A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity
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 carboxycyclopro...
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| Main Authors: | , , , , , , , , , , , |
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| Format: | Article |
| Published: |
Elsevier
2010
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| Subjects: | |
| Online Access: | http://eprints.um.edu.my/12517/ |
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| Summary: | 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. (C) 2010 Elsevier Ltd. All rights reserved. |
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