Metabotropic glutamate receptor 5 is an excitatory G q -coupled G protein-coupled receptor [5] predominantly expressed on the postsynaptic sites of neurons. [6] . In humans, it is encoded by the GRM5 gene. [7][8]

mGluR5 knockout mice have been intensely studied in models of learning and memory, addiction, motor regulation, and obesity. Most recently, mGluR5 has emerged as a novel player in the treatment of fragile X syndrome based, in part, on studies with knockout animals (discussed further in the following section).

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. Keywords: CNS; Drug development; Neuroimaging; Positron emission tomography; mGluR5.

2023年2月16日 · Pharmacological manipulation of mGluR5 has showed that mGluR5 is implicated in the pathophysiology of anxiety and mGluR5 has been proposed as a potential drug target for anxiety disorders....

We have provided an overview of the justification of targeting mGlu5 receptors in the treatment of these disorders, summarized the preclinical evidence for negatively modulating mGlu5 receptors as a therapeutic target for MDD and nicotine dependence …

This article provides medicinal chemistry highlights around the chemical classes of potent and highly selective mGluR5 negative allosteric modulators (NAMs) and their therapeutic potential. In addition, it describes the medicinal chemistry approach from the discovery to the clinical candidate selection of a new series of heteroaryl ...

PET is an attractive molecular imaging modality that can deliver quantitative measures of biochemical parameters such as concentrations of receptors, transporters or enzymes in target organs. PET could provide an effective tool to assess specificity of mGluR5 drugs, selection of dose regimens in clinical trials, and drug mechanisms of action.

Furthermore, selective agents acting as allosteric antagonists at the mGluR5 subtype have demonstrated therapeutic potential. The identification and characterization of mGluR5 antagonists and recent progress in clinical development are summarized.

2014年1月28日 · Metabotropic glutamate receptor subtype 5 (mGluR5) is an exciting novel drug target for the treatment of psychiatric disorders including schizophrenia and major depression [1,2].

2024年11月5日 · Drug discovery efforts directed toward metabotropic glutamate receptor subtype 5 (mGlu 5) have been particularly fruitful, with a wealth of drug candidates and pharmacological tools identified. mGlu 5 negative allosteric modulators (NAMs) are promising novel therapeutics for developmental, neuropsychiatric and neurodegenerative disorders (e.g ...