Dipartimento Farmaceutico, Università degli Studi di Parma, Italy.
Expert Opin Ther Pat. 2010 Aug;20(8):1059-77. doi: 10.1517/13543776.2010.496455.
Increasing clinical evidences suggest that melatonin receptor agonists can represent a novel therapeutic approach for the treatment of sleep disturbances and depression. A variety of studies also revealed a role of melatonin and its receptors in different patho-physiological conditions. Due to the multiple effects of this hormone, the design of new agents able to interact selectively with melatonin receptors has become an area of great interest during the last decade.
An extensive inspection of patents and scientific literature about MT(1) and MT(2) melatonin receptor agonists reported from 1999 to early 2010.
A comprehensive review of structures recently claimed as melatonin receptor agonists and a broad overview of structure-activity relationships for these ligands.
After 5 decades of research, the field of melatonin receptor agonists comprises a variety of chemical entities, belonging to structurally different classes. Patents filed since 1999 claim new melatonin receptor agonists, characterized either by improved pharmacokinetic or pharmacodynamic properties, compared to those of melatonin receptor agonists already approved for clinical uses. The results of preclinical studies on animal models show that melatonin receptor agonists can be considered promising agents for the treatment of CNS-related pathologies.
越来越多的临床证据表明，褪黑素受体激动剂可能代表一种治疗睡眠障碍和抑郁症的新的治疗方法。各种研究也揭示了褪黑素及其受体在不同病理生理条件下的作用。由于这种激素的多种作用，设计能够选择性地与褪黑素受体相互作用的新型药物已成为过去十年的一个研究热点。
对 1999 年初至 2010 年初报道的 MT(1)和 MT(2)褪黑素受体激动剂的专利和科学文献进行了广泛的检查。
对最近被称为褪黑素受体激动剂的结构的全面回顾，以及这些配体的结构-活性关系的广泛概述。
经过 50 年的研究，褪黑素受体激动剂领域包含了多种化学实体，属于结构不同的类别。自 1999 年以来提交的专利声称具有新的褪黑素受体激动剂，与已经批准用于临床用途的褪黑素受体激动剂相比，这些激动剂具有改善的药代动力学或药效学特性。对动物模型的临床前研究结果表明，褪黑素受体激动剂可被视为治疗中枢神经系统相关疾病的有前途的药物。
