Jockers Ralf, Delagrange Philippe, Dubocovich Margarita L, Markus Regina P, Renault Nicolas, Tosini Gianluca, Cecon Erika, Zlotos Darius P
Inserm, U1016, Institut Cochin, Paris, France.
CNRS UMR 8104, Paris, France.
Br J Pharmacol. 2016 Sep;173(18):2702-25. doi: 10.1111/bph.13536. Epub 2016 Aug 8.
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.
褪黑素受体是属于GPCR超家族的七次跨膜蛋白。在哺乳动物中，存在两种褪黑素受体亚型——MT1和MT2——分别由MTNR1A和MTNR1B基因编码。本综述由国际基础与临床药理学联合会相应小组委员会提供褪黑素受体的最新信息。我们将重点介绍褪黑素受体配体（包括放射性配体）的最新进展，并给出褪黑素受体敲除小鼠最新表型分析结果的最新情况。将总结褪黑素受体结构的现状和前景。将讨论褪黑素受体二聚体的生理重要性以及褪黑素受体与2型糖尿病相关的生物学重要遗传变异。褪黑素受体在生理学和疾病中的作用将通过其在免疫系统和中枢神经系统中的功能进一步举例说明。最后，将批判性地探讨褪黑素的抗氧化和自由基清除特性及其与褪黑素受体的关系。
