Please use this identifier to cite or link to this item:
|Scopus||Web of Science®||Altmetric|
|Title:||A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity|
|Citation:||Bioorganic & Medicinal Chemistry, 2010; 18(16):6089-6098|
|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|
|Appears in Collections:||Chemistry publications|
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.