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

…, D Steensma, M Varasi, S Pshenichkin, E Surina…

Index: Kozikowski, Alan P.; Steensma, Darryl; Varasi, Mario; Pshenichkin, Sergey; Surina, Elena; Wroblewski, Jarda T. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 5 p. 447 - 452

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Citation Number: 11

Abstract

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 ...

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