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alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists
A P Kozikowski1, D Steensma, M Varasi
1Drug Discovery Program, Georgetown University Medical Center, Washington, DC 20007-2197, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
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.