Bioorganic and Medicinal Chemistry Letters p. 447 - 452 (1998)
Update date:2022-08-02
Topics:
Kozikowski, Alan P.
Steensma, Darryl
Varasi, Mario
Pshenichkin, Sergey
Surina, Elena
Wroblewski, Jarda T.
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.
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