title: Antinociceptive action of GLYX-13: an N-methyl-D-aspartate receptor glycine site partial agonist.
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.
authors.affiliation: Falk Center for Molecular Therapeutics, Department of Biomedical Engineering, McCormick School of Engineering and Applied Sciences, Northwestern University, Evanston, Illinois 60201, USA.
authors.forename: Paul L
authors.initials: PL
authors.lastname: Wood
authors.forename: Siddique A
authors.initials: SA
authors.lastname: Mahmood
authors.forename: Joseph R
authors.initials: JR
authors.lastname: Moskal
mesh_terms: 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
chemical_list: D000588:Amines; D000700:Analgesics; D003509:Cyclohexanecarboxylic Acids; D009842:Oligopeptides; D005557:Formaldehyde; D005680:gamma-Aminobutyric Acid; C507283:GLYX-13 peptide; D000077206:Gabapentin