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ID: ALA1148386

Journal: J Med Chem

Title: (2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.

Authors: Collado I, Pedregal C, Bueno AB, Marcos A, González R, Blanco-Urgoiti J, Pérez-Castells J, Schoepp DD, Wright RA, Johnson BG, Kingston AE, Moher ED, Hoard DW, Griffey KI, Tizzano JP.

Abstract: The asymmetric synthesis and biological activity of (2S,1'S,2'R,3'R)-2-(2'-carboxy-3'-hydroxymethylcyclopropyl) glycine ((+)-3) is described. This novel C-3' substituted carboxy cyclopropyl glycine is a highly potent group 2 and group 3 mGluR agonist that has proven to be orally active in both fear potentiated startle (animal model for anxiety) and PCP-induced motor activation (animal model for psychosis) assays in rats.

CiteXplore: 14711315

DOI: 10.1021/jm030967o