28
Views
2
CrossRef citations to date
0
Altmetric
Review

Therapeutic potential of melatonin receptor agonists and antagonists

Pages 153-173 | Published online: 24 Feb 2005

Bibliography

  • Dubocovich ML, Cardinali DP, Guardiola-Lemaitre B et al.: Melatonin receptors. In: The IUPHAR Compendium of Receptor Characterization and Classification. Deborah Girdlestone (Ed.) IUPHAR Media, London, UK (1998) :187–193.
  • ••The first publication to describe the IUPHAR nomenclature (mt, MT) and classification (mti,MT2, MT3) of melatonin receptors in mammals.
  • 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.
  • LIU C, WEAVER DR, JINX et al.: Molecular dissection of two distinct actions of melatoninon the suprachiasmatic circadian clock. Neuron (1997) 19:91–102.
  • •This publication describes the first mti knock-out mice. In the SCN of the mti knock-out mice the melatonin-mediated decreases in neuronal firing are impaired. However, the phase advances of neuronal firing rhythms remained unaltered. These studies led to the conclusion that a melatonin receptor other than mti mediates phase-shifts of circadian rhythms in the SCN.
  • REPPERT SM, GODSON C, MAHLE CD, WEAVER DR, SLAUGENHAUPT SA, GUSELLA JF: Molecular characterization of a second melatonin receptor expressed in human retina and brain: the melib melatonin receptor. Proc. Natl. Acad. Sci. USA (1995) 92:8734–8738.
  • DUBOCOVICH ML, MASANA MI, JACOB S, SAURI DM: Melatonin receptor antagonists that differentiate between the human Melia and Melib recombinant subtypes are used to assess the pharmacological profile of the rabbit retina MLI presynaptic heteroreceptor. Naunyn Schmiedebergs Arch. Pharmacol. (1997) 355:365–375.
  • ••The first report describing pharmacological differences between the recombinant human mtiand MT2 melatonin receptors using melatonin receptor antagonists and antagonists. This paper also demonstrates that the presynaptic melatonin heteroreceptor inhibiting dopamine release from rabbit retina is an MT2 receptor.
  • DUBOCOVICH ML, YUN K, AL-GHOUL WM, BENLOUCIF S, MASANA MI: Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms. FASEB J. (1998) 12:1211–1220.
  • •This paper describes for the first time, the presence of MT2 melatonin receptor mRNA in the mammalian SCN using in situ hybridisation. Furthermore, it demonstrates that selective MT2 melatonin receptor antagonists completely blocked the phase advance of circadian activity rhythms induced by melatonin.
  • DOOLEN S, KRAUSE DN, DUBOCOVICH ML, DUCKLES SP: Melatonin mediates two distinct responses in vascular smooth muscle. Eur. J. Pharmacol. (1998) 345:67–69.
  • FOULKES NS, BORJIGIN J, SNYDER SH, SASSONE-CORSI P: Rhythmic transcription: the molecular basis of circadian melatonin synthesis. Trends Neurosci. (1997) 20:487–492.
  • KRAUSE DN, DUBOCOVICH ML: Regulatory sites in the melatonin system of mammals. Trends Neurosci. (1990) 13:464–470.
  • REITER RJ: Pineal melatonin: cell biology of its synthesis and its physiological interactions. Endocr. Rev. (1991) 12:151–180.
  • CASSONE VM: Effects of melatonin on vertebrate circadian systems. Trends Neurosci. (1990) 13:457–464.
  • MORGAN PJ, BARRETT P, HOWELL HE, HELLIWELL R: Melatonin receptors: localization, molecular pharmacology and physiological significance. Neurochem. Int. (1994) 24:101–146.
  • DUBOCOVICH ML: Melatonin receptors: are there multiple subtypes Trends Pharmacol. Sci. (1995) 16:50–56.
  • HAGAN RM, OAKLEY NR: Melatonin comes of age Trends Pharmacol. Sci. (1995) 16:81–83.
  • DUBOCOVICH ML, BENLOUCIF S, MASANA MI: Melatonin receptors in the mammalian suprachiasmatic nucleus. Behav. Brain Res. (1996) 73:141–147.
  • Yu HS, Reiter RJ (Eds.), CRC Press, Boca Raton, Florida, USA (1993) :187–224.
  • WIRZ-JUSTICE A: Biological rhythms in mood disorders. In: Psychopharmacology: The fourth generation of progress. Bloom FE, Kupfer DJ (Eds.) Raven Press, New York, NY, USA (1995)999–1017.
  • DUBOCOVICH ML: Pharmacology and function of melatonin receptors. FASEB J. (1988) 2:2765–2773.
  • SLAUGENHAUPT SA, ROCA AL, LIEBERT CB, ALTHERR MR, GUSELLA JF, REPPERT SM: Mapping of the gene for the Melia melatonin receptor to human chromosome 4 (MTNRiA) and mouse chromosome 8 (Mtnria). Genomics (1995) 27:355–357.
  • EIS ON AS, MULLINS UL: Melatonin binding sites are functionally coupled to phosphoinositide hydrolysis in Syrian hamster RPMI 1846 melanoma cells. Life Sci. (1993) 53:L393–L398.
  • MOLINARI EJ, NORTH PC, DUBOCOVICH ML: 211251]iodo-5-methoxycarbonylamino-N-acetyltryptamine: a selective radioligand for the characterization of melatonin ML2 binding sites. Eur. J. Pharmacol. (1996) 301:159–168.
  • BENITEZ-KING G, ANTON-TAY F: Calmodulin mediates melatonin cytoskeletal effects. Experientia (1993) 49:635–641.
  • MENENDEZ-PELAEZ A, REITER RJ: Distribution of melatonin in mammalian tissues: the relative importance of nuclear versus cytosolic localization. J. Pineal Res. (1993) 15:59–69.
  • ACUNA-CASTROVIEJO D, REITER RJ, MENEDEZ-PELAEZ A, PABLOS MI, BURGOS A: Characterization of high-affinity melatonin binding sites in purified cell nuclei of rat liver. J. Pineal Res. (1994) 16:100–112.
  • BECKER-ANDRE M, WIESENBERG I, SCHAEREN-WIEMERS N, et al.: Pineal gland hormone melatonin binds and activates an orphan of the nuclear receptor superfamily. J. Biol. Chem. (1994) 269:28531–28534.
  • •The first publication describing melatonin as a potential ligand of RZRO, an orphan of the nuclear retinoid receptor superfamily.
  • WIESENBERG I, MISSBACH M, KAHLEN J-P, SCHRADER M, CARLBERG C: Transcriptional activation of the nuclear receptor RZRoc by the pineal gland hormone melatonin and identification of CGP 52608 as a synthetic ligand. Nucl. Acid Res. (1995) 23:327–333.
  • CAJOCHEN C, KRAUCHI K, MORI D, GRAW P, WIRZ-JUSTICE A: Melatonin and S-20098 increase REM sleep and wake-up propensity without modifying NREM sleep homeostasis. Am. J. Physiol. (1997) 272:R1189–R1196.
  • NOWELL PD, MAZUMDAR S, BUYSSE DJ, DEW MA, REYNOLDS CF, KUPFER DJ: Benzodiazepines and zolpidem for chronic insomnia: a meta-analysis of treatment efficacy. JAMA (1997) 278:2170–2177.
  • ARENDT J, ALDHOUS M: Further evaluation of the treatment ofjet-lag with melatonin: A double-blind crossover study. Ann. Rev. Chronopharmacol. (1988) 5:53–55.
  • PETRIE K, DAWSON AG, THOMPSON L, BROOK R: A double-blind trial of melatonin as a treatment for jet lag in international cabin crew. Biol. Psychiat. (1993) 33:526–530.
  • SACK RL, LEWY AJ: Melatonin as a chronobiotic: treatment of circadian desynchrony in night workers and the blind. J. Biol. Rhythms (1997) 12:595–603.
  • CZEISLER CA, JOHNSON MP, DUFFY JF, BROWN EN, RONDA JM, KRONAUER RE: Exposure to bright light and darkness to treat physiologic maladaptation to night work. New Engl. J. Med. (1990) 322:1253–1259.
  • Wehr TA, Goodwin FK (Eds.), Boxwood Press, Pacific Grove, CA, USA (1983) 129–184.
  • DAHLITZ M, ALVAREZ B, VIGNAU J, ENGLISH J, ARENDT J, PARKES JD: Delayed sleep phase syndrome response to melatonin. Lancet (1991) 337:1121–1124.
  • NAGTEGAAL JE, KERKHOF GA, SMITS MG, SWART AC, VAN DER MEER YG: Delayed sleep phase syndrome: A placebo-controlled cross-over study on the effects of melatonin administered five hours before the individual dim light melatonin onset. J. Sleep Res. (1998) 7:135–143.
  • LEWY AJ, BAUER VK, CUTLER NL, et al.: Morning vs. evening light treatment of patients with winter depression. Arch. Gen. Psychiat. (1998) 55:890–896.
  • KOKKORIS CP, WEITZMAN ED, POLLAK CP, SPIELMAN AJ, CZEISLER CA, BRADLOW H: Long-term ambulatory temperature monitoring in a subject with a hypernychthemeral sleep-wake cycle disturbance. Sleep (1978) 1:177–190.
  • KENNAWAY DJ, VAN DORP CF: Free-running rhythms of melatonin, cortisol, electrolytes, and sleep in humans in Antarctica. Am. J. Physiol. (1991) 260:R1137–R1144.
  • SACK RL, HUGHES RJ, EDGAR DM, LEWY AJ: Sleep-promoting effects of melatonin: at what dose, in whom, under what conditions, and by what mechanisms Sleep (1997) 20:908–915.
  • ETZIONI A, LUBOSHITZKY R, TIOSANO D, BEN-HARUSH M, GOLDSHER D, LAVIE P: Melatonin replacement corrects sleep disturbances in a child with pineal tumor. Neurology (1996) 46:261–263.
  • BALTER MB, UHLENHUTH EH: New epidemiologic findings about insomnia and its treatment. J. Clin. Psychiat. (1992) 53:34–39.
  • LINSEN SM, ZITMAN FG, BRETELER MH: Defining benzodiazepine dependence: the confusion persists. Eur. Psychiat. (1995) 10:306–311.
  • WALSH JK, ENGELHARDT CL: Trends in the pharmacologic treatment of insomnia. J. Clin. Psychiat. (1992) 53:10–17.
  • WARE JC: Tricyclic antidepressants in the treatment of insomnia. J. Clin. Psychiat. (1983) 44:25–28.
  • LILIE JK, LAHMEYER H: Psychiatric management of sleep disorders. Psychiatr. Med. (1991)9:245–260.
  • PEARCE PL: Trends in pharmacologic treatment of insomnia. J. Clin. Psychiat. (1994)55:163–164.
  • STAEDT J, STOPPE G, HAJAK C, MULLERSTRUCK A, RUTHER E: Chronic insomnia: what should be done if minor tranquilizers are no longer helpful Fortschr. Neurol. Psychiatr. (1995) 63:368–372.
  • LEIPZIG RM, CUMMING RG, TINETTI ME: Drugs and falls in older people: a systematic review and meta-analysis: I. Psychotropic drugs. J. Am. Geriatr. Soc. (1999) 47:30–39.
  • TUREK FW: Pharmacological probes of the mammalian circadian clock: use of the phase response curve approach. Trends Pharmacol. Sci. (1987) 8:212–217.
  • TUREK FW, VAN REETH O: Altering the mammalian circadian clock with the short-acting benzodiazepine, triazolam. Trends Neurosci. (1988) 11:535–541.
  • DAAN S, LEVVY AJ: Scheduled exposure to daylight: a potential strategy to reduce 'jet lag' following trans-meridian flight. Psychopharmacol. Bull. (1984) 20:566–568.
  • TERMAN M, LEVVY AJ, DIJK DJ, BOULOS Z, EASTMAN CI, CAMPBELL SS: Light treatment for sleep disorders: consensus report. IV. Sleep phase and duration disturbances. J. Biol. Rhythms (1995) 10:135–147.
  • ZHANG Y, KORNHAUSER JM, ZEE PC, MAYO KE, TAKAHASHI JS, TUREK FW: Effects of aging on light-induced phase-shifting of circadian behavioral rhythms, fos expression and CREB phosphorylation in the hamster (SCN). Neuroscience (1996) 70:951–961.
  • SUGAWARA T, SIEVING PA, IUVONE PM, BUSH RA: The melatonin antagonist luzindole protects retinal photoreceptors from light damage in the rat. Invest. Ophthalmol. Vis. Sci. (1998) 39:2458–2465.
  • VAN CAUTER E, VAN ONDERBERGEN A, BOOSSON D: Triazolam accelerates the adaptation of the circadian rhythm of cortisol to an 8-hour delay of the sleep-wake cycle in man. Soc. Neurosci. Abstr. (1987) 12:1040.
  • VAN CAUTER E, POLONSKY KS, SCHEEN AJ: Roles of circadian rhythmicity and sleep in human glucose regulation. Endocr. Rev. (1997) 18:716–738.
  • DONALDSON E, KENNAWAY DJ: Effects of temazepam on sleep, performance, and rhythmic 6-sulphatoxymelatonin and cortisol excretion after transmeridian travel. Aviat. Space Environ. Med. (1991) 62:654–660.
  • LERNER AB, CASE JD, HEIZELMAN RV: Structure of melatonin. J. Am. Chem. Soc. (1959) 81:6084–6085.
  • Moller M, Pevet P (Eds.), John Libbey & Co. Ltd, London, UK (1994) :333–348.
  • BERESFORD IJ, BROWNING C, STARKEY SJ, et al.: GR196429: a non-indolic agonist at high-affinity melatonin receptors. J. Pharmacol. Exp. Ther. (1998) 285:1239–1245.
  • •A detailed pharmacological profile of the non-indolic melatonin receptor agonist, GR196429.
  • ZHDANOVA IV, WURTMAN RJ, LYNCH HJ, et al.: Sleep-inducing effects of low doses of melatonin ingested in the evening. Clin. Pharmacol. Ther. (1995) 57:552–558.
  • KRAUSE DN, BARRIOS VE, DUCKLES SP: Melatonin receptors mediate potentiation of contractile responses to adrenergic nerve stimulation in rat caudal artery. Eur. J. Pharmacol. (1995) 276:207–213.
  • TING K, DUNN W, DAVIES D, et al.: Studies on the vasoconstrictor action of melatonin and putative melatonin receptor ligands in the tail artery of juvenile Wistar rats. Br. J. Pharmacol. (1997) 122:1299–1306.
  • VOLLRATH L, SEMM P, GAMMEL G: Sleep induction by intranasal application of melatonin. Adv. Biosci. (1981) 29:327–329.
  • ANTON-TAY F, DIAZ JL, FERNANDEZ-GUARDIOLA A: On the effect of melatonin upon human brain. Its possible therapeutic implications. Life Sci. (1971) 10:841–850.
  • DOLLINS AB, ZHDONOVA IV, WURTMAN RJ, LYNCH HJ, DENG MH: Effect of inducing nocturnal serum melatonin concentrations in daytime on sleep, mood, body temperature, and performance. Proc. Natl. Acad. Sci. USA (1994) 91:1824–1828.
  • TZISCHINSKY O, LAVIE P: Melatonin possesses time-dependent hypnotic effects. Sleep (1994) 17:638–645.
  • ZHDANOVA IV, LYNCH HJ, WURTMAN RJ: Melatonin: a sleep-promoting hormone. Sleep (1997) 20:899–907.
  • •A thorough and current review describing the sleep promoting effects of physiological doses of melatonin, and discussing this finding in relation to the ability of melatonin to phase-shift the biological clock.
  • JAMES SP, MENDELSON WB, SACK DA, ROSENTHAL NE, WEHR TA: The effect of melatonin on normal sleep. Neuropsychopharmacology (1987) 1:41–44.
  • NAVE R, HERER P, HAIMOV I, SHLITNER A, LA VIE P: Hypnotic and hypothermic effects of melatonin on daytime sleep in humans: lack of antagonism by flumazenil. Neurosci. Lett. (1996) 214:123–126.
  • •This paper describes the hypnotic and hypothermic effects of melatonin and demonstrate that the benzodiazepine antagonist flumazemil did not impair the effect of this hormone.
  • ZHDANOVA IV, WURTMAN RJ, MORABITO C, PIOTROVSKA VR, LYNCH HJ: Effects of low oral doses of melatonin given 2-24 h before habitual bedtime, on sleep in normal young humans. Sleep (1996) 19:423–431.
  • LEVVY AJ, AHMED S, LATHAM-JACKSON JM, SACK RL: Melatonin shifts human circadian rhythms according to a phase-response curve. Chronobiol. Int. (1992) 9:380–392.
  • SACK RL, LEVVY AJ, BLOOD ML, STEVENSON J, KEITH LD: Melatonin administration to blind people: phase advances and entrainment. J. Biol. Rhythms (1991) 6:249–261.
  • SACK RL, LEWY AJ, HUGHES RJ, MCARTHUR AF, BLOOD ML: Melatonin as a chronobiotic drug. Drug News Perspect. (1996) 9:325–332.
  • REPPERT SM, WEAVER DR, RIVKEES SA, STOPA EG: Putative melatonin receptors in a human biological clock. Science (1988) 242:78–81.
  • BRZEZINSKI A: Melatonin in humans. New Engl. J. Med. (1997) 336:186–95.
  • ••A thorough review describing the potential physiological functions and mechanisms ofmelatonin action.
  • GUARDIOLA-LEMAITRE B: Toxicology of melatonin. J. Biol. Rhythms (1997) 12:697–706.
  • TUREK FW: Melatonin hype hard to swallow. Nature (1996) 379:295–296.
  • GARFINKEL D, LAUDON M, NOF D, ZISAPEL N: Improvement of sleep quality in elderly people by controlled-release melatonin. Lancet (1995) 346:541–544.
  • ATSMON J, OAKNIN S, LAUDON M, et al.: Reciprocal effects of chronic diazepam and melatonin on brain melatonin and benzodiazepine binding sites. J. Pineal Res. (1996) 20:65–71.
  • YING SW, RUSAK B, DELAGRANGE P, MOCAER E, RENARD P, GUARDIOLA-LEMAITRE B: Melatonin analogues as agonists and antagonists in the circadian system and other brain areas. Eur. J. Pharmacol. (1996) 296:33–42.
  • REDMAN JR, GUARDIOLA-LEMAITRE B, BROWN M, DELAGRANGE P, ARMSTRONG SM: Dose dependent effects of S-20098, a melatonin agonist, on direction of re-entrainment of rat circadian activity rhythms. Psychopharmacology (1995) 118:385–390.
  • ARMSTRONG SM, MCNULTY OM, GUARDIOLA-LEMAITRE B, REDMAN JR: Successful use of S20098 and melatonin in an animal model of delayed sleep-phase syndrome (DSPS). Pharmacol. Biochem. Behav. (1993) 46:45–49.
  • •Describes an animal model for DSPS, which can be used to screen melatonin receptor agonists that phase-shift the clock.
  • REDMAN JR, FRANCIS AJ: Entrainment of rat circadian rhythms by the melatonin agonist S-20098 requires intact suprachiasmatic nuclei but not the pineal. J. Biol. Rhythms (1998) 13:39–51.
  • BENLOUCIF S, DUBOCOVICH ML: Melatonin and light induce phase-shifts of circadian rhythms in the C3H/HeN mouse. J. Biol. Rhythms (1996) 11:113–125.
  • GRASSI-ZUCCONI G, SEMPREVIVO M, MOCAER E, KRISTENSSON K, BENTIVOGLIO M: Melatonin and its new agonist S-20098 restore synchronized sleep fragmented by experimental trypanosome infection in the rat. Brain Res. Bull. (1996) 39:63–68.
  • TOBLER I, JAGGI K, BORBELY AA: Effects of melatonin and the melatonin receptor agonist S-20098 on the vigilance states, EEG spectra, and cortical temperature in the rat. J. Pineal Res. (1994) 16:26–32
  • KRAUCHI K, CAJOCHEN C, MORI D, GRAW P, WIRZ-JUSTICE A: Early evening melatonin and S-20098 advance circadian phase and nocturnal regulation of core body temperature. Am. J. Physiol. (1997) 41:R1178–R1188.
  • •First description on the effects of S- 1920098 on circadian phase and core body temperature in human volunteers.
  • GOLDBERG MJ, BERGSTROM RF, SMITH BP: LY156735, a melatonin agonist: Phase 1 pharmacokinetic and pharmacodynamic studies. ACNP Scientific Abst. (1998) :144.
  • LEVINE LR, SMITH BP, SCHARF M, ROTH T: LY156735, a melatonin analog, reduces sleep-onset latency in patients with moderate sleep-onset insomnia. ACNP Scientific Abst. (1998):143.
  • NICKELSON T, SAMEL A, DRUMMER C, WENZEL J, VEJVODA M, POTTER WZ: LY156735, a melatonin agonist, enhances readaptation of desynchronized circadian rhythms following a simulated 9-hour time shift. ACNP Scientific Abst. (1998) :225.
  • BERESFORD IJM, STARKEY SJ, OAKLEY NR, STRATTON SC HAGAN RM: GR 196429, a non indolic agonist at high affinity melatonin receptors which mediate the actions of melatonin on the rat circadian clock. Brit. J. Pharmacol. (1997) 120:360P.
  • DUBOCOVICH ML, MOGILNICKA E, ARESO P: Antidepressant-like activity of the melatonin receptor antagonist luzindole (N-0774) in the mouse behavioral despair test. Eur. J. Pharmacol. (1990) 182:313–325.
  • •This paper describes the potential antidepressant effects of luzindole in the mice swimming test in mice known to synthesise melatonin in the pineal gland.
  • LE GOUIC S, DELAGRANGE P, ATGIE C, et al.: Effects of both a melatonin agonist and antagonist on seasonal changes in body mass and energy intake in the garden dormouse. Int. J. Obes. Relat. Metab. Disord. (1996) 20:661–667.
  • •First report on the actions of synthetic melatonin receptor agonists and antagonists on seasonal changes on body mass and energy intake.
  • DUBOCOVICH ML: Melatonin receptor agonists and antagonists. Proceedings of the 9th Noordwijherhout-Camerino Symposium on Trends in Drug Research. Leevwenhorst, The Netherlands (1993) 15:285–291.
  • MAHLE CD, GOGGINS GD, AGARWAL P, RYAN E, WATSON AJ: Melatonin modulates vascular smooth muscle tone. J. Biol. Rhythms (1997) 12:690–696.
  • •A thorough review of the cardiovascular effects of melatonin in mammals including human arterial vessels.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.