Metabotropic glutamate receptor 5

Metabotropic glutamate receptor 5 (mGluR5) is a type of G protein-coupled receptor (GPCR) that is activated by the neurotransmitter glutamate. It is part of the metabotropic glutamate receptor family, which plays a crucial role in the modulation of synaptic transmission and neuronal excitability.

Structure

mGluR5 is a large protein composed of 1212 amino acids. It has a seven-transmembrane domain structure, characteristic of GPCRs, with an extracellular N-terminus and an intracellular C-terminus. The N-terminus contains the glutamate binding site, while the C-terminus is involved in intracellular signaling pathways.

Function

mGluR5 receptors are primarily found in the central nervous system, including the cerebral cortex, hippocampus, and basal ganglia, where they regulate a variety of physiological processes. They modulate synaptic plasticity, a key process in learning and memory, and are involved in the regulation of neuronal excitability. mGluR5 receptors also play a role in neurodevelopment and have been implicated in several neurological and psychiatric disorders.

Clinical significance

Alterations in mGluR5 function have been associated with a range of neurological and psychiatric disorders, including schizophrenia, depression, anxiety disorders, and fragile X syndrome. mGluR5 antagonists have shown promise in preclinical and clinical trials for these disorders. Additionally, mGluR5 has been implicated in drug addiction, with mGluR5 antagonists reducing drug-seeking behavior in animal models.

Pharmacology

Several drugs that target mGluR5 have been developed for therapeutic use. These include both agonists, which activate the receptor, and antagonists, which block its activity. mGluR5 antagonists have been investigated for their potential use in treating conditions such as Parkinson's disease, chronic pain, and anxiety disorders.

See also

• Metabotropic glutamate receptor
• G protein-coupled receptor
• Glutamate receptor

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