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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 & Medicinal Chemistry, 2010; 18(16):6089-6098
Publisher: Pergamon-Elsevier Science
Issue Date: 2010
ISSN: 0968-0896
Statement of
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
RMID: 0020100375
DOI: 10.1016/j.bmc.2010.06.051
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Appears in Collections:Chemistry publications
IPAS publications

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