Synthesis and pharmacology of new enantiopure Δ3-4-arylkainoids
Seven Δ3-4-arylkainoids possessing various 4-position aromatic and heteroaromatic groups were synthesized and their apparent affinities were measured in order to explore the influences of 4-position electron density and stereochemistry on receptor affinity and specificity. Kainoids 1a-f were shown to be selective agonists at the NMDA receptor and the electron rich furanyl and thienyl analogues exhibited the highest affinities. Naphthylkainoid 1g proved to be a nonselective antagonist at the iGluRs. (C) 2000 Elsevier Science Ltd. All rights reserved.
Rondeau, Dany,Gill, Patrice,Chan, Monique,Curry, Kenneth,Lubell, William D.
p. 771 - 773
(2007/10/03)
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