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

Alan P. Kozikowski, Darryl Steensma, Mario Varasi, Sergey Pshenichkin, Elena Surina, Jarda T. Wroblewski

Research output: Contribution to journalArticlepeer-review

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 properties with relative selectivity for group II metabotropic glutamate receptors.

Original languageEnglish
Pages (from-to)447-452
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number5
DOIs
Publication statusPublished - Mar 3 1998

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Fingerprint Dive into the research topics of 'α-Substituted quisqualic acid analogs: New metabotropic glutamate receptor group II selective antagonists'. Together they form a unique fingerprint.

Cite this