TY - JOUR
T1 - α-Substituted quisqualic acid analogs
T2 - New metabotropic glutamate receptor group II selective antagonists
AU - Kozikowski, Alan P.
AU - Steensma, Darryl
AU - Varasi, Mario
AU - Pshenichkin, Sergey
AU - Surina, Elena
AU - Wroblewski, Jarda T.
N1 - Copyright:
Copyright 2007 Elsevier B.V., All rights reserved.
PY - 1998/3/3
Y1 - 1998/3/3
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0032478241&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0032478241&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(98)00052-3
DO - 10.1016/S0960-894X(98)00052-3
M3 - Article
C2 - 9871596
AN - SCOPUS:0032478241
VL - 8
SP - 447
EP - 452
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 5
ER -