The DOI matches its Crossref record; 41 of the 44 references it cites were found in a registry or an index.
Melatonin receptors: Role on sleep and circadian rhythm regulation
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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“Melatonin not only mediates seasonal changes, but also affects influences circadian rhythms and sleep [see (Dubocovich, 2007), for review].”
From Biological rhythms, higher brain function, and behavior: Gaps, opportunities, and challenges (2009) · cites this paper as Dubocovich, 2007
Citations
Cites
Functional Selectivity and Classical Concepts of Quantitative Pharmacology
Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B. K., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M., et al. (2006) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.106.104463 · Cited by 1,131
The melatonin rhythm: both a clock and a calendar
Reiter, R. J. (1993) · Cellular and Molecular Life Sciences · doi:10.1007/bf01923947 · Cited by 997
Functional MT1 and MT2 Melatonin Receptors in Mammals
Dubocovich, M. L., & Markowska, M. (2005) · Endocrine · doi:10.1385/endo:27:2:101 · Cited by 832
Molecular Dissection of Two Distinct Actions of Melatonin on the Suprachiasmatic Circadian Clock
Liu, C., Weaver, D. R., Jin, X., Shearman, L. P., Pieschl, R. L., Gribkoff, V. K., & Reppert, S. M. (1997) · Neuron · doi:10.1016/s0896-6273(00)80350-5 · Cited by 723
Melatonin: The chemical expression of darkness
Reiter, R. J. (1991) · Molecular and Cellular Endocrinology · doi:10.1016/0303-7207(91)90087-9 · Cited by 634
Arendt, J., & Skene, D. J. (2005) · Sleep Medicine Reviews · doi:10.1016/j.smrv.2004.05.002 · Cited by 629
Dollins, A. B., Zhdanova, I. V., Wurtman, R. J., Lynch, H. J., & Deng, M. (1994) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.91.5.1824 · Cited by 579
Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist
Kato, K., Hirai, K., Nishiyama, K., Uchikawa, O., FUKATSU, K., Ohkawa, S., Kawamata, Y., Hinuma, S., & Miyamoto, M. (2004) · Neuropharmacology · doi:10.1016/j.neuropharm.2004.09.007 · Cited by 541
Molecular pharmacology regulation and function of mammalian melatonin receptors
Dubocovich, M. L. (2003) · Frontiers in bioscience · doi:10.2741/1089 · Cited by 453
Melatonin receptors step into the light: cloning and classification of subtypes
Reppart, S. M., Weaver, D. R., & Godson, C. (1996) · Trends in Pharmacological Sciences · doi:10.1016/0165-6147(96)10005-5 · Cited by 426
Dubocovich, M. L., Yun, K., Al‐Ghoul, W. M., Benloucif, S., & Masana, M. I. (1998) · The FASEB Journal · doi:10.1096/fasebj.12.12.1211 · Cited by 364
Lewy, A. J., Bauer, V. K., Ahmed, S., Thomas, K. H., Cutler, N. L., Singer, C. M., Moffit, M. T., & Sack, R. L. (1998) · Chronobiology International · doi:10.3109/07420529808998671 · Cited by 360
Dubocovich, M. L., Masana, M. I., Iacob, S., & Sauri, D. (1997) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/pl00004956 · Cited by 333
Hunt, A. E., Al‐Ghoul, W. M., Gillette, M. U., & Dubocovich, M. L. (2001) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.2001.280.1.c110 · Cited by 266
Molecular tools to study melatonin pathways and actions.
Boutin, J., Audinot, V., Ferry, G., & Delagrange, P. (2005) · TIPS - Trends in Pharmacological Sciences · doi:10.1016/j.tips.2005.06.006 · Cited by 265
McArthur, A. J., Hunt, A. E., & Gillette, M. U. (1997) · Endocrinology · doi:10.1210/endo.138.2.4925 · Cited by 263
New selective ligands of human cloned melatonin MT1 and MT2 receptors
Audinot, V., Mailliet, F., Brasseur, C., Bonnaud, A., Gall, A. L., Amossé, C., Dromaint, S., Rodriguez, M., Nagel, N., Galizzi, J., et al. (2003) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-003-0751-2 · Cited by 250
Targeted Disruption of the Mouse Mel1b Melatonin Receptor
Jin, X., von Gall, C., Pieschl, R. L., Gribkoff, V. K., Stehle, J. H., Reppert, S. M., & Weaver, D. R. (2003) · Molecular and Cellular Biology · doi:10.1128/mcb.23.3.1054-1060.2003 · Cited by 240
Functional Melatonin Receptors in Rat Ovaries at Various Stages of the Estrous Cycle
Soares, J. M., Masana, M. I., Erşahin, Ç. H., & Dubocovich, M. L. (2003) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.049916 · Cited by 210
Zhdanova, I. V. (2004) · Sleep Medicine Reviews · doi:10.1016/j.smrv.2004.04.003 · Cited by 208
Sleep Disorders Medicine. Basic Science, Technical Considerations and Clinical Aspects.
Olejniczak, P. W. (1999) · Journal of Clinical Neurophysiology · doi:10.1097/00004691-199911000-00009 · Cited by 184
G protein-coupled receptor adaptation mechanisms
Ferguson, S. S. G., & Caron, M. G. (1998) · Seminars in Cell and Developmental Biology · doi:10.1006/scdb.1997.0216 · Cited by 181
Effects of melatonin on neuronal activity in the rat suprachiasmatic nucleus in vitro
Shibata, S., Cassone, V. M., & Moore, R. Y. (1989) · Neuroscience Letters · doi:10.1016/0304-3940(89)90153-5 · Cited by 158
Gerdin, M. J., Masana, M. I., Rivera-Bermudez, M. A., Hudson, R. L., Earnest, D. J., Gillette, M. U., & Dubocovich, M. L. (2004) · The FASEB Journal · doi:10.1096/fj.03-1339com · Cited by 137
Pharmacological characterization of human recombinant melatonin mt1 and MT2 receptors
Browning, C., Beresford, I. J. M., Fraser, N., & Giles, H. (2000) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0703130 · Cited by 136
Melatonin in Patients with Reduced REM Sleep Duration: Two Randomized Controlled Trials
Kunz, D., Mahlberg, R., Müller, C., Tilmann, A., & Bes, F. (2004) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2002-021057 · Cited by 135
THE PINEAL GLAND AND MELATONIN: Molecular and Pharmacologic Regulation
Borjigin, J., Li, X., & Snyder, S. H. (1999) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.39.1.53 · Cited by 135
Dubocovich, M. L., Hudson, R. L., Sumaya, I. C., Masana, M. I., & Manna, E. (2005) · Journal of Pineal Research · doi:10.1111/j.1600-079x.2005.00230.x · Cited by 129
Melatonin promotes sleep in three species of diurnal nonhuman primates
Zhdanova, I. V., Geiger, D. A., Schwagerl, A. L., Leclair, O. U., Killiany, R., Taylor, J. A., Rosene, D. L., Moss, M. B., & Madras, B. K. (2002) · Physiology & Behavior · doi:10.1016/s0031-9384(02)00654-6 · Cited by 129
Melatonin-mediated regulation of human MT1 melatonin receptors expressed in mammalian cells
Gerdin, M. J., Masana, M. I., & Dubocovich, M. L. (2004) · Biochemical Pharmacology · doi:10.1016/j.bcp.2004.01.027 · Cited by 81
Melatonin limits transcriptional impact of phosphoCREB in the mouse SCN via the Mel1a receptor
von Gall, C., Weaver, D. R., Kock, M., Korf, H., & Stehle, J. H. (2000) · Neuroreport · doi:10.1097/00001756-200006260-00002 · Cited by 65
Design and Synthesis of Naphthalenic Dimers as Selective MT1Melatoninergic Ligands
Descamps‐Francois, C., Yous, S., Chavatte, P., Audinot, V., Bonnaud, A., Boutin, J. A., Delagrange, P., Bennejean, C., Renard, P., & Lesieur, D. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm0255872 · Cited by 63
Design of subtype selective melatonin receptor agonists and antagonists
Sugden, D., Yeh, L.-K., & Teh, M. (1999) · annales de biologie animale biochimie biophysique · doi:10.1051/rnd:19990306 · Cited by 61
MULCHAHEY, J. J., Goldwater, D. R., & Zemlan, F. P. (2004) · Life Sciences · doi:10.1016/j.lfs.2004.03.023 · Cited by 53
Handbook of Contemporary Neuropharmacology
(2006) · Wiley eBooks · doi:10.1002/9780470101001 · Cited by 46
Chokroverty, S. (2017) · Springer: New York · doi:10.1007/978-1-4939-6578-6 · Cited by 45
Agomelatine targets a range of major depressive disorder symptoms.
Dubocovich, M. L. (2006) · PubMed · Cited by 43
Handbook of Contemporary Neuropharmacology
Brown, W. A., Solomon, D. A., & Khan, A. O. (2007) · JAMA · doi:10.1001/jama.298.22.2682 · Cited by 27
The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems
(2000) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-57081-0 · Cited by 24
Melatonin Receptors in Central Nervous System
Dubocovich, M. L. (2007) · Wiley eBooks · doi:10.1002/9780470101001.hcn047 · Cited by 5
Kenakin, T. (2000) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-57081-0_8 · Cited by 4
Flagged first, then by citations
3 of the 44 references couldn’t be matched to a known paper.
Research works printed but not linked: 2
- Hudson, 2005, Distinct roles for MT1 and MT2 melatonin (MLT) receptors in MLT-mediated phase shifts of circadian rhythms, Neuropsychopharmacology, 30, S267
- Hudson, 2004, Melatonin (MLT) phase advances the circadian rhythm of neuronal firing rate in suprachiasmatic nucleus (SCN) slices of C57BL/6 mice through activation of MT2 MLT receptors, FASEB J, 18
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New perspectives on the role of melatonin in human sleep, circadian rhythms and their regulation
Zisapel, N. (2018) · British Journal of Pharmacology · doi:10.1111/bph.14116 · Cited by 947
Melatonin—A pleiotropic, orchestrating regulator molecule
Hardeland, R., Cardinali, D. P., Srinivasan, V., Spence, D. W., Brown, G. M., & Pandi-Perumal, S. R. (2011) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2010.12.004 · Cited by 843
MT1 and MT2 Melatonin Receptors: A Therapeutic Perspective
Liu, J., Clough, S. J., Hutchinson, A. J., Adamah‐Biassi, E. B., Popovska‐Gorevski, M., & Dubocovich, M. L. (2015) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010814-124742 · Cited by 660
Dubocovich, M. L., Delagrange, P., Krause, D. N., Sugden, D., Cardinali, D. P., & Olcese, J. (2010) · Pharmacological Reviews · doi:10.1124/pr.110.002832 · Cited by 636
Update on melatonin receptors: IUPHAR Review 20
Jockers, R., Delagrange, P., Dubocovich, M. L., Markus, R. P., Renault, N., Tosini, G., Cecon, E., & Zlotos, D. P. (2016) · British Journal of Pharmacology · doi:10.1111/bph.13536 · Cited by 450
Metadata
- Authors
- Dubocovich, M. L.
- Affiliations
- Northwestern University (US)
- Corresponding author
- Dubocovich, Margarita L.
- Venue
- Sleep Medicine
- Publisher
- Elsevier BV
- Published
- 2007-12
- Volume
- 8
- Pages
- 34-42
- ISSN
- 1389-9457 (ISSN-L)
- 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
- 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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