Frontiers in CNS Drug Discovery

Volume: 1

Indexed in: Scopus, EMBASE, Book Citation Index, Science Edition, BIOSIS

“Frontiers in CNS Drug Discovery” is an eBook series devoted to publishing the latest and the most important advances in Central Nervous System (CNS) drug design and discovery. Eminent scientists ...
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In Search of Novel and Therapeutically Significant Melatoninergic Ligands

Pp. 600-610 (11)

Sejal M. Mody, Yueqing Hu, Maurice K.C.Ho and Yung H. Wong

Abstract

Melatonin, the pineal gland hormone, is widely distributed in mammalian tissues and exerts its action via two melatonin receptor sub-types, MT1 and MT2. Melatonin is known to play functional roles in regulating circadian rhythms and seasonal reproduction. In recent years, growing evidence has also linked melatonin to a variety of other body systems and disease states, thus highlighting its significance as a therapeutic agent. However, due to its properties, melatonin is ineffective in clinical use, thus prompting the development of melatoninergic ligands that mimic the actions of melatonin but in a manner that is more potent and specific for melatonin receptors. An additional focus has been to develop ligands that exhibit receptor subtype selectivity. While there are over seventy patents on melatoninergic ligands, success in developing therapeutically effective melatoninergic ligands has been varied. However, the recent approval of Ramelteon for treatment of sleep disorders and the evaluation of other compounds in clinical trials have highlighted their clinical importance. In this review an overview of recently developed novel melatoninergic ligands is provided including recently filed patents and compounds undergoing clinical evaluation.

Keywords:

Melatonin, melatoninergic ligands, MT1 receptor, MT2 receptor, ramelteon, agomelatine, sleep disorders, patents

Affiliation:

Department of Biochemistry and Biotechnology Research Institute, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.