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https://hdl.handle.net/2440/61716
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Type: | Journal article |
Title: | A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity |
Author: | Stanley, N. Hutchinson, M. Kvist, T. Nielsen, B. Mathiesen, J. Brauner-Osborne, H. Avery, T. Tiekink, E. Pedersen, D. Irvine, R. Abell, A. Taylor, D. |
Citation: | Bioorganic and Medicinal Chemistry, 2010; 18(16):6089-6098 |
Publisher: | Pergamon-Elsevier Science |
Issue Date: | 2010 |
ISSN: | 0968-0896 1464-3391 |
Statement of Responsibility: | Nathan J. Stanley, Mark R. Hutchinson, Trine Kvist, Birgitte Nielsen, Jesper Mosolff Mathiesen Hans Bräuner-Osborne, Thomas D. Avery, Edward R. T. Tiekink, Daniel Sejer Pedersen, Rodney J. Irvine, Andrew D. Abell and Dennis K. Taylor |
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. |
Keywords: | CHO Cells Animals Cricetulus Rats Rats, Sprague-Dawley Neuralgia Hyperalgesia Cyclopropanes Glycine Receptors, Metabotropic Glutamate Analgesics Cricetinae Male |
Rights: | © 2010 Elsevier Ltd. All rights reserved |
DOI: | 10.1016/j.bmc.2010.06.051 |
Grant ID: | http://purl.org/au-research/grants/nhmrc/465423 |
Published version: | http://dx.doi.org/10.1016/j.bmc.2010.06.051 |
Appears in Collections: | Aurora harvest Chemistry publications IPAS publications |
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