Metabotropic Glutamate Receptor mGLUR5 Antibodies

mGluR5 (GRM5) is a Group I metabotropic glutamate receptor and a class C GPCR that plays a major role in mediating the postsynaptic effects of glutamate. It predominantly couples to Gq/11 proteins, activating phospholipase C, increasing intracellular Ca2+ and stimulating downstream PKC, ERK/MAPK and other signaling pathways. mGluR5 is widely expressed in the central nervous system, with particularly high levels in the cerebral cortex, hippocampus, striatum, amygdala and other regions involved in cognition, emotion and motor control. The receptor is mainly localized postsynaptically and forms functional complexes with NMDA receptors and other synaptic proteins, allowing it to regulate neuronal excitability and synaptic plasticity. mGluR5 signaling is involved in learning and memory, pain processing, anxiety, reward mechanisms and regulation of neuronal development. Abnormal mGluR5 activity has been implicated in several neurological and psychiatric disorders, including Fragile X syndrome, autism spectrum disorders, schizophrenia, depression, anxiety, epilepsy, Parkinson’s disease and chronic pain. Numerous selective negative allosteric modulators have been developed, including fenobam, mavoglurant, basimglurant and CTEP, which reduce receptor activity without directly competing with glutamate at the orthosteric binding site. Although these compounds have shown therapeutic potential in preclinical models and several have entered clinical trials, no selective mGluR5-targeting drug has yet achieved broad clinical approval. Overall, mGluR5 is one of the best-characterized CNS GPCR drug targets and remains an attractive receptor for developing allosteric modulators for neurological and psychiatric diseases. For more information on mGluR5 pharmacology please refer to the IUPHAR database. For further reading refer to:

Gregory KJ, Goudet C. (2021) International Union of Basic and Clinical Pharmacology. CXI. Pharmacology, Signaling, and Physiology of Metabotropic Glutamate Receptors. Pharmacol Rev, 73 (1): 521-569.