title: Metabotropic glutamate receptor 5 - a promising target in drug development and neuroimaging.
abstract: This review summarizes the contributions by various teams of scientists in assessing the metabotropic glutamate receptor 5 (mGluR5) as a biomarker in neuropsychiatric disorders and diseases. Development of positive and negative allosteric modulators of mGluR5 is reviewed, as is the development of PET radioligands that have the potential to measure mGluR5 receptor density in neurological disorders and during therapeutic interventions. PET imaging provides an effective tool to assess the specificity of new drugs, select dose regimens in clinical trials, and study drug mechanisms of action. We summarize and deliver comparative analyses of mGluR5-specific PET radiotracers and their applications in understanding the pathophysiology of mGluR5-related nervous system disorders and to speed up drug development.
authors.affiliation: Department of Psychiatry, Stony Brook University Health Science Center, Stony Brook, NY, USA.
authors.forename: Rajapillai L I
authors.initials: RL
authors.lastname: Pillai
authors.affiliation: Department of Psychiatry, Stony Brook University Health Science Center, Stony Brook, NY, USA. dnyanesht@yahoo.com.
authors.forename: Dnyanesh N
authors.initials: DN
authors.lastname: Tipre
mesh_terms: D000818:Animals; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D001523:Mental Disorders / Q000000981:diagnostic imaging / Q000188:drug therapy; D058990:Molecular Targeted Therapy / Q000379:methods*; D009422:Nervous System Diseases / Q000000981:diagnostic imaging / Q000188:drug therapy; D059906:Neuroimaging / Q000379:methods*; D064529:Receptor, Metabotropic Glutamate 5 / Q000378:metabolism*
chemical_list: D064529:Receptor, Metabotropic Glutamate 5
keywords: CNS; Drug development; Neuroimaging; Positron emission tomography; mGluR5