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A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity.

Abstract：

:As part of the vital search towards improved therapeutic agents for the treatment of neuropathic pain, the central nervous system glutamate receptors have become a major focus of research. Outlined herein are the syntheses of two new biologically active 3'-cycloalkyl-substituted carboxycyclopropylglycines, utilizing novel synthetic chemistry. The reaction between substituted 1,2-dioxines and an aminophosphonate furnished the cyclopropane core in a single step with all required stereochemistry of pendant groups. In vitro binding assays at metabotropic glutamate receptors revealed selective activity. In vivo testing in a rodent model of neuropathic pain indicated one amino acid significantly and dose-dependently decreased mechanical allodynia.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Stanley NJ,Hutchinson MR,Kvist T,Nielsen B,Mathiesen JM,Bräuner-Osborne H,Avery TD,Tiekink ER,Pedersen DS,Irvine RJ,Abell AD,Taylor DK

doi

10.1016/j.bmc.2010.06.051

subject

Has Abstract

pub_date

2010-08-15 00:00:00

pages

6089-98

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00579-1

journal_volume

18

pub_type

杂志文章

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