α-Substituted quisqualic acid analogs: New metabotropic glutamate receptor group II selective antagonists

Article abstract of DOI:10.1016/S0960-894X(98)00052-3

Syntheses of both the α-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.