ALPHA-SUBSTITUTED QUISQUALIC ACID ANALOGS - NEW METABOTROPIC GLUTAMATE-RECEPTOR GROUP-II SELECTIVE ANTAGONISTS

Authors
KOZIKOWSKI AP STEENSMA D VARASI M PSHENICHKIN S SURINA E WROBLEWSKI JT
Citation
Ap. Kozikowski et al., ALPHA-SUBSTITUTED QUISQUALIC ACID ANALOGS - NEW METABOTROPIC GLUTAMATE-RECEPTOR GROUP-II SELECTIVE ANTAGONISTS, Bioorganic & medicinal chemistry letters, 8(5), 1998, pp. 447-452
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
5
Year of publication
1998
Pages
447 - 452
Database
ISI
SICI code
0960-894X(1998)8:5<447:AQAA-N>2.0.ZU;2-U
Abstract
Syntheses of both the alpha-methyl and benzyl analogs of quisqualic ac id are described. Testing of these compounds for their activity at exc itatory amino acid receptors revealed a striking change in activity in comparison to quisqualic acid. This structural modification results i n the loss of quisqualate's potent agonist action at both non-NMDA ion otropic glutamate receptors as well as at group I mGluRs, while allowi ng these analogs to acquire antagonist properties with relative select ivity for group II metabotropic glutamate receptors. (C) 1998 Elsevier Science Ltd. All rights reserved.