论文部分内容阅读
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。
Meleotronin receptors are widely present in the central nervous system and in other tissues of the body. The endogenous ligands, meleldonin, act on different subtype receptors (MT1, MT2 and MT3) and are involved in the regulation of different physiological functions of the body . Since melatonin itself has no subtype selectivity, selective ligand studies of different subtype receptors are of great importance to the physiological role of subtype receptors and the development of new drugs. This review summarizes the studies on the more mature MT2 receptor selective ligands and explores the development of receptor ligands for melo tolbutamide by studying the relationship between ligand structure and affinity and selectivity Provide guidance.