A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity
Research output: Contribution to journal › Journal article › Research › peer-review
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.
|Journal||Bioorganic & Medicinal Chemistry|
|Publication status||Published - 2010|
Keywords: 1,2-Dioxines; Carboxycyclopropylglycines; Metabotropic glutamate receptors; In vivo; Neuropathic pain; Allodynia
- Former Faculty of Pharmaceutical Sciences