美乐托宁受体MT_2亚型选择性配体的研究进展

Selective melatoninergic ligands for MT_2 subtype receptor

美乐托宁受体广泛存在于中枢神经系统以及机体其他组织中,其内源性配体美乐托宁可作用于不同亚型受体(MT1,MT2和MT3),参与调节机体的不同生理功能。由于美乐托宁自身无亚型选择性,因此不同亚型受体的选择性配体研究对亚型受体的生理作用和新药研发具有重要意义。本文对研究得较为成熟的MT2受体选择性配体研究做一综述,通过探讨配体结构与亲和性和选择性之间的关系,为美乐托宁受体亚型配体的开发研究提供指导。

Melatonin receptors have three different subtypes including MT~, MT2 and MT3, which are widely distributed in the central nervous system and in peripheral tissues. The endogenous ligand melatonin plays an important role in modulating diverse physiological activities through acting on MT1 , MT2 or MT3. As melatonin has no subtype-selectivity, it is very important to develop different subtype-selective ligands for receptor research and drug development. In order to provide guidance for develop high selective ligands, this paper focused on the MT2-selective ligand, and reviewed the relationship between the structure of ligand and selectivity of receptor subtype.