XB-ART-36188
J Med Chem
2007 May 17;5010:2408-14. doi: 10.1021/jm061439q.
Show Gene links
Show Anatomy links
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.
???displayArticle.abstract???
Replacement of the methyl group of the AMPA receptor agonist 2-amino-3-[3-hydroxy-5-(2-methyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid (2-Me-Tet-AMPA) with a benzyl group provided the first AMPA receptor agonist, compound 7, capable of discriminating GluR2-4 from GluR1 by its more than 10-fold preference for the former receptor subtypes. An X-ray crystallographic analysis of this new analogue in complex with the GluR2-S1S2J construct shows that accommodation of the benzyl group creates a previously unobserved pocket in the receptor, which may explain the remarkable pharmacological profile of compound 7.
???displayArticle.pubmedLink??? 17455929
???displayArticle.link??? J Med Chem
Species referenced: Xenopus laevis
Genes referenced: gria1 gria2