(2S,l'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

摘要

The asymmetric synthesis and biological activity of (2S,l'S,2'R,3'R)-2-(2'-carboxy-3'-hydroxy-methylcyclopropyl) 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.