Competitive antagonism at metabotropic glutamate receptors by (S)-4-carboxyphenylglycine and (RS)-alpha-methyl-4-carboxyphenylglycine

Eur J Pharmacol. 1993 Jan 15;244(2):195-7. doi: 10.1016/0922-4106(93)90028-8.

Abstract

Two phenylglycine derivates, (S)-4-carboxyphenylglycine and (RS)-alpha-methyl-4-carboxyphenylglycine, competitively antagonised (1S,3R)-1-aminocyclopentane-1,3-dicarboxylate (ACPD)-stimulated phosphoinositide hydrolysis in rat cerebral cortical slices. The same phenylglycine derivatives selectively antagonized ACPD-induced depolarization in neonatal rat spinal motoneurones and rate thalamic neurones relative to depolarization or excitation induced by N-methyl-D-aspartate (NMDA) or alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA). Both phenylglycine derivatives also selectively depressed synaptic excitation in thalamic neurones evoked by noxious thermal stimuli, without affecting the synaptic stimulation of the same cells by non-noxious stimuli.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Animals, Newborn
  • Benzoates / pharmacology*
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • Chromatography, High Pressure Liquid
  • Cycloleucine / analogs & derivatives
  • Cycloleucine / antagonists & inhibitors
  • Cycloleucine / pharmacology
  • Excitatory Amino Acid Antagonists*
  • Glycine / analogs & derivatives*
  • Glycine / pharmacology
  • In Vitro Techniques
  • Motor Neurons / drug effects
  • N-Methylaspartate / pharmacology
  • Phosphatidylinositols / metabolism
  • Rats
  • Spinal Cord / cytology
  • Spinal Cord / drug effects
  • Synapses / drug effects
  • Thalamus / cytology
  • Thalamus / drug effects

Substances

  • Benzoates
  • Excitatory Amino Acid Antagonists
  • Phosphatidylinositols
  • Cycloleucine
  • 1-amino-1,3-dicarboxycyclopentane
  • alpha-methyl-4-carboxyphenylglycine
  • N-Methylaspartate
  • 4-carboxyphenylglycine
  • Glycine