Abstract

Pineal hormone melatonin is widely used in the treatment of disorders of circadian rhythms. The presence of melatonin receptors in various animal tissues motivates the use of this hormone in some other diseases. For this reason, in recent years investigators continued the search for synthetic analogues of melatonin which are metabolically stable and selective to receptors. This review includes recent information about the most famous melatonin analogues, their structure, properties, and physiological features of the interaction with melatonin receptors.

Highlights

  • Almost since its opening in the mid-20th century epiphyseal hormone melatonin is seen as a valuable pharmacological agent

  • Structure-activity relationships (SARs) of melatonin derivatives have been comprehensively analyzed [62,63,64,65], and we only summarize general strategies used in the development of melatoninergic ligands

  • After half a century of studying melatonin, it is considered as an integral part of the homeostatic mechanisms of the organism and a hormone involved in regulating a large number of various physiological processes

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Summary

Introduction

Almost since its opening in the mid-20th century epiphyseal hormone melatonin is seen as a valuable pharmacological agent. The positive results of the use of melatonin were obtained for the treatment of insomnia, circadian rhythm disorders associated with shift work, the change of time zones, and seasonal disorders [1,2,3]. The company Neurim Pharmaceuticals has produced drug called Circadin, mimicking physiological profile of epiphyseal hormone secretion. The second path involves the creation of more stable agonists, which could selectively bind with a specific type of melatonin receptor. At present, this area is considered to be more promising.

Melatonin
Melatonin Receptors
Melatonin Binding Sites
Synthetic Ligands of Melatonin Receptors
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Findings
Conclusion
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