Metabotropic Glutamate Receptors as Targets for Analgesia: Antagonism, Activation, and Allosteric Modulation

Montana MC, Gereau RW 4th (2011). Curr Pharm Biotechnol, Epub
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The metabotropic glutamate receptors (mGluRs) are expressed pre- and post-synaptically throughout the nervous system where they serve as modulators of synaptic transmission and neuronal excitability. Activation of mGluRs can be pro- or anti-nociceptive, depending on their anatomic location and the signaling cascades to which they couple. Antagonists of Group I mGluRs and agonists of Group II and III mGluRs have shown therapeutic promise in animal pain models. This article reviews the potential therapeutic utility of several agents that act predominantly via mGluRs, specifically focusing on their analgesic efficacy and discussing possible off-target effects.

Posted on October 19, 2011
Posted in: Axon Injury & Repair, Publications, Therapeutics & Diagnostics Authors: