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

(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.

Author information

1
Lilly, SA, Avda. de la Industria 30, 28108 Alcobendas, Madrid, Spain. collado_ivan@lilly.com

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.

PMID:
14711315
DOI:
10.1021/jm030967o
[Indexed for MEDLINE]

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