Understanding melatonin receptor pharmacology: Latest insights from mouse models, and their relevance to human disease

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 be...

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Bibliographic Details
Published in:BioEssays 2014-08, Vol.36 (8), p.778-787
Main Authors: Tosini, Gianluca, Owino, Sharon, Guillaume, Jean-Luc, Jockers, Ralf
Format: Article
Language:English
Subjects:
Animals
Circadian Rhythm
diabetes
Diabetes Mellitus, Type 2 - metabolism
Disease Models, Animal
Humans
melatonin
Melatonin - physiology
melatonin receptors
Mice
Photoperiod
photoperiodism
Receptors, Melatonin - physiology
retina
Rodents
Signal Transduction
Sleep
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Summary: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. Melatonin is synthesized at night and regulates many physiological functions. Melatonin acts via two types of receptors (MT1 and MT2), which are expressed in many different tissues. Melatonin receptors knock‐out mice have provided an important tool to understand the role of melatonin signaling in the pathogenesis of many diseases.
ISSN:0265-9247
1521-1878
DOI:10.1002/bies.201400017