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ID: ALA1133269

Journal: Bioorg Med Chem Lett

Title: 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.

Authors: Baker SR, Bleakman D, Ezquerra J, Ballyk BA, Deverill M, Ho K, Kamboj RK, Collado I, Domínguez C, Escribano A, Mateo AI, Pedregal C, Rubio A.

Abstract: Twenty-four 4-alkylidene glutamic acids were synthesised and tested as potential subtype selective GluR5 and 6 ligands. It was found that a critical size of alkylidene group gave potent and selective GluR5 receptor agonists. LY339624 had Kis of 0.0326 and >100 microM on GluR5 and 6 receptors, respectively.

CiteXplore: 10969973

DOI: 10.1016/s0960-894x(00)00346-2