Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/61716
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dc.contributor.author | Stanley, N. | - |
dc.contributor.author | Hutchinson, M. | - |
dc.contributor.author | Kvist, T. | - |
dc.contributor.author | Nielsen, B. | - |
dc.contributor.author | Mathiesen, J. | - |
dc.contributor.author | Brauner-Osborne, H. | - |
dc.contributor.author | Avery, T. | - |
dc.contributor.author | Tiekink, E. | - |
dc.contributor.author | Pedersen, D. | - |
dc.contributor.author | Irvine, R. | - |
dc.contributor.author | Abell, A. | - |
dc.contributor.author | Taylor, D. | - |
dc.date.issued | 2010 | - |
dc.identifier.citation | Bioorganic and Medicinal Chemistry, 2010; 18(16):6089-6098 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.issn | 1464-3391 | - |
dc.identifier.uri | http://hdl.handle.net/2440/61716 | - |
dc.description.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. | - |
dc.description.statementofresponsibility | 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 | - |
dc.language.iso | en | - |
dc.publisher | Pergamon-Elsevier Science | - |
dc.rights | © 2010 Elsevier Ltd. All rights reserved | - |
dc.source.uri | http://dx.doi.org/10.1016/j.bmc.2010.06.051 | - |
dc.subject | CHO Cells | - |
dc.subject | Animals | - |
dc.subject | Cricetulus | - |
dc.subject | Rats | - |
dc.subject | Rats, Sprague-Dawley | - |
dc.subject | Neuralgia | - |
dc.subject | Hyperalgesia | - |
dc.subject | Cyclopropanes | - |
dc.subject | Glycine | - |
dc.subject | Receptors, Metabotropic Glutamate | - |
dc.subject | Analgesics | - |
dc.subject | Cricetinae | - |
dc.subject | Male | - |
dc.title | A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1016/j.bmc.2010.06.051 | - |
dc.relation.grant | http://purl.org/au-research/grants/nhmrc/465423 | - |
pubs.publication-status | Published | - |
dc.identifier.orcid | Stanley, N. [0000-0002-2625-9876] | - |
dc.identifier.orcid | Hutchinson, M. [0000-0003-2154-5950] | - |
dc.identifier.orcid | Avery, T. [0000-0001-6882-5461] | - |
dc.identifier.orcid | Abell, A. [0000-0002-0604-2629] | - |
dc.identifier.orcid | Taylor, D. [0000-0002-3302-4610] [0000-0002-4274-3983] [0000-0003-0633-7424] | - |
Appears in Collections: | Aurora harvest Chemistry publications IPAS publications |
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