(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.

作者信息

Collado Iván, Pedregal Concepción, Bueno Ana Belén, Marcos Alicia, González Rosario, Blanco-Urgoiti Jaime, Pérez-Castells Javier, Schoepp Darryle D, Wright Rebecca A, Johnson Bryan G, Kingston Ann E, Moher Eric D, Hoard David W, Griffey Kelly I, Tizzano Joseph P

机构信息

Lilly, SA, Avda. de la Industria 30, 28108 Alcobendas, Madrid, Spain.

出版信息

J Med Chem. 2004 Jan 15;47(2):456-66. doi: 10.1021/jm030967o.

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.