Melatonin receptor 1A

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Melatonin receptor 1A
Symbols MTNR1A ; MEL-1A-R; MT1
External IDs OMIM600665 MGI102967 HomoloGene21207 IUPHAR: 287 ChEMBL: 1945 GeneCards: MTNR1A Gene
RNA expression pattern
PBB GE MTNR1A 221369 at tn.png
More reference expression data
Species Human Mouse
Entrez 4543 17773
Ensembl ENSG00000168412 ENSMUSG00000054764
UniProt P48039 Q61184
RefSeq (mRNA) NM_005958 NM_008639
RefSeq (protein) NP_005949 NP_032665
Location (UCSC) Chr 4:
186.53 – 186.56 Mb
Chr 8:
45.07 – 45.09 Mb
PubMed search [1] [2]

Melatonin receptor type 1A is a protein that in humans is encoded by the MTNR1A gene.[1][2]


This gene encodes the MT1 protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This receptor is a G protein-coupled, 7-transmembrane receptor that is responsible for melatonin effects on mammalian circadian rhythm and reproductive alterations affected by day length. The receptor is an integral membrane protein that is readily detectable and localized to two specific regions of the brain. The hypothalamic suprachiasmatic nucleus appears to be involved in circadian rhythm while the hypophysial pars tuberalis may be responsible for the reproductive effects of melatonin.[2]


  1. Melatonin – full agonist
  2. Afobazole – agonist
  3. Agomelatine – agonist

See also[edit]


  1. ^ Slaugenhaupt SA, Roca AL, Liebert CB, Altherr MR, Gusella JF, Reppert SM (May 1995). "Mapping of the gene for the Mel1a-melatonin receptor to human chromosome 4 (MTNR1A) and mouse chromosome 8 (Mtnr1a)". Genomics 27 (2): 355–7. doi:10.1006/geno.1995.1056. PMID 7558006. 
  2. ^ a b "Entrez Gene: MTNR1A melatonin receptor 1A". 

Further reading[edit]

  • Brzezinski A (Jan 1997). "Melatonin in humans". The New England Journal of Medicine 336 (3): 186–95. doi:10.1056/NEJM199701163360306. PMID 8988899. 
  • Khan AU, Olson DL (Aug 1975). "Physical therapy and exercise-induced bronchospasm". Physical Therapy 55 (8): 878–81. PMID 1144527. 
  • Reppert SM, Weaver DR, Ebisawa T (Nov 1994). "Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses". Neuron 13 (5): 1177–85. doi:10.1016/0896-6273(94)90055-8. PMID 7946354. 
  • Witt-Enderby PA, Dubocovich ML (Jul 1996). "Characterization and regulation of the human ML1A melatonin receptor stably expressed in Chinese hamster ovary cells". Molecular Pharmacology 50 (1): 166–74. PMID 8700109. 
  • Witt-Enderby PA, Masana MI, Dubocovich ML (Jul 1998). "Physiological exposure to melatonin supersensitizes the cyclic adenosine 3',5'-monophosphate-dependent signal transduction cascade in Chinese hamster ovary cells expressing the human mt1 melatonin receptor". Endocrinology 139 (7): 3064–71. doi:10.1210/en.139.7.3064. PMID 9645677. 
  • Ebisawa T, Kajimura N, Uchiyama M, Katoh M, Sekimoto M, Watanabe T, Ozeki Y, Ikeda M, Jodoi T, Sugishita M, Iwase T, Kamei Y, Kim K, Shibui K, Kudo Y, Yamada N, Toyoshima R, Okawa M, Takahashi K, Yamauchi T (Sep 1999). "Alleic variants of human melatonin 1a receptor: function and prevalence in subjects with circadian rhythm sleep disorders". Biochemical and Biophysical Research Communications 262 (3): 832–7. doi:10.1006/bbrc.1999.1308. PMID 10471411. 
  • Brydon L, Roka F, Petit L, de Coppet P, Tissot M, Barrett P, Morgan PJ, Nanoff C, Strosberg AD, Jockers R (Dec 1999). "Dual signaling of human Mel1a melatonin receptors via G(i2), G(i3), and G(q/11) proteins". Molecular Endocrinology 13 (12): 2025–38. doi:10.1210/me.13.12.2025. PMID 10598579. 
  • Niles LP, Wang J, Shen L, Lobb DK, Younglai EV (Oct 1999). "Melatonin receptor mRNA expression in human granulosa cells". Molecular and Cellular Endocrinology 156 (1-2): 107–10. doi:10.1016/S0303-7207(99)00135-5. PMID 10612428. 
  • Song CK, Bartness TJ (Aug 2001). "CNS sympathetic outflow neurons to white fat that express MEL receptors may mediate seasonal adiposity". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology 281 (2): R666–72. PMID 11448873. 
  • Roy D, Angelini NL, Fujieda H, Brown GM, Belsham DD (Nov 2001). "Cyclical regulation of GnRH gene expression in GT1-7 GnRH-secreting neurons by melatonin". Endocrinology 142 (11): 4711–20. doi:10.1210/en.142.11.4711. PMID 11606436. 
  • Savaskan E, Olivieri G, Meier F, Brydon L, Jockers R, Ravid R, Wirz-Justice A, Müller-Spahn F (Jan 2002). "Increased melatonin 1a-receptor immunoreactivity in the hippocampus of Alzheimer's disease patients". Journal of Pineal Research 32 (1): 59–62. doi:10.1034/j.1600-079x.2002.00841.x. PMID 11841602. 
  • Savaskan E, Wirz-Justice A, Olivieri G, Pache M, Kräuchi K, Brydon L, Jockers R, Müller-Spahn F, Meyer P (Apr 2002). "Distribution of melatonin MT1 receptor immunoreactivity in human retina". The Journal of Histochemistry and Cytochemistry 50 (4): 519–26. doi:10.1177/002215540205000408. PMID 11897804. 
  • Ayoub MA, Couturier C, Lucas-Meunier E, Angers S, Fossier P, Bouvier M, Jockers R (Jun 2002). "Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer". The Journal of Biological Chemistry 277 (24): 21522–8. doi:10.1074/jbc.M200729200. PMID 11940583. 
  • Yuan L, Collins AR, Dai J, Dubocovich ML, Hill SM (Jun 2002). "MT(1) melatonin receptor overexpression enhances the growth suppressive effect of melatonin in human breast cancer cells". Molecular and Cellular Endocrinology 192 (1-2): 147–56. doi:10.1016/S0303-7207(02)00029-1. PMID 12088876. 
  • Slominski A, Pisarchik A, Zbytek B, Tobin DJ, Kauser S, Wortsman J (Jul 2003). "Functional activity of serotoninergic and melatoninergic systems expressed in the skin". Journal of Cellular Physiology 196 (1): 144–53. doi:10.1002/jcp.10287. PMID 12767050. 
  • Morcuende JA, Minhas R, Dolan L, Stevens J, Beck J, Wang K, Weinstein SL, Sheffield V (Sep 2003). "Allelic variants of human melatonin 1A receptor in patients with familial adolescent idiopathic scoliosis". Spine 28 (17): 2025–8; discussion 2029. doi:10.1097/01.BRS.0000083235.74593.49. PMID 12973153. 
  • Aust S, Thalhammer T, Humpeler S, Jäger W, Klimpfinger M, Tucek G, Obrist P, Marktl W, Penner E, Ekmekcioglu C (Jan 2004). "The melatonin receptor subtype MT1 is expressed in human gallbladder epithelia". Journal of Pineal Research 36 (1): 43–8. doi:10.1046/j.1600-079X.2003.00095.x. PMID 14675129.