Update on melatonin receptors: IUPHAR Review 20.
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.
Inserm, U1016, Institut Cochin, Paris, France.|CNRS UMR 8104, Paris, France.|University Paris Descartes, Paris, France.
Ralf
R
Jockers
Institut de Recherches Servier, Croissy, France.
Philippe
P
Delagrange
Department Pharmacology and Toxicology, Jacobs School of Medicine and Biomedical Science, University at Buffalo (SUNY), Buffalo, USA.
Margarita L
ML
Dubocovich
Institute of Biosciences, University of São Paulo, São Paulo, Brazil.
Regina P
RP
Markus
Inserm UMR 995, LIRIC, UFR Pharmacie, Lille, France.
Nicolas
N
Renault
Neuroscience Institute and Department of Pharmacology and Toxicology, Morehouse School of Medicine, Atlanta, GA, USA.
Gianluca
G
Tosini
Inserm, U1016, Institut Cochin, Paris, France.|CNRS UMR 8104, Paris, France.|University Paris Descartes, Paris, France.
Erika
E
Cecon
Department of Pharmaceutical Chemistry, The German University in Cairo, New Cairo City, Cairo, Egypt.
Darius P
DP
Zlotos
D000818:Animals; D006801:Humans; D008024:Ligands; D044094:Receptors, Melatonin / Q000737:chemistry / Q000172:deficiency / Q000276:immunology
D008024:Ligands; D044094:Receptors, Melatonin