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.
Export Options
About this article
Cite this article as:
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 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Human Endometrial and Ovarian Cancer Cells: Histone Deacetylase Inhibitors Exhibit Antiproliferative Activity, Potently Induce Cell Cycle Arrest, and Stimulate Apoptosis
Current Medicinal Chemistry Natural Compounds and Drug Discovery: Can Cnidarian Venom Play a Role?
Central Nervous System Agents in Medicinal Chemistry The ALK Gene, An Attractive Target for Inhibitor Development
Current Topics in Medicinal Chemistry Modulation of intracellular pH in human ovarian cancer.
Current Molecular Medicine Nongenomic Actions of Thyroid Hormones: From Basic Research to Clinical Applications. An Update
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) <i>Uncaria tomentosa</i> (Willd. ex Schult.): Focus on Nutraceutical Aspects
Current Bioactive Compounds Gene Expression Under the Influence: Transcriptional Profiling of Ethanol in the Brain
Current Psychopharmacology Biotransformation of Microcystins in Eukaryotic Cells - Possible Future Research Directions
Mini-Reviews in Medicinal Chemistry Newer Insights in Personalized and Evidence Based Medicine- the Role of MicroRNAs
Current Pharmacogenomics and Personalized Medicine Adverse Effects and Safety of Etirinotecan Pegol, a Novel Topoisomerase Inhibitor, in Cancer Treatment: A Systematic Review
Current Cancer Therapy Reviews Membrane Rafts in the Respiratory System
Current Respiratory Medicine Reviews The Effects of Weightlessness on the Human Organism and Mammalian Cells
Current Molecular Medicine Neuroprotection with Natural Antioxidants and Nutraceuticals in the Context of Brain Cell Degeneration: The Epigenetic Connection
Current Topics in Medicinal Chemistry Maternal Choline Supplementation: A Potential Prenatal Treatment for Down Syndrome and Alzheimer’s Disease
Current Alzheimer Research Sigma Receptors in Oncology: Therapeutic and Diagnostic Applications of Sigma Ligands
Current Pharmaceutical Design Pharmacological Approaches of Neurofibrillary Degeneration
Current Alzheimer Research Antibodies for Therapeutic Uses and the Evolution of Biotechniques
Current Medicinal Chemistry Role of Metal Ions in the Aβ Oligomerization in Alzheimers Disease and in Other Neurological Disorders
Current Alzheimer Research Glycosphingolipid Structure and Function in Membranes
Current Organic Chemistry Ubiquitin-Proteasome Pathway Components as Therapeutic Targets for CNS Maladies
Current Pharmaceutical Design