NOVEL BENZIMIDAZOLES AS LIGANDS FOR THE STRYCHNINE-INSENSITIVE N-METHYL-D-ASPARTATE-LINKED GLYCINE RECEPTOR

Two new benzimidazole derivatives were synthesized and evaluated for t heir ability to inhibit the binding at the strychnine-insensitive N-me thyl-D-aspartate(NMDA)-linked glycine receptor. The most potent one, t he 4,6-dichlorobenzimidazole-2-carboxylic acid 6, was found to have su bmicromolar affinity for this receptor. The result of its functional t est suggests that it acts as an antagonist of the NMDA receptor comple x. Thus, this class of benzimidazole derivatives seems to constitute a group of potential antagonists for the strychnine-insensitive glycine receptor.