Metabotropic glutamate receptor 5 (mGluR5) (mGluR5)

Metabotropic glutamate receptor 5 (mGluR5) is a Class C G protein-coupled receptor that plays a critical role in modulating excitatory neurotransmission in the central nervous system (UniProt P41594). It is primarily coupled to the Gq/11 signaling pathway, leading to the activation of phospholipase C and subsequent intracellular calcium release (PubMed: 25159913). mGluR5 is widely expressed in the cerebral cortex, hippocampus, and basal ganglia, where it regulates synaptic plasticity, long-term depression, and cognitive functions (PubMed: 18443503). Dysregulation of mGluR5 signaling is implicated in a variety of neurological and psychiatric conditions, including Fragile X syndrome, schizophrenia, and Parkinson's disease (PubMed: 21854749). Consequently, it has become a significant therapeutic target for the development of allosteric modulators, such as negative allosteric modulators (NAMs) for Fragile X and positive allosteric modulators (PAMs) for schizophrenia, aimed at treating cognitive deficits and movement disorders (PubMed: 24635425).

Other names

GRM5GPRC1EmGlu5Metabotropic glutamate receptor subtype 5

Negative allosteric modulation (NAM), Positive allosteric modulation (PAM), and orthosteric antagonism or agonism of the metabotropic glutamate receptor 5.