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

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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.
OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind18
Udgave nummer16
Sider (fra-til)6089-6098
ISSN0968-0896
DOI
StatusUdgivet - 2010

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Copyright © 2010 Elsevier Ltd. All rights reserved.

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