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Review

Melatonin receptors as therapeutic targets in the suprachiasmatic nucleus

Pages 1209-1218 | Received 06 Feb 2016, Accepted 18 Mar 2016, Published online: 26 Apr 2016

References

  • Dibner C, Schibler U, Albrecht U. The mammalian circadian timing system: organization and coordination of central and peripheral clocks. Ann Rev Physiol. 2010;72:517–549.
  • Pevet P, Challet E. Melatonin: both master clock output and internal time-giver in the circadian clocks network. J Physiol Paris. 2011;105:170–182.
  • Mohawk JA, Green CB, Takahashi JS. Central and peripheral circadian clocks in mammals. Annu Rev Neurosci. 2012;35:445–462.
  • Hastings MH, Herzog ED. Clock genes, oscillators, and cellular networks in the suprachiasmatic nuclei. J Biol Rhythms. 2004;19:400–413.
  • Piggins HD, Loudon A. Circadian biology: clocks within clocks. Curr Biol. 2005;15:R455–R457.
  • Meijer JH, Michel S, Vanderleest HT, et al. Daily and seasonal adaptation of the circadian clock requires plasticity of the SCN neuronal network. Eur J Neurosci. 2010;32:2143–2151.
  • Challet E, Pevet P. Interactions between photic and nophotic stimuli to synchronize the mammalian circadian clock. Front Biosci. 2003;8:246–257.
  • Buhr ED, Yoo S-H, Takahashi JS. Temperature as a universal resetting cue for mammalian circadian oscillators. Science. 2010;330:379–385.
  • Buijs R, Salgado R, Sabath E, et al. Peripheral circadian oscillators: time and food. Prog Mol Biol Transl Sci. 2013;119:83–03.
  • Challet E. Circadian clocks, food intake, and metabolism. Prog Mol Biol Transl Sci. 2013;119:105–135.
  • Buhr ED, Takahashi JS. Molecular components of the mammalian circadian clock. Handb Exp Pharmacol. 2013;217:3–27.
  • Gachon F, Nagoshi E, Brown SA, et al. The mammalian circadian timing system: from gene expression to physiology. Chromosoma. 2004;113:103–112.
  • Segall LA, Amir S. Glucocorticoid regulation of clock gene expression in the mammalian limbic forebrain. J Mol Neurosci. 2010;42:168–175.
  • Mendoza J, Pevet P, Felder-Schmittbuhl M-P, et al. The cerebellum harbors a circadian oscillator involved in food anticipation. J Neurosci. 2010;30:1894–1904.
  • Schernhammer ES, Kroenke CH, Laden F, et al. Night work and risk of breast cancer. Epidemiology. 2006;17:108–111.
  • Lewy AJ, Lefler BJ, Emens JS, et al. The circadian basis of winter depression. Proc Natl Acad Sci U S A. 2006;103:7414–7419.
  • Rüger M, Scheer FA. Effects of circadian disruption on the cardiometabolic system. Rev Endocr Metab Disord. 2009;10:245–260.
  • Bechtold DA, Gibbs JE, Loudon AS. Circadian dysfunction in disease. Trends Pharmacol Sci. 2010;31:191–198.
  • Sahar S, Sassone-Corsi P. Regulation of metabolism: the circadian clock dictates the time. Trends Endocrinol Metab. 2012;23:1–8.
  • Benedetti F. Antidepressant chronotherapeutics for bipolar depression. Dialogues Clin Neurosci. 2012;1:22–36.
  • Schroeder AM, Colwell CS. How to fix a broken clock. Trends Pharmacol Sci. 2013;34:605–619.
  • Marcheva B, Ramsey KM, Peek CB, et al. Circadian clocks and metabolism. Handb Exp Pharmacol. 2013;217:127–155.
  • Delezie J, Dumont S, Dardente H, et al. The nuclear receptor REV-ERBα is required for the daily balance of carbohydrate and lipid metabolism. FASEB J. 2012;26:3321–3335.
  • Zelinski EL, Deibel SH, McDonald RJ. The trouble with circadian clock dysfunction: multiple deleterious effects on the brain and body. Neurosci Biobehav Rev. 2014;40C:80–101.
  • Buijs RM, Kalsbeek A. Hypothalamic integration of central and peripheral clocks. Nat Rev Neurosci. 2001;2:521–526.
  • Barclay JL, Tsang AH, Oster H. Interaction of central and peripheral clocks in physiological regulation. Prog Brain Res. 2012;199:163–181.
  • Schroeder AM, Truong D, Loh DH, et al. Voluntary scheduled exercise alters diurnal rhythms of behaviour, physiology and gene expression in wild-type and vasoactive intestinal peptide-deficient mice. J Physiol. 2012;590:6213–6226.
  • Hughes AT, Piggins HD. Feedback actions of locomotor activity to the circadian clock. Prog Brain Res. 2012;199:305–336.
  • Leise TL, Harrington ME, Molyneux PC, et al. Voluntary exercise can strengthen the circadian system in aged mice. Age. 2013;35:2137–2152.
  • Barger LK, Wright KP Jr, Hughes RJ, et al. Daily exercise facilitates phase delays of circadian melatonin rhythm in very dim light. Am J Physiol Regul Integr Comp Physiol. 2004;286:R1077–R1084.
  • Buxton OM, Lee CW, L’Hermite-Baleriaux M, et al. Exercise elicits phase shifts and acute alterations of melatonin that vary with circadian phase. Am J Physiol Regul Integr Comp Physiol. 2003;284:R714–R724.
  • Van Someren EJ, Lijzenga C, Mirmiran M, et al. Long-term fitness training improves the circadian rest-activity rhythm in healthy elderly males. J Biol Rhythms. 1997;12:146–156.
  • Terman M, Terman JS. Light therapy for seasonal and non seasonal depression: efficacy,protocol safety and side effects. CNS Spectr. 2005;10:647–663.
  • Wirz-Justice A, Terman M, Oren DA, et al. Brightening depression. Science. 2004;303:467–469.
  • Riemersma-van der Lek RF, Swaab DF, Twisk J, et al. Effect of bright light and melatonin on cognitive and noncognitive function in elderly residents of group care facilities: a randomized controlled trial. JAMA. 2008;299:2642–2655.
  • Duffy JF, Czeisler CA. Effect of light on human circadian physiology. Sleep Med Clin. 2009;4:165–177.
  • Lieverse R, Van Someren EJ, Nielen MM, et al. Bright light treatment in elderly patients with nonseasonal major depressive disorder: a randomized placebo-controlled trial. Arch Gen Psychiatry. 2011;68:61–70.
  • Royer M, Ballentine NH, Eslinger PJ, et al. Light therapy for seniors in long term care. J Am Med Dir Assoc. 2012;13:100–102.
  • Chen Z, Yoo S-H, Takahashi JS. Small molecule modifiers of circadian clocks. Cell Mol Life Sci. 2013;70:2985–2998.
  • Cho H, Zhao X, Hatori M, et al. Regulation of circadian behaviour and metabolism by REV-ERB-α and REV-ERB-β. Nature. 2012;485:123–127.
  • Raghuram S, Stayrook KR, Huang P, et al. Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-erbbeta. Nat. Struct Mol Biol. 2007;14:1207–1213.
  • Solt LA, Wang Y, Banerjee S, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012;485:62–68.
  • Lerner AB, Case JD, Takahashi Y. Isolation of melatonin and 5- methoxyindole-3-acetic acid from bovine pineal glands. J Biol Chem. 1960;235:1992–1997.
  • Pevet P. The melatonin. Dialogues Clin Neurosci. 2002;4:57–72.
  • Perreau-Lenz S, Kalsbeek A, van Der Vliet V, et al. In vivo evidence for a controlled offset of melatonin synthesis at dawn by the suprachiasmatic nucleus in the rat. Neuroscience. 2005;130:797–803.
  • Arendt J. Melatonin: characteristics, concerns, and prospects. J Biol Rhythms. 2005;20:291–303.
  • Simonneaux V, Ancel C, Poirel VJ, et al. Kisspeptins and RFRP-3 act in concert to synchronize rodent reproduction with seasons. Front Neurosci. 2013;7:22. doi:10.3389/fnins.2013.00022.
  • Dardente H. Melatonin-dependent timing of seasonal reproduction by the pars tuberalis: pivotal roles for long daylengths and thyroid hormones. J Neuroendocrinol. 2012;24:249–266.
  • Reiter RJ, Tan DX, Fuentes-Broto L. Melatonin: a multitasking molecule. Prog Brain Res. 2010;181:127–251.
  • Benítez-King G. Melatonin as a cytoskeletal modulator: implications for cell physiology and disease. J Pineal Res. 2006;40:1–9.
  • Reiter RJ, Tan D-X, Rosales-Corral S, et al. The universal nature, unequal distribution and antioxidant functions of melatonin and its derivatives. Mini Rev Med Chem. 2013;13:373–384.
  • Nosjean O, Ferro M, Coge F, et al. Identification of the melatonin-binding site MT3 as the quinone reductase 2. J Biol Chem. 2000;275:31311–31317.
  • Boutin JA. Quinone reductase 2 as a promising target of melatonin therapeutic actions. Expert Opin Ther Targets. 2015;20:1–15.
  • Slominski RM, Reiter RJ, Schlabritz-Loutsevitch N, et al. Melatonin membrane receptors in peripheral tissues: distribution and functions. Mol Cell Endocrinol. 2012;351:152–166.
  • Masson-Pevet M, George D, Kalsbeek A, et al. An attempt to correlate brain areas containing melatonin binding sites with rhythmic functions: a study in five hibernator species. Cell Tissue Res. 1994;278:97–106.
  • Reppert SM, Weaver DR, Ebisawa T. Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses. Neuron. 1994;13:1177–1185.
  • Dubocovich ML, Markowska M. Functional MT1 and MT2 melatonin receptors in mammals. Endocrine. 2005;27:101–110.
  • Reppert SM. Melatonin receptors: molecular biology of a new family of G protein-coupled receptors. J Biol. Rhythms. 1997;12:528–531.
  • Dubocovich ML, Delagrange P, Krause DN, et al. International union of basic and clinical pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors. Pharmacol Rev. 2010;62:343–380.
  • Pevet P. The internal time-giver role of melatonin. A key for our health. Rev Neurol (Paris). 2014;170:646–652.
  • Liu J, Clough SJ, Hutchinson AJ, et al. MT1 and MT2 melatonin receptors: a therapeutic perspective. Annu Rev Pharmacol Toxicol. 2016;56:361–383.
  • Kamal M, Gbahou F, Guillaume J-L, et al. Convergence of melatonin and serotonin (5-HT) signaling at MT2/5-HT2C receptor heteromers. J Biol Chem. 2015;290:11537–11546.
  • Zlotos DP, Jockers R, Cecon E, et al. MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014;57:3161–3185.
  • Ferré S, Casadó V, Devi LA, et al. G protein-coupled receptor oligomerization revisited: functional and pharmacological perspectives. Pharmacol Rev. 2014;66:413–434.
  • Lacoste B, Angeloni D, Dominguez-Lopez S, et al. Anatomical and cellular localization of melatonin MT1 and MT2 receptors in the adult rat brain. J Pineal Res. 2015;58:397–417.
  • Hablitz LM, Molzof HE, Abrahamsson KE, et al. GIRK channels mediate the nonphotic effects of exogenous melatonin. J Neurosci. 2015;35:14957–14965.
  • Von Gall C, Garabette ML, Kell CA, et al. Rhythmic gene expression in pituitary depends on heterologous sensitization by the neurohormone melatonin. Nat Neurosci. 2002;5:234–238.
  • Dardente H, Menet JS, Poirel VJ, et al. Melatonin induces Cry1 expression in the pars tuberalis of the rat. Brain Res Mol Brain Res. 2003;114:101–116.
  • Torres-Farfan C, Mendez N, Abarzua-Catalan L, et al. A circadian clockentrained by melatonin is ticking in the rat fetal adrenal. Endocrinology. 2011;152:1891–1900.
  • Pevet P, Bothorel B, Slotten H, et al. The chronobiotic properties of melatonin. Cell Tissue Res. 2002;309:183–191.
  • Arendt J, Skene DJ. Melatonin as a chronobiotic. Sleep Med Rev. 2005;9:25–39.
  • Gillette MU, McArthur AJ. Circadian actions of melatonin at the suprachiasmatic nucleus. Behav Brain Res. 1995;73:135–139.
  • Redman JR, Armstrong S, Ng KT. Free-running activity rhythms in the rat: entrainment by melatonin. Science. 1983;219:1089–1091.
  • Pitrosky B, Kirsch R, Malan A, et al. Organization of rat circadian rhythms during daily infusion of melatonin or S20098, a melatonin agonist. Am J Physiol. 1999;277:R8126–R828.
  • Slotten HA, Pitrosky B, Pevet P. Entrainment of rat circadian rhythms by daily administration of melatonin: influence of the role of administration. J Biol Rhythms. 1999;14:347–353.
  • Lemoine P, Zisapel N. Prolonged-release formulation of melatonin (Circadin) for the treatment of insomnia. Expert Opin Pharmacother. 2012;13:895–05.
  • Emens JS, Burgess HJ. Effect of light and melatonin and other melatonin receptor agonists on human circadian physiology. Sleep Med Clin. 2015;10:435–453.
  • Skene DJ, Arendt J. Circadian rhythm sleep disorders in the blind and their treatment with melatonin. Sleep Med. 2007;8:651–655.
  • Bothorel B, Barassin S, Saboureau M, et al. In the rat, exogenous melatonin increases the amplitude of pineal melatonin secretion by a direct action on the circadian clock. Eur J Neurosci. 2002;16:1090–1098.
  • Zaidan R, Geoffriau M, Brun J, et al. Melatonin is able to influence its secretion in humans: description of a phase-response curve. Neuroendocrinology. 1994;60:105–112.
  • Castanho A, Bothorel B, Seguin L, et al. Like melatonin, agomelatine (S20098) increases the amplitude of oscillations of two clock outputs: melatonin and temperature rhythms. Chronobiol Int. 2014;31:371–381.
  • Jockers R, Maurice P, Boutin JA, et al. Melatonin receptors, heterodimerization, signal transduction and binding sites: what’s new? Br J Pharmacol. 2008;154:1182–1195.
  • Liu C, Weaver DR, Jin X, et al. Molecular dissection of two distinct actions of melatonin on the suprachiasmatic circadian clock. Neuron. 1997;19:91–102.
  • Dubocovich ML, Hudson RL, Sumaya IC, et al. Effect of MT1 melatonin receptor deletion on melatonin-mediated phase shift of circadian rhythms in the C57BL/6 mouse. J Pineal Res. 2005;39:113–120.
  • Dubocovich ML. Melatonin receptors: role on sleep and circadian rhythm regulation. Sleep Med. 2007;8 Suppl 3:34–42.
  • Reppert SM, Weaver DR, Rivkees SA, et al. Putative melatonin receptors in a human biological clock. Science. 1988;242:78–81.
  • Siuciak JA, Fang JM. Dubocovich ML autoradiographic localization of 2-[125I]iodomelatonin binding sites in the brains of C3H/HeN and C57BL/6J strains of mice. Eur J Pharmacol. 1990;180:387–390.
  • Hunt AE, Al-Ghoul WM, Gillette MU, et al. Activation of MT(2) melatonin receptors in rat suprachiasmatic nucleus phase advances the circadian clock. Am J Physiol Cell Physiol. 2001;280:C110–C118.
  • Poirel V-J, Masson-Pevet M, Pevet P, et al. MT1 melatonin receptor mRNA expression exhibits a circadian variation in the rat suprachiasmatic nuclei. Brain Res. 2002;946:64–71.
  • Schuster C, Gauer F, Malan A, et al. The circadian clock, light/dark cycle and melatonin are differentially involved in the expression of daily and photoperiodic variations in mt(1) melatonin receptors in the Siberian and Syrian hamsters. Neuroendocrinology. 2001;74:55–68.
  • Weaver DR, Reppert SM. The Mel1a melatonin receptor gene is expressed in human suprachiasmatic nuclei. Neuroreport. 1996;8:109–112.
  • Masana MI, Benloucif S, Dubocovich ML. Circadian rhythm of mt1 melatonin receptor expression in the suprachiasmatic nucleus of the C3H/HeN mouse. J Pineal Res. 2000;28:185–192.
  • Poirel V-J, Cailotto C, Streicher D, et al. MT1 melatonin receptor mRNA tissular localization by PCR amplification. Neuro Endocrinol Lett. 2003;24:33–38.
  • Wu Y-H, Ursinus J, Zhou J-N, et al. Alterations of melatonin receptors MT1 and MT2 in the hypothalamic suprachiasmatic nucleus during depression. J Affect Disord. 2013;148:357–367.
  • Wu Y-H, Zhou J-N, Balesar R, et al. Distribution of MT1 melatonin receptor immunoreactivity in the human hypothalamus and pituitary gland: colocalization of MT1 with vasopressin, oxytocin, and corticotropin-releasing hormone. J Comp Neurol. 2006;499:897–10.
  • Cassone VM, Chesworth MJ, Armstrong SM. Dose-dependent entrainment of rat circadian rhythms by daily injection of melatonin. J Biol Rhythms. 1986;1:219–229.
  • Dugovic C, Leysen JE, Wauquier A. Melatonin modulates the sensitivity of 5-hydroxytryptamine-2 receptor-mediated sleep-wakefulness regulation in the rat. Neurosci Lett. 1989;104:320–325.
  • Eison AS, Freeman RP, Guss VB, et al. Melatonin agonists modulate 5-HT2A receptor-mediated neurotransmission: behavioral and biochemical studies in the rat. J Pharmacol Exp Ther. 1995;273:304–308.
  • Maywood ES, Mrosovsky N, Field MD, et al. Rapid down-regulation of mammalian period genes during behavioral resetting of the circadian clock. Proc Natl Acad Sci U S A. 1999;96:15211–15216.
  • Caldelas I, Feillet CA, Dardente H, et al. Timed hypocaloric feeding and melatonin synchronize the suprachiasmatic clockwork in rats, but with opposite timing of behavioral output. Eur J Neurosci. 2005;22:921–929.
  • Poirel VJ, Boggio V, Dardente H, et al. Contrary to other non-photic cues, acute melatonin injection does not induce immediate changes of clock gene mRNA expression in the rat suprachiasmatic nuclei. Neuroscience. 2003;120:745–755.
  • Agez L, Laurent V, Pevet P, et al. Melatonin affects nuclear orphan receptors mRNA in the rat suprachiasmatic nuclei. Neuroscience. 2007;144:522–530.
  • Carocci A, Catalano A, Sinicropi MS. Melatonergic drugs in development. Clin Pharmacol. 2014;6:127–137.
  • Mor M, Rivara S, Pala D, et al. Recent advances in the development of melatonin MT1 and MT2 receptor agonists. Expert Opin Ther Pat. 2010;20:1059–1073.
  • Rivara S, Pala D, Bedini A, et al. Therpeutic uses of melatonin and melatonin derivatives: a patent review (2012–2014). Expert Opin Ther Pat. 2015;25:425–441.
  • Spadoni G, Bedini A, Lucarini S, et al. Highly potent and selective MT2 melatonin receptor full agonists from conformational analysis of 1-benzyl-2-acylaminomethyl-tetrahydroquinolines. J Med Chem. 2015;58:7512–7525.
  • Morgan PJ, Barrett P, Howell HE, et al. Melatonin receptors: localization, molecular pharmacology and physiological significance. Neurochem Int. 1994;24:101–146.
  • Maywood ES, Bittman EL, Ebling FJ, et al. Regional distribution of iodomelatonin binding sites within the suprachiasmatic nucleus of the Syrian hamster and the Siberian hamster. J Neuroendocrinol. 1995;7:215–223.
  • Song CK, Bartness TJ, Petersen SL, et al. Co-expression of melatonin (MEL1a) receptor and arginine vasopressin mRNAs in the Siberian hamster suprachiasmatic nucleus. J Neuroendocrinol. 2000;12:627–634.
  • Savaskan E, Wirz-Justice A, Olivieri G, et al. Distribution of melatonin MT1 receptor immunoreactivity in human retina. J Histochem Cytochem. 2002;50:519–526.
  • Schepelmann M, Molcan L, Uhrova H, et al. The presence and localization of melatonin receptors in the rat aorta. Cell Mol Neurobiol. 2011;31:1257–1265.
  • Sheng W-L, Chen W-Y, Yang X-L, et al. Co-expression of two subtypes of melatonin receptor on rat M1-type intrinsically photosensitive retinal ganglion cells. PLoS One. 2015;10:e0117967.
  • Söderquist F, Hellström PM, Cunningham JL, et al. Human gastroenteropancreatic expression of melatonin and its receptors MT1 and MT2. PLoS One. 2015;10:e0120195.
  • Klosen P, Bienvenu C, Demarteau O, et al. The mt1 melatonin receptor and RORbeta receptor are co-localized in specific TSH-immunoreactive cells in the pars tuberalis of the rat pituitary. J Histochem Cytochem. 2002;50:1647–1657.
  • Vishwas DK, Haldar C. Photoperiodic induced melatonin regulates immunity and expression pattern of melatonin receptor MT1 in spleen and bone marrow mononuclear cells of male golden hamster. J Photochem Photobiol B. 2013;128:107–114.
  • Waly N, Hallworth R. Circadian pattern of melatonin MT1 and MT2 receptor localization in the rat suprachiasmatic nucleus. J Circadian Rhythms. 2015;13:1–7.
  • Adamah-Biassi EB, Zhang Y, Jung H, et al. Distribution of MT1 melatonin receptor promoter-driven RFP expression in the brains of BAC C3H/HeN transgenic mice. J Histochem Cytochem. 2014;62:70–84.

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