Cited by 364Circadian rhythm and melatoninSleep and Wakefulness ResearchSleep and Work-Related Fatigue

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Melatonin receptors: Role on sleep and circadian rhythm regulation

Dubocovich, Margarita L.·2007·Sleep Medicine

DOI 10.1016/j.sleep.2007.10.007

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Abstract

The circadian release of the hormone melatonin is regulated by the suprachiasmatic nucleus (SCN), which feeds back into the nucleus to modulate sleep and circadian phase through activation of the MT(1) and/or MT(2) melatonin receptors. Considering the functions of the SCN as a sleep and circadian rhythm regulator, melatonin and melatonin receptor agonists have attracted interest as being possible treatments for sleep and circadian rhythm sleep disorders. Part of this interest has centered on elucidating which melatonin receptors are targets for the regulation of these functions within the SCN. Two G-protein coupled melatonin receptors, the MT(1) and MT(2), inhibit neuronal activity and phase shift circadian firing rhythms in the SCN, respectively. Recent reports have uncovered possible interactions between the two types of receptors in the mammalian SCN, as well as the role of physiological and supraphysiological levels of melatonin on the molecular pharmacology and cellular changes of human and rodent melatonin receptors via desensitization and internalization mechanisms. These data outline the complexity of the interplay between melatonin and its receptors in the SCN and their corresponding roles in sleep and circadian regulation. Although further studies are necessary, a great deal of progress has been made toward understanding how melatonin and its agonists contribute to sleep and circadian phase changes, and how best to develop compounds that can target the functions of the SCN specifically and effectively.

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Authors: Dubocovich, M. L.
Affiliations: Northwestern University (US)
Corresponding author: Dubocovich, Margarita L.
ORCID: Dubocovich, Margarita L.
Venue: Sleep Medicine
Publisher: Elsevier BV
Published: 2007-12
Volume: 8
Pages: 34-42
ISSN: 1389-9457 (ISSN-L)
DOI: 10.1016/j.sleep.2007.10.007
OpenAlex: W2046526031
Cited by: 364
References: 44
Citations by year: 2026: 10 · 2025: 12 · 2024: 20 · 2023: 21 · 2022: 39 · 2021: 36 · 2020: 32 · 2019: 13 · 2018: 23 · 2017: 19 · 2016: 13 · 2015: 15 · 2014: 16 · 2013: 18 · 2012: 17
FWCI: 5.86
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Sleep Medicine (publishedVersion)
PubMed (publishedVersion)
Funders: U.S. Public Health Service (MH 42922, MH52685)
Topics: Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Circadian rhythm and melatonin
Life Sciences › Neuroscience › Cognitive Neuroscience › Sleep and Wakefulness Research
Social Sciences › Psychology › Experimental and Cognitive Psychology › Sleep and Work-Related Fatigue
Keywords: melatonin receptors, MT1 receptor, MT2 receptor, suprachiasmatic nucleus, circadian rhythm, sleep regulation, circadian phase shift, G protein-coupled receptors, receptor desensitization, receptor internalization, melatonin receptor agonists, sleep disorders, circadian rhythm sleep disorders
MeSH terms: Circadian Rhythm, Humans, Melatonin, Receptors, Cell Surface, Sleep, Suprachiasmatic Nucleus, Receptor, Melatonin, MT1, Receptor, Melatonin, MT2

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Melatonin receptors: Role on sleep and circadian rhythm regulation

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