Abstract
Metabotropic glutamate (mGlu) receptors are G protein-coupled receptors expressed primarily on neurons and glial cells modulating the effects of glutamatergic neurotransmission. The pharmacological manipulation of these receptors has been postulated to be valuable in the management of some neurological disorders. Accordingly, the targeting of mGlu5 receptors as a therapeutic approach for Parkinson’s disease (PD) has been proposed, especially to manage the adverse symptoms associated to chronic treatment with classical PD drugs. Thus, the specific pharmacological blocking of mGlu5 receptors constitutes one of the most attractive non-dopaminergic-based strategies for PD management in general and for the L-DOPA-induced diskynesia (LID) in particular. Overall, we provide here an update of the current state of the art of these mGlu5 receptor-based approaches that are under clinical study as agents devoted to alleviate PD symptoms.
Keywords: mGlu5R; Parkinson’s disease, GPCR oligomerization, clinical trial, AFQ056.
CNS & Neurological Disorders - Drug Targets
Title:Targeting Striatal Metabotropic Glutamate Receptor Type 5 in Parkinson’s Disease: Bridging Molecular Studies and Clinical Trials
Volume: 12 Issue: 8
Author(s): A. Vallano, V. Fernandez-Duenas, G. Garcia-Negredo, M.A. Quijada, C.P. Simon, M.L. Cuffí, L. Carbonell, S. Sanchez, J.M. Arnau and F. Ciruela
Affiliation:
Keywords: mGlu5R; Parkinson’s disease, GPCR oligomerization, clinical trial, AFQ056.
Abstract: Metabotropic glutamate (mGlu) receptors are G protein-coupled receptors expressed primarily on neurons and glial cells modulating the effects of glutamatergic neurotransmission. The pharmacological manipulation of these receptors has been postulated to be valuable in the management of some neurological disorders. Accordingly, the targeting of mGlu5 receptors as a therapeutic approach for Parkinson’s disease (PD) has been proposed, especially to manage the adverse symptoms associated to chronic treatment with classical PD drugs. Thus, the specific pharmacological blocking of mGlu5 receptors constitutes one of the most attractive non-dopaminergic-based strategies for PD management in general and for the L-DOPA-induced diskynesia (LID) in particular. Overall, we provide here an update of the current state of the art of these mGlu5 receptor-based approaches that are under clinical study as agents devoted to alleviate PD symptoms.
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Vallano A., Fernandez-Duenas V., Garcia-Negredo G., Quijada M.A., Simon C.P., Cuffí M.L., Carbonell L., Sanchez S., Arnau J.M. and Ciruela F., Targeting Striatal Metabotropic Glutamate Receptor Type 5 in Parkinson’s Disease: Bridging Molecular Studies and Clinical Trials, CNS & Neurological Disorders - Drug Targets 2013; 12 (8) . https://dx.doi.org/10.2174/18715273113129990115
DOI https://dx.doi.org/10.2174/18715273113129990115 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
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