title: Understanding melatonin receptor pharmacology: latest insights from mouse models, and their relevance to human disease.
abstract: Melatonin, the neuro-hormone synthesized during the night, has recently seen an unexpected extension of its functional implications toward type 2 diabetes development, visual functions, sleep disturbances, and depression. Transgenic mouse models were instrumental for the establishment of the link between melatonin and these major human diseases. Most of the actions of melatonin are mediated by two types of G protein-coupled receptors, named MT1 and MT2 , which are expressed in many different organs and tissues. Understanding the pharmacology and function of mouse MT1 and MT2 receptors, including MT1 /MT2 heteromers, will be of crucial importance to evaluate the relevance of these mouse models for future therapeutic developments. This review will critically discuss these aspects, and give some perspectives including the generation of new mouse models.
authors.affiliation: Neuroscience Institute and Department of Pharmacology and Toxicology, Morehouse School of Medicine, Atlanta, GA, USA.
authors.forename: Gianluca
authors.initials: G
authors.lastname: Tosini
authors.forename: Sharon
authors.initials: S
authors.lastname: Owino
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Guillaume
authors.forename: Ralf
authors.initials: R
authors.lastname: Jockers
mesh_terms: D000818:Animals; D002940:Circadian Rhythm; D003924:Diabetes Mellitus, Type 2 / Q000378:metabolism; D004195:Disease Models, Animal; D006801:Humans; D008550:Melatonin / Q000502:physiology; D051379:Mice; D017440:Photoperiod; D044094:Receptors, Melatonin / Q000502:physiology*; D015398:Signal Transduction; D012890:Sleep
chemical_list: D044094:Receptors, Melatonin; D008550:Melatonin
keywords: circadian rhythm; diabetes; melatonin; melatonin receptors; photoperiodism; retina; sleep