Target intelligence / Profile preview

Metabotropic glutamate receptor 5 (mGluR5)

Target
mGluR5
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

Metabotropic glutamate receptor 5 (mGluR5) is a G protein-coupled receptor (GPCR) that plays a critical role in the central nervous system, particularly in modulating excitatory neurotransmission and synaptic plasticity. Upon activation by glutamate, it couples to Gq proteins, leading to activation of phospholipase C and subsequent intracellular signaling cascades such as increased IP3 and calcium release. Altered mGluR5 function or expression has been implicated in various neuropsychiatric and neurodegenerative disorders, making it a potential therapeutic target.

Other names
GRM5
02

Mechanism of action

Allosteric modulation (positive and negative) of receptor activity

03

Biological functions

Signal transductionModulation of neuronal excitabilityModulation of synaptic plasticityRegulation of gene expression
04

Disease associations

Mood disorders (e.g., anxiety)Addiction (notably alcohol use disorder)Neurodegenerative diseases (including Alzheimer’s disease and Huntington’s disease)
05

Safety considerations

Potential for off-target effects due to widespread expression in the CNSComplex signaling pathways may lead to unpredictable effectsLong-term effects of chronic modulation are not fully understood

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