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Pharmacol Rev. 2010 Sep;62(3):343-80. doi: 10.1124/pr.110.002832. Epub 2010 Jul 6.

International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors.

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  • 1Department of Pharmacology and Toxicology, School of Medicine and Biomedical Sciences, University at Buffalo State University of New York, 3435 Main Street, Buffalo, NY 14214, USA. mdubo@buffalo.edu

Abstract

The hormone melatonin (5-methoxy-N-acetyltryptamine) is synthesized primarily in the pineal gland and retina, and in several peripheral tissues and organs. In the circulation, the concentration of melatonin follows a circadian rhythm, with high levels at night providing timing cues to target tissues endowed with melatonin receptors. Melatonin receptors receive and translate melatonin's message to influence daily and seasonal rhythms of physiology and behavior. The melatonin message is translated through activation of two G protein-coupled receptors, MT(1) and MT(2), that are potential therapeutic targets in disorders ranging from insomnia and circadian sleep disorders to depression, cardiovascular diseases, and cancer. This review summarizes the steps taken since melatonin's discovery by Aaron Lerner in 1958 to functionally characterize, clone, and localize receptors in mammalian tissues. The pharmacological and molecular properties of the receptors are described as well as current efforts to discover and develop ligands for treatment of a number of illnesses, including sleep disorders, depression, and cancer.

PMID:
20605968
PMCID:
PMC2964901
DOI:
10.1124/pr.110.002832
[PubMed - indexed for MEDLINE]
Free PMC Article
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