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

Stanley, N.J. and Hutchinson, M.R. and Kvist, T. and Nielsen, B. and Mathiesen, J.M. and Brauner-Osborne, H. and Avery, T.D. and Tiekink, E.R.T. and Pedersen, D.S. and Irvine, R. and Abell, A.D. and Taylor, D.K. (2010) A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity. Bioorganic & Medicinal Chemistry, 18 (16). pp. 6089-6098.

Full text not available from this repository.

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. (C) 2010 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: 1,2-Dioxines; Carboxycyclopropylglycines; Metabotropic glutamate receptors; In vivo; Neuropathic pain; Allodynia
Subjects: Q Science > Q Science (General)
Depositing User: Mr Faizal 2
Date Deposited: 04 Feb 2015 02:12
Last Modified: 05 Jul 2017 08:49
URI: http://eprints.um.edu.my/id/eprint/12517

Actions (login required)

View Item View Item