701-3

Honoré T, Davies SN, Drejer J, Fletcher EJ, Jacobsen P, Lodge D, Nielsen FE

Abstract

The N-methyl-D-aspartate (NMDA)-subtype of glutamate receptors has been well described as a result of the early appearance of NMDA antagonists, but no potent antagonist for the "non-NMDA" glutamate receptors has been available. Quinoxalinediones have now been found to be potent and competitive antagonists at non-NMDA glutamate receptors. These compounds will be useful in the determination of the structure-activity relations of quisqualate and kainate receptors and the role of such receptors in synaptic transmission in the mammalian brain.

MeSH Terms
6-Cyano-7-nitroquinoxaline-2,3-dione Action Potentials/drug effects Animals Aspartic Acid/analogs & derivatives,pharmacology Binding, Competitive Cell Membrane/metabolism Cerebral Cortex/metabolism Ibotenic Acid/analogs & derivatives,metabolism Kainic Acid/metabolism Ketamine/pharmacology N-Methylaspartate Neurons/physiology Piperazines/metabolism Quinoxalines/pharmacology Rats Receptors, AMPA Receptors, Drug/drug effects,metabolism Receptors, Glutamate Receptors, Kainic Acid Receptors, N-Methyl-D-Aspartate Receptors, Neurotransmitter/drug effects,metabolism Spinal Cord/physiology alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Chemicals
Piperazines Quinoxalines Receptors, AMPA Receptors, Drug Receptors, Glutamate Receptors, Kainic Acid Receptors, N-Methyl-D-Aspartate Receptors, Neurotransmitter Ibotenic Acid Aspartic Acid FG 9041 N-Methylaspartate Ketamine 6-Cyano-7-nitroquinoxaline-2,3-dione alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid Kainic Acid
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Honoré T
Ferroson Research Division, Soeborg, Denmark.
Davies S N
Drejer J
Fletcher E J
Jacobsen P
Lodge D
Nielsen F E
Article Info
Journal
Science (New York, N.Y.)
Abbr.
Science
ISSN
0036-8075
Published
1988-08-05
Pages
701-3
Language
English
Region
United States
NLM ID
0404511
Subset
IM
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