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.

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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

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