Update on melatonin receptors: IUPHAR Review 20

被引：321

作者：

Jockers, Ralf ^{[1
,2
,3
]}

Delagrange, Philippe ^{[4
]}

Dubocovich, Margarita L. ^{[5
]}

Markus, Regina P. ^{[6
]}

Renault, Nicolas ^{[7
]}

Tosini, Gianluca ^{[8
,9
]}

Cecon, Erika ^{[1
,2
,3
]}

Zlotos, Darius P. ^{[10
]}

机构：

[1] Inst Cochin, INSERM, U1016, 22 Rue Mechain, F-75014 Paris, France

[2] CNRS, UMR 8104, Paris, France

[3] Univ Paris 05, Paris, France

[4] Inst Rech Servier, Croissy Sur Seine, France

[5] SUNY Buffalo, Jacobs Sch Med & Biomed Sci, Dept Pharmacol & Toxicol, Buffalo, NY USA

[6] Univ Sao Paulo, Inst Biosci, Sao Paulo, Brazil

[7] LIRIC, UFR Pharm, INSERM, UMR 995, Lille, France

[8] Morehouse Sch Med, Inst Neurosci, Atlanta, GA 30310 USA

[9] Morehouse Sch Med, Dept Pharmacol & Toxicol, Atlanta, GA 30310 USA

[10] German Univ Cairo, Dept Pharmaceut Chem, Cairo, Egypt

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 2016年 / 173卷 / 18期

基金：

美国国家卫生研究院; 英国惠康基金; 巴西圣保罗研究基金会;

关键词：

PROTEIN-COUPLED RECEPTOR; NERVE TRANSECTION DECREASES; RAT SUPRACHIASMATIC NUCLEUS; FASTING PLASMA-GLUCOSE; MT2; MELATONIN; ALZHEIMERS-DISEASE; CRYSTAL-STRUCTURE; CONCISE GUIDE; PHARMACOLOGICAL CHARACTERIZATION; MOLECULAR PHARMACOLOGY;

D O I：

10.1111/bph.13536

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：2702 / 2725

页数：24

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