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In mammals, including humans, the neurohormone melatonin is mainly secreted from the pineal gland at night and acts on two high-affinity G protein-coupled receptors, the melatonin MT1 and MT2 receptors. Major functions of melatonin receptors in the brain are the regulation of circadian rhythms and sleep. Correspondingly, the main indications of the currently available drugs for these receptors indicate this as targets. Yet these drugs may not only improve circadian rhythm- and sleep-related disorders but may also be beneficial for complex diseases like major depression, Alzheimer's disease, autism, and attention-deficit/hyperactivity disorders. Here, we will focus on the hypothalamic functions of melatonin receptors by updating our knowledge on their hypothalamic expression pattern at normal, aged, and disease states, by discussing their capacity to regulate circadian rhythms and sleep and by presenting the clinical applications of the melatonin receptor-targeting drugs ramelteon, tasimelteon, and agomelatine or of prolonged-release melatonin formulations. Finally, we speculate about future trends in the field of melatonin receptor drugs. Copyright © 2021 Elsevier B.V. All rights reserved.


Atsuro Oishi, Florence Gbahou, Ralf Jockers. Melatonin receptors, brain functions, and therapies. Handbook of clinical neurology. 2021;179:345-356

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PMID: 34225974

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