Antinociceptive action of GLYX-13: an N-methyl-D-aspartate receptor glycine site partial agonist

Neuroreport. 2008 Jul 2;19(10):1059-61. doi: 10.1097/WNR.0b013e32830435c9.

Abstract

Inhibition of N-methyl-D-aspartate (NMDA)-mediated neurotransmission has been demonstrated to provide antinociceptive actions in a number of animal models of tonic and neuropathic pain. However, both competitive and noncompetitive NMDA receptor antagonists are ataxic at analgesic doses. Partial agonists and antagonists of the NMDA-associated glycine site have demonstrated antinociceptive actions at doses that are not ataxic. In this study, we present data showing that GLYX-13, an NMDA receptor, glycine-site, partial agonist, also is antinociceptive in the rat formalin model of tonic pain and in the rat constriction nerve injury model of neuropathic pain at doses not inducing ataxia.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amines / therapeutic use
  • Analgesics / therapeutic use*
  • Animals
  • Behavior, Animal / drug effects
  • Cyclohexanecarboxylic Acids / therapeutic use
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Formaldehyde / adverse effects
  • Gabapentin
  • Male
  • Oligopeptides / therapeutic use*
  • Pain / chemically induced
  • Pain / drug therapy*
  • Pain Measurement
  • Pain Threshold / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Time Factors
  • gamma-Aminobutyric Acid / therapeutic use

Substances

  • Amines
  • Analgesics
  • Cyclohexanecarboxylic Acids
  • Oligopeptides
  • Formaldehyde
  • gamma-Aminobutyric Acid
  • GLYX-13 peptide
  • Gabapentin