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

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dc.contributor.authorStanley, N.
dc.contributor.authorHutchinson, M.
dc.contributor.authorKvist, T.
dc.contributor.authorNielsen, B.
dc.contributor.authorMathiesen, J.
dc.contributor.authorBrauner-Osborne, H.
dc.contributor.authorAvery, T.
dc.contributor.authorTiekink, E.
dc.contributor.authorPedersen, D.
dc.contributor.authorIrvine, R.
dc.contributor.authorAbell, A.
dc.contributor.authorTaylor, D.
dc.date.issued2010
dc.description.abstractAs 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.
dc.description.statementofresponsibilityNathan 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
dc.identifier.citationBioorganic and Medicinal Chemistry, 2010; 18(16):6089-6098
dc.identifier.doi10.1016/j.bmc.2010.06.051
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.orcidStanley, N. [0000-0002-2625-9876]
dc.identifier.orcidHutchinson, M. [0000-0003-2154-5950]
dc.identifier.orcidAvery, T. [0000-0001-6882-5461]
dc.identifier.orcidAbell, A. [0000-0002-0604-2629]
dc.identifier.orcidTaylor, D. [0000-0002-3302-4610] [0000-0002-4274-3983] [0000-0003-0633-7424]
dc.identifier.urihttp://hdl.handle.net/2440/61716
dc.language.isoen
dc.publisherPergamon-Elsevier Science
dc.relation.granthttp://purl.org/au-research/grants/nhmrc/465423
dc.rights© 2010 Elsevier Ltd. All rights reserved
dc.source.urihttps://doi.org/10.1016/j.bmc.2010.06.051
dc.subjectCHO Cells
dc.subjectAnimals
dc.subjectCricetulus
dc.subjectRats
dc.subjectRats, Sprague-Dawley
dc.subjectNeuralgia
dc.subjectHyperalgesia
dc.subjectCyclopropanes
dc.subjectGlycine
dc.subjectReceptors, Metabotropic Glutamate
dc.subjectAnalgesics
dc.subjectCricetinae
dc.subjectMale
dc.titleA new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity
dc.typeJournal article
pubs.publication-statusPublished

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