Antinociceptive action of GLYX-13: an N-methyl-D-aspartate receptor glycine site partial agonist.
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.
Wood
Paul L
PL
Falk Center for Molecular Therapeutics, Department of Biomedical Engineering, McCormick School of Engineering and Applied Sciences, Northwestern University, Evanston, Illinois 60201, USA.
Mahmood
Siddique A
SA
Moskal
Joseph R
JR
D000588:Amines / Q000627:therapeutic use; D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D003509:Cyclohexanecarboxylic Acids / Q000627:therapeutic use; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005557:Formaldehyde / Q000009:adverse effects; D000077206:Gabapentin; D008297:Male; D009842:Oligopeptides / Q000627:therapeutic use*; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D010147:Pain Measurement; D017288:Pain Threshold / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors; D005680:gamma-Aminobutyric Acid / Q000627:therapeutic use
D000588:Amines; D000700:Analgesics; D003509:Cyclohexanecarboxylic Acids; D009842:Oligopeptides; D005557:Formaldehyde; D005680:gamma-Aminobutyric Acid; C507283:GLYX-13 peptide; D000077206:Gabapentin