Artículo
International union of basic and clinical pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors
Dubocovich, Margarita L.; Delagrange, Philippe; Krause, Diana N.; Sugden, David; Cardinali, Daniel Pedro
; Olcese, James
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Fecha de publicación:
09/2010
Editorial:
American Society for Pharmacology and Experimental Therapeutics
Revista:
Pharmacological Reviews
ISSN:
0031-6997
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
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, MT1 and MT2, 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.
Palabras clave:
MELATONINA
,
NOMENCLATURA
,
FARMACOLOGIA
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Articulos(SEDE CENTRAL)
Articulos de SEDE CENTRAL
Articulos de SEDE CENTRAL
Citación
Dubocovich, Margarita L.; Delagrange, Philippe; Krause, Diana N.; Sugden, David; Cardinali, Daniel Pedro; et al.; International union of basic and clinical pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors; American Society for Pharmacology and Experimental Therapeutics; Pharmacological Reviews; 62; 3; 9-2010; 343-380
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