(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

被引：31

作者：

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

机构：

[1] Lilly SA, Madrid 28108, Spain

[2] Univ San Pablo, Fac Ciencias Expt & Salud, Madrid, Spain

[3] Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 02期

关键词：

D O I：

10.1021/jm030967o

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The asymmetric synthesis and biological activity of (2S,1'S,2R,3R)-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.

引用

页码：456 / 466

页数：11

共 82 条

[1] Anti-epileptogenic and anticonvulsant activity of L-2-amino-4-phosphonobutyrate, a presynaptic glutamate receptor agonist [J].