褪黑素能类药物研究进展

Melatonergic drugs: research advances

褪黑激素(美乐托宁)是一种专司调节生物节律的神经激素,具有调节免疫系统、抑制肿瘤细胞增殖、保护胃肠道、抗脑损伤和痛觉调制等多种生理作用。褪黑激素主要通过介导两个G蛋白偶联受体MT1和MT2而发挥作用。由于其半衰期短、临床应用受限,多种褪黑激素衍生物和类似物被研究,以获得活性高、药代动力学性质良好的药物。本文主要介绍已上市和处于临床试验的褪黑素能类药物的研究概况。

Melatonin is a hormone responsible for regulating biological rhythms. It has multiple physiological actions such as immune regulation, inhibition of tumor, gastrointestinal tract protection, brain injury prevention and pain regulation, and exerts its ac- tions mainly through two G-protein-coupled receptors MT1 and MT2. To overcome its shortcomings of short half-life and limited clinical application, a variety of melatonin derivatives and analogues have been developed in order to get compounds with high activity and good pharmacokinetic properties. Recent advances in melatonergic drugs which have been listed or in clinical trials are summarized in this review.