Metabotropic glutamate receptors: physiology, pharmacology, and disease.

Niswender CM, Conn PJ
Annu Rev Pharmacol Toxicol. 2010 50: 295-322

PMID: 20055706 · PMCID: PMC2904507 · DOI:10.1146/annurev.pharmtox.011008.145533

The metabotropic glutamate receptors (mGluRs) are family C G-protein-coupled receptors that participate in the modulation of synaptic transmission and neuronal excitability throughout the central nervous system. The mGluRs bind glutamate within a large extracellular domain and transmit signals through the receptor protein to intracellular signaling partners. A great deal of progress has been made in determining the mechanisms by which mGluRs are activated, proteins with which they interact, and orthosteric and allosteric ligands that can modulate receptor activity. The widespread expression of mGluRs makes these receptors particularly attractive drug targets, and recent studies continue to validate the therapeutic utility of mGluR ligands in neurological and psychiatric disorders such as Alzheimer's disease, Parkinson's disease, anxiety, depression, and schizophrenia.

MeSH Terms (7)

Allosteric Regulation Alternative Splicing Animals Humans Protein Structure, Tertiary Receptors, Metabotropic Glutamate Signal Transduction

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