Metabotropic glutamate receptor agonist DCG-IV as NMDA receptor agonist in immature rat hippocampal neurons

Eur J Pharmacol. 1994 Sep 12;262(3):287-91. doi: 10.1016/0014-2999(94)90743-9.

Abstract

The electrophysiological action of (2S,1'R;2'R,3'R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV) on the NMDA receptor was investigated with the help of concentration-jump experiments on freshly dissociated hippocampal CA1 and CA3 neurons of rats. Inward currents elicited by a pulse of DCG-IV were insensitive to 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and could be blocked by D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5) and magnesium and enhanced by glycine. The substance displayed cross-desensitization with NMDA but not with kainate or (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA). Dose-response curves showed that DCG-IV was weaker than NMDA but more potent than glutamate in eliciting agonist-gated currents. From these data we conclude that DCG-IV has to be used with caution as a tool for the investigation of metabotropic glutamate receptors.

MeSH terms

  • 2-Amino-5-phosphonovalerate / pharmacology
  • 6-Cyano-7-nitroquinoxaline-2,3-dione / pharmacology
  • Animals
  • Cyclopropanes / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Electrophysiology
  • Glycine / analogs & derivatives*
  • Glycine / pharmacology
  • Hippocampus / cytology
  • Hippocampus / drug effects*
  • Kainic Acid / pharmacology
  • Magnesium / pharmacology
  • N-Methylaspartate / pharmacology
  • Neurons / cytology
  • Neurons / drug effects
  • Patch-Clamp Techniques
  • Rats
  • Rats, Wistar
  • Receptors, Metabotropic Glutamate / agonists*
  • Receptors, N-Methyl-D-Aspartate / agonists*
  • Stereoisomerism

Substances

  • Cyclopropanes
  • Receptors, Metabotropic Glutamate
  • Receptors, N-Methyl-D-Aspartate
  • 2-(2,3-dicarboxycyclopropyl)glycine
  • N-Methylaspartate
  • 6-Cyano-7-nitroquinoxaline-2,3-dione
  • 2-Amino-5-phosphonovalerate
  • Magnesium
  • Kainic Acid
  • Glycine