alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.

Basic Information

ID: ALA1130758

Journal: Bioorg Med Chem Lett

Title: alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.

Authors: Kozikowski AP, Steensma D, Varasi M, Pshenichkin S, Surina E, Wroblewski JT.

Abstract: Syntheses of both the alpha-methyl and benzyl analogs of quisqualic acid are described. Testing of these compounds for their activity at excitatory amino acid receptors revealed a striking change in activity in comparison to quisqualic acid. This structural modification results in the loss of quisqualate's potent agonist action at both non-NMDA ionotropic glutamate receptors as well as at group I mGluRs, while allowing these analogs to acquire antagonist properties with relative selectivity for group II metabotropic glutamate receptors.

CiteXplore: 9871596

DOI: 10.1016/s0960-894x(98)00052-3

Patent ID: