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Br J Pharmacol. 2016 Sep;173(18):2702-25. doi: 10.1111/bph.13536. Epub 2016 Aug 8.

Update on melatonin receptors: IUPHAR Review 20.

Author information

1
Inserm, U1016, Institut Cochin, Paris, France.
2
CNRS UMR 8104, Paris, France.
3
University Paris Descartes, Paris, France.
4
Institut de Recherches Servier, Croissy, France.
5
Department Pharmacology and Toxicology, Jacobs School of Medicine and Biomedical Science, University at Buffalo (SUNY), Buffalo, USA.
6
Institute of Biosciences, University of São Paulo, São Paulo, Brazil.
7
Inserm UMR 995, LIRIC, UFR Pharmacie, Lille, France.
8
Neuroscience Institute and Department of Pharmacology and Toxicology, Morehouse School of Medicine, Atlanta, GA, USA.
9
Department of Pharmaceutical Chemistry, The German University in Cairo, New Cairo City, Cairo, Egypt.

Abstract

Melatonin receptors are seven transmembrane-spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist - MT1 and MT2 - encoded by the MTNR1A and MTNR1B genes respectively. The current review provides an update on melatonin receptors by the corresponding subcommittee of the International Union of Basic and Clinical Pharmacology. We will highlight recent developments of melatonin receptor ligands, including radioligands, and give an update on the latest phenotyping results of melatonin receptor knockout mice. The current status and perspectives of the structure of melatonin receptor will be summarized. The physiological importance of melatonin receptor dimers and biologically important and type 2 diabetes-associated genetic variants of melatonin receptors will be discussed. The role of melatonin receptors in physiology and disease will be further exemplified by their functions in the immune system and the CNS. Finally, antioxidant and free radical scavenger properties of melatonin and its relation to melatonin receptors will be critically addressed.

PMID:
27314810
PMCID:
PMC4995287
DOI:
10.1111/bph.13536
[Indexed for MEDLINE]
Free PMC Article

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