Specificity and potency of N-methyl-D-aspartate glycine site antagonists and of mephenesin on the rat spinal cord in vitro.

Article date: 1992/2/17

PubMed ID: 1378953

Journal name: Neuroscience letters (ISSN: 0304-3940)


The potency, specificity and reversibility of various presumed glycine site N-methyl-D-aspartate (NMDA) antagonists was studied on neonatal rat spinal cord using the grease gap technique. 5,7-Dichlorokynurenate was the most potent and specific glycine site antagonist among the compounds tested. On the other hand mephenesin was a weak non-specific excitatory amino acid (EAA) antagonist; reduction of the response to NMDA was not reversed by D-serine. The EAA antagonist properties of mephenesin could explain its mode of action at the cellular level. The lack of effect of D-serine alone suggests that in our experimental conditions glycine sites on spinal neurones are occupied by an endogenous ligand.

Author List: Pralong E, Millar J D, Lodge D

Publication Types: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't

Substances mentioned in the article: Indoles; Pyrrolidinones; Quinoxalines; Receptors, N-Methyl-D-Aspartate; 5-chloroindole-2-carboxylate; 5,7-dinitroquinoxaline-2,3-dione; Ibotenic Acid; N-Methylaspartate; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; Mephenesin; 1-hydroxy-3-amino-2-pyrrolidone; Kynurenic Acid; 7-chlorokynurenic acid; 5,7-dichlorokynurenic acid; Glycine;

Mesh terms: Animals; Binding Sites; Glycine; Ibotenic Acid/analogs & derivatives; Indoles/pharmacology; Kynurenic Acid/analogs & derivatives; Mephenesin/pharmacology; N-Methylaspartate/antagonists & inhibitors; Pyrrolidinones/pharmacology; Quinoxalines/pharmacology; Rats; Receptors, N-Methyl-D-Aspartate/drug effects; Spinal Cord/drug effects; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid;

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