Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists

Science. 1988 Aug 5;241(4866):701-3. doi: 10.1126/science.2899909.

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.

Publication types

  • Comparative Study

MeSH terms

  • 6-Cyano-7-nitroquinoxaline-2,3-dione
  • Action Potentials / drug effects
  • Animals
  • Aspartic Acid / analogs & derivatives
  • Aspartic Acid / pharmacology
  • Binding, Competitive
  • Cell Membrane / metabolism
  • Cerebral Cortex / metabolism
  • Ibotenic Acid / analogs & derivatives
  • Ibotenic Acid / metabolism
  • Kainic Acid / metabolism
  • Ketamine / pharmacology
  • N-Methylaspartate
  • Neurons / physiology
  • Piperazines / metabolism
  • Quinoxalines / pharmacology*
  • Rats
  • Receptors, AMPA
  • Receptors, Drug / drug effects
  • Receptors, Drug / metabolism
  • Receptors, Glutamate
  • Receptors, Kainic Acid
  • Receptors, N-Methyl-D-Aspartate
  • Receptors, Neurotransmitter / drug effects*
  • Receptors, Neurotransmitter / metabolism
  • Spinal Cord / physiology
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid

Substances

  • 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