MT<sub>1</sub> receptor | Melatonin receptors | IUPHAR/BPS Guide to PHARMACOLOGY

MT1 receptor

Target id: 287

Nomenclature: MT1 receptor

Family: Melatonin receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for MT1 receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 350 4q35.1 MTNR1A melatonin receptor 1A 60-61,72
Mouse 7 353 8 B1.1 Mtnr1a melatonin receptor 1A 64
Rat 7 353 16q11 Mtnr1a melatonin receptor 1A 3
Previous and Unofficial Names
mel1a receptor | MelR
Database Links
Specialist databases
GPCRDB mtr1a_human (Hs), mtr1a_mouse (Mm)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Associated Proteins
Interacting Proteins
Name Effect References
MT2 receptor 5-6
GPR50 44
Natural/Endogenous Ligands
melatonin

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]SD6 Hs Full agonist 10.9 pKd 43
pKd 10.9 (Kd 1.4x10-11 M) [43]
2-[125I]melatonin Hs Full agonist 9.9 – 10.7 pKd 4,25
pKd 9.9 – 10.7 (Kd 1.19x10-10 – 2.13x10-11 M) [4,25]
[3H]melatonin Hs Full agonist 9.4 – 9.9 pKd 12
pKd 9.4 – 9.9 (Kd 4x10-10 – 1.3x10-10 M) [12]
ramelteon Hs Full agonist 10.9 pKi 38
pKi 10.9 [38]
2-iodo-melatonin Hs Full agonist 10.2 – 11.0 pKi 4,19
pKi 10.2 – 11.0 [4,19]
2-methoxy-α,β-didehydro-agomelatine Hs Full agonist 10.5 pKi 53
pKi 10.5 (Ki 3x10-11 M) [53]
difluoroagomelatine Hs Full agonist 10.5 pKi 31
pKi 10.5 (Ki 3x10-11 M) [31]
agomelatine Hs Full agonist 10.0 – 10.4 pKi 4,8
pKi 10.0 – 10.4 [4,8]
EFPPEA Hs Full agonist 10.2 pKi 40
pKi 10.2 (Ki 6.2x10-11 M) [40]
LY 156735 Hs Full agonist 10.1 pKi 54
pKi 10.1 [54]
GR 196429 Hs Full agonist 9.4 – 9.9 pKi 8,12
pKi 9.4 – 9.9 [8,12]
tasimelteon Hs Full agonist 9.5 pKi 80
pKi 9.5 (Ki 3.04x10-10 M) [80]
melatonin Hs Full agonist 9.1 – 9.7 pKi 4,19,25
pKi 9.1 – 9.7 [4,19,25]
CBOBNEA Hs Partial agonist 9.3 pKi 55
pKi 9.3 (Ki 5.5x10-10 M) [55]
UCM 793 Hs Full agonist 9.1 pKi 62
pKi 9.1 [62]
6-hydroxymelatonin Hs Full agonist 8.9 – 9.2 pKi 8,12,19,25
pKi 8.9 – 9.2 [8,12,19,25]
AAE-M-PBP-amine Hs Partial agonist 8.9 pKi 63
pKi 8.9 [63]
S26284 Hs Partial agonist 8.5 – 9.2 pKi 4
pKi 8.5 – 9.2 [4]
6-Cl-MLT Hs Full agonist 7.9 – 9.2 pKi 4,8,19,25
pKi 7.9 – 9.2 [4,8,19,25]
IIK7 Hs Full agonist 8.3 pKi 32
pKi 8.3 [32]
5-HEAT Hs Full agonist 7.8 pKi 58
pKi 7.8 [58]
S24014 Hs Partial agonist 7.5 pKi 4
pKi 7.5 [4]
S24773 Hs Full agonist 7.1 pKi 4
pKi 7.1 [4]
GR 128107 Hs Partial agonist 6.9 pKi 25,75
pKi 6.9 [25,75]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
S26131 Hs Antagonist 8.4 – 9.3 pKi 4
pKi 8.4 – 9.3 [4]
S22153 Hs Antagonist 7.8 – 8.1 pKi 4
pKi 7.8 – 8.1 [4]
UCM 549 Hs Antagonist 7.6 – 8.2 pKi 46,74
pKi 7.6 – 8.2 [46,74]
K185 Hs Antagonist 7.2 pKi 32
pKi 7.2 [32]
UCM 724 Hs Antagonist 6.9 pKi 74
pKi 6.9 [74]
4P-PDOT Hs Antagonist 6.2 – 7.2 pKi 4,25,27
pKi 6.2 – 7.2 [4,25,27]
S20928 Hs Antagonist 6.4 – 6.9 pKi 4
pKi 6.4 – 6.9 [4]
luzindole Hs Antagonist 6.2 – 6.8 pKi 4,12,20,25
pKi 6.2 – 6.8 [4,12,20,25]
AZD7325 Hs Antagonist 6.9 pIC50 2
pIC50 6.9 (IC50 1.26x10-7 M) [2]
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  26,38,47,51,60
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Potassium channel
Calcium channel
References:  26,47,51,65
Tissue Distribution
Retina.
Species:  Human
Technique:  RT-PCR.
References:  69
Fetal kidney.
Species:  Human
Technique:  RT-PCR.
References:  18
Coronary artery.
Species:  Human
Technique:  RT-PCR.
References:  29-30
Granulosa cells.
Species:  Human
Technique:  RT-PCR.
References:  57,73
Retina.
Species:  Human
Technique:  Immunocytochemistry.
References:  67-70
Brain: cerebellum, occipital cortex, parietal cortex, temporal cortex, thalamus, frontal cortex, hippocampus.
Species:  Human
Technique:  RT-PCR.
References:  52
Hippocampus.
Species:  Human
Technique:  Immunohistochemistry.
References:  67
Cerebellum.
Species:  Human
Technique:  in situ hybridisation.
References:  1
Brown and white adipose tissue, PAZ6 adipocytes.
Species:  Human
Technique:  RT-PCR.
References:  13
Suprachiasmatic nucleus.
Species:  Human
Technique:  in situ hybridisation.
References:  83
Cerebellar granule cells.
Species:  Human
Technique:  in situ hybridisation.
References:  52
Brain, heart, lung, liver, kidney.
Species:  Mouse
Technique:  RT-PCR.
References:  56
Retina
Species:  Mouse
Technique:  In situ hybridisation, immunohistochemistry
References:  7,71
Hypothalamus, retina, small intestine.
Species:  Rat
Technique:  RT-PCR.
References:  66
Tissue Distribution Comments
For a review on melatonin receptor function see [21-22,24,26,78,87].
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of the potentiation of adrenergic contraction in vascular beds.
Species:  Rat
Tissue:  Caudal artery.
Response measured:  Vasoconstriction.
References:  17,33,41,50,76-77
Measurement of neuronal firing in the mouse suprachiasmatic nucleus.
Species:  Mouse
Tissue:  Suprachiasmatic nucleus slice.
Response measured:  Inhibition of neuronal firing.
References:  45
Measurement of cAMP levels in NIH 3T3 cells transfected with the human MT1 receptor.
Species:  Human
Tissue:  NIH 3T3 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  32
Measurement of [35S]GTPγS binding in CHO cells transfected with the human MT1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  [35S]GTPγS binding.
References:  4,9
Measurement of [35S]GTPγS binding in NIH 3T3 cells transfected with the human MT1 receptor.
Species:  Human
Tissue:  NIH 3T3 cells.
Response measured:  [35S]GTPγS binding.
References:  58
Measurement of melatonin-mediated vasoconstriction in rat cerebral arteries.
Species:  Rat
Tissue:  Cerebral arteries.
Response measured:  Vasoconstriction.
References:  34,48
Measurement of cAMP levels in CHO cells transfected with the human MT1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP accumulation.
References:  12,38,85
Physiological Functions
Inhibition of neuronal firing.
Species:  Mouse
Tissue:  Suprachiasmatic nucleus slice.
References:  45
Inhibition LH and FSH.
Species:  Rat
Tissue:  Pituitary.
References:  36-37,81
Inhibition of prolactin secretion.
Species:  Mouse
Tissue:  Pars tuberalis.
References:  82
Inhibition of cancer cell growth.
Species:  Human
Tissue:  MCF-7 human breast cancer cells.
References:  10-11,59
Vasoconstriction.
Species:  Human
Tissue:  Coronary artery.
References:  48
Inhibition of insulin release.
Species:  Rat
Tissue:  Pancreatic b cells (INS-1 b).
References:  39
Inhibition of GnRH-dependent testosterone secretion.
Species:  Rat
Tissue:  Leydig cells.
References:  79
Induction of IL-2 by melatonin is mediated by MT1R
Species:  Human
Tissue:  Jurkat cells (immortalized line of human lymphocytes)
References:  42
Induction of IL-2 by melatonin is mediated by MT1R
Species:  Human
Tissue:  Peripheral blood mononuclear cells
References:  14
Physiological Consequences of Altering Gene Expression
MT1 receptor knockout mice exhibit depression-like behaviour and reduced mobility in the forced swim test compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  84
Loss of phase shift of circadian rhythms of activity by melatonin in MT1 knockout mice.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  23
MT1 receptor knockout exhibit altered gene expression in Pars Tuberalis
Species:  Mouse
Tissue:  Pars tuberalis
Technique:  Transgenic
References:  35,82,86
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Mtnr1atm1Rep Mtnr1atm1Rep/Mtnr1atm1Rep
involves: 129S4/SvJae * C57BL/6
MGI:102967  MP:0001502 abnormal circadian rhythm PMID: 9247266 
Mtnr1atm1Rep Mtnr1atm1Rep/Mtnr1atm1Rep
involves: 129S4/SvJae * C57BL/6
MGI:102967  MP:0002564 advanced circadian phase PMID: 9247266 
Biologically Significant Variants
Type:  Missense mutation
Species:  Human
Description:  Rare variant identified in control population with reduced cAMP inhibition
Amino acid change:  K334N
Nucleotide accession: 
Protein accession: 
References:  16
Type:  Missense mutation
Species:  Human
Description:  Common variant identified in control population, impaired cell surface expression, cAMP inhibition and reduced ERK1/2 activation
Amino acid change:  I212T
Nucleotide accession: 
Protein accession: 
References:  16
Type:  Missense mutation
Species:  Human
Description:  Rare variant identified in autism spectrum disorder patients, impaired cell surface expression, melatonin binding, cAMP inhibition and ERK1/1 activation
Amino acid change:  I49N
Nucleotide accession: 
Protein accession: 
References:  16
Type:  Missense mutation
Species:  Human
Description:  Common variant identified in control population, impaired cell surface expression, reduced cAMP inhibition and ERK1/2 activation
Amino acid change:  G166E
Nucleotide accession: 
Protein accession: 
References:  16
Type:  Missense mutation
Species:  Human
Description:  Common variant identified in control population without obvious functional defect
Amino acid change:  A157V
Nucleotide accession: 
Protein accession: 
References:  16,28
Type:  Missense mutation
Species:  Human
Description:  Common variant identified in control population without obvious functional defect
Amino acid change:  R54W
Nucleotide accession: 
Protein accession: 
References:  28
Type:  Nonsense mutation
Species:  Human
Description:  Rare variant identified in attention-deficit hyperactivity disorder (ADHD) patient, premature STOP codon with impaired cell surface expression and cAMP inhibition
Amino acid change:  Y170X
Nucleotide accession: 
Protein accession: 
References:  15
Type:  Missense mutation
Species:  Human
Description:  Common variant identified in control population with reduced ERK1/2 activation
Amino acid change:  A266V
Nucleotide accession: 
Protein accession: 
References:  16
General Comments
The molecular pharmacology of ovine melatonin receptors has been shown to be different to human recombinant melatonin receptors [49].

References

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1. Al-Ghoul WM, Herman MD, Dubocovich ML. (1998) Melatonin receptor subtype expression in human cerebellum. Neuroreport, 9: 4063-4068. [PMID:9926848]

2. AstraZeneca. AZD7325. Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd7325/

3. Audinot V, Bonnaud A, Grandcolas L, Rodriguez M, Nagel N, Galizzi JP, Balik A, Messager S, Hazlerigg DG, Barrett P et al.. (2008) Molecular cloning and pharmacological characterization of rat melatonin MT1 and MT2 receptors. Biochem. Pharmacol., 75 (10): 2007-19. [PMID:18384758]

4. Audinot V, Mailliet F, Lahaye-Brasseur C, Bonnaud A, Le Gall A, Amossé C, Dromaint S, Rodriguez M, Nagel N, Galizzi JP, Malpaux B, Guillaumet G, Lesieur D, Lefoulon F, Renard P, Delagrange P, Boutin JA. (2003) New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol, 367: 553-561. [PMID:12764576]

5. Ayoub MA, Couturier C, Lucas-Meunier E, Angers S, Fossier P, Bouvier M, Jockers R. (2002) Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer. J. Biol. Chem., 277 (24): 21522-8. [PMID:11940583]

6. Ayoub MA, Levoye A, Delagrange P, Jockers R. (2004) Preferential formation of MT1/MT2 melatonin receptor heterodimers with distinct ligand interaction properties compared with MT2 homodimers. Mol. Pharmacol., 66 (2): 312-21. [PMID:15266022]

7. Baba K, Pozdeyev N, Mazzoni F, Contreras-Alcantara S, Liu C, Kasamatsu M, Martinez-Merlos T, Strettoi E, Iuvone PM, Tosini G. (2009) Melatonin modulates visual function and cell viability in the mouse retina via the MT1 melatonin receptor. Proc. Natl. Acad. Sci. U.S.A., 106 (35): 15043-8. [PMID:19706469]

8. Beresford IJ, Browning C, Starkey SJ, Brown J, Foord SM, Coughlan J, North PC, Dubocovich ML, Hagan RM. (1998) GR196429: a nonindolic agonist at high-affinity melatonin receptors. J Pharmacol Exp Ther, 285: 1239-1245. [PMID:9618428]

9. Beresford IJ, Harvey FJ, Hall DA, Giles H. (1998) Pharmacological characterisation of melatonin mt1 receptor-mediated stimulation of [35S]-GTPgammaS binding. Biochem Pharmacol, 56: 1167-1174. [PMID:9802327]

10. Blask DE, Brainard GC, Dauchy RT, Hanifin JP, Davidson LK, Krause JA, Sauer LA, Rivera-Bermudez MA, Dubocovich ML, Jasser SA, Lynch DT, Rollag MD, Zalatan F. (2005) Melatonin-depleted blood from premenopausal women exposed to light at night stimulates growth of human breast cancer xenografts in nude rats. Cancer Res, 65: 11174-11184. [PMID:16322268]

11. Blask DE, Dauchy RT, Sauer LA, Krause JA, Brainard GC. (2002) Light during darkness, melatonin suppression and cancer progression. Neuro Endocrinol Lett, 23 Suppl 2: 52-56. [PMID:12163849]

12. Browning C, Beresford I, Fraser N, Giles H. (2000) Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors. Br. J. Pharmacol., 129: 877-886. [PMID:10696085]

13. Brydon L, Petit L, Delagrange P, Strosberg AD, Jockers R. (2001) Functional expression of MT2 (Mel1b) melatonin receptors in human PAZ6 adipocytes. Endocrinology, 142: 4264-4271. [PMID:11564683]

14. Carrillo-Vico A, García-Mauriño S, Calvo JR, Guerrero JM. (2003) Melatonin counteracts the inhibitory effect of PGE2 on IL-2 production in human lymphocytes via its mt1 membrane receptor. FASEB J., 17 (6): 755-7. [PMID:12594180]

15. Chaste P, Clement N, Botros HG, Guillaume JL, Konyukh M, Pagan C, Scheid I, Nygren G, Anckarsäter H, Rastam M et al.. (2011) Genetic variations of the melatonin pathway in patients with attention-deficit and hyperactivity disorders. J. Pineal Res., 51 (4): 394-9. [PMID:21615493]

16. Chaste P, Clement N, Mercati O, Guillaume JL, Delorme R, Botros HG, Pagan C, Périvier S, Scheid I, Nygren G, Anckarsäter H, Rastam M, Ståhlberg O, Gillberg C, Serrano E, Lemière N, Launay JM, Mouren-Simeoni MC, Leboyer M, Gillberg C, Jockers R, Bourgeron T. (2010) Identification of pathway-biased and deleterious melatonin receptor mutants in autism spectrum disorders and in the general population. PLoS ONE, 5 (7): e11495. [PMID:20657642]

17. Doolen S, Krause DN, Dubocovich ML, Duckles SP. (1998) Melatonin mediates two distinct responses in vascular smooth muscle. Eur J Pharmacol, 345: 67-69. [PMID:9593596]

18. Drew JE, Williams LM, Hannah LT, Barrett P, Abramovich DR. (1998) Melatonin receptors in the human fetal kidney: 2-[125I]iodomelatonin binding sites correlated with expression of Mel1a and Mel1b receptor genes. J Endocrinol, 156: 261-267. [PMID:9518871]

19. Dubocovich ML. (1985) Characterization of a retinal melatonin receptor. J. Pharmacol. Exp. Ther., 234 (2): 395-401. [PMID:2991499]

20. Dubocovich ML. (1988) Luzindole (N-0774): a novel melatonin receptor antagonist. J. Pharmacol. Exp. Ther., 246 (3): 902-10. [PMID:2843633]

21. Dubocovich ML. (2007) Melatonin receptors: role on sleep and circadian rhythm regulation. Sleep Med., 8 Suppl 3: 34-42. [PMID:18032103]

22. Dubocovich ML, Delagrange P, Krause DN, Sugden D, Cardinali DP, Olcese J. (2010) International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors. Pharmacol. Rev., 62 (3): 343-80. [PMID:20605968]

23. Dubocovich ML, Hudson RL, Sumaya IC, Masana MI, Manna E. (2005) Effect of MT1 melatonin receptor deletion on melatonin-mediated phase shift of circadian rhythms in the C57BL/6 mouse. J Pineal Res, 39: 113-120. [PMID:16098087]

24. Dubocovich ML, Markowska M. (2005) Functional MT1 and MT2 melatonin receptors in mammals. Endocrine, 27: 101-110. [PMID:16217123]

25. Dubocovich ML, Masana MI, Iacob S, Sauri DM. (1997) Melatonin receptor antagonists that differentiate between the human Mel1aand Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch. Pharmacol., 355: 365-375. [PMID:9089668]

26. Dubocovich ML, Rivera-Bermudez MA, Gerdin MJ, Masana MI. (2003) Molecular pharmacology, regulation and function of mammalian melatonin receptors. Front Biosci, 8: d1093-d1108. [PMID:12957828]

27. Dubocovich ML, Yun K, Al-Ghoul WM, Benloucif S, Masana MI. (1998) Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms. FASEB J, 12: 1211-1220. [PMID:9737724]

28. Ebisawa T, Kajimura N, Uchiyama M, Katoh M, Sekimoto M, Watanabe T, Ozeki Y, Ikeda M, Jodoi T, Sugishita M et al.. (1999) Alleic variants of human melatonin 1a receptor: function and prevalence in subjects with circadian rhythm sleep disorders. Biochem. Biophys. Res. Commun., 262 (3): 832-7. [PMID:10471411]

29. Ekmekcioglu C, Haslmayer P, Philipp C, Mehrabi MR, Glogar HD, Grimm M, Leibetseder VJ, Thalhammer T, Marktl W. (2001) Expression of the MT1 melatonin receptor subtype in human coronary arteries. J Recept Signal Transduct Res, 21: 85-91. [PMID:11693175]

30. Ekmekcioglu C, Haslmayer P, Philipp C, Mehrabi MR, Glogar HD, Grimm M, Thalhammer T, Marktl W. (2001) 24h variation in the expression of the mt1 melatonin receptor subtype in coronary arteries derived from patients with coronary heart disease. Chronobiol Int, 18: 973-985. [PMID:11777084]

31. Ettaoussi M, Sabaouni A, Rami M, Boutin JA, Delagrange P, Renard P, Spedding M, Caignard DH, Berthelot P, Yous S. (2012) Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I). Eur J Med Chem, 49: 310-23. [PMID:22301214]

32. Faust R, Garratt PJ, Jones R, Yeh LK, Tsotinis A, Panoussopoulou M, Calogeropoulou T, Teh MT, Sugden D. (2000) Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles. J Med Chem, 43: 1050-1061. [PMID:10737738]

33. Geary GG, Duckles SP, Krause DN. (1998) Effect of melatonin in the rat tail artery: role of K+ channels and endothelial factors. Br J Pharmacol, 123: 1533-1540. [PMID:9605558]

34. Geary GG, Krause DN, Duckles SP. (1997) Melatonin directly constricts rat cerebral arteries through modulation of potassium channels. Am J Physiol, 273: H1530-H1536. [PMID:9321846]

35. Jilg A, Moek J, Weaver DR, Korf HW, Stehle JH, von Gall C. (2005) Rhythms in clock proteins in the mouse pars tuberalis depend on MT1 melatonin receptor signalling. Eur. J. Neurosci., 22 (11): 2845-54. [PMID:16324119]

36. Johnston JD, Messager S, Barrett P, Hazlerigg DG. (2003) Melatonin action in the pituitary: neuroendocrine synchronizer and developmental modulator?. J Neuroendocrinol, 15: 405-408. [PMID:12622841]

37. Johnston JD, Messager S, Ebling FJ, Williams LM, Barrett P, Hazlerigg DG. (2003) Gonadotrophin-releasing hormone drives melatonin receptor down-regulation in the developing pituitary gland. Proc Natl Acad Sci U S A, 100: 2831-2835. [PMID:12598657]

38. Kato K, Hirai K, Nishiyama K, Uchikawa O, Fukatsu K, Ohkawa S, Kawamata Y, Hinuma S, Miyamoto M. (2005) Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology, 48: 301-310. [PMID:15695169]

39. Kemp DM, Ubeda M, Habener JF. (2002) Identification and functional characterization of melatonin Mel 1a receptors in pancreatic beta cells: potential role in incretin-mediated cell function by sensitization of cAMP signaling. Mol Cell Endocrinol, 191: 157-166. [PMID:12062899]

40. Koike T, Takai T, Hoashi Y, Nakayama M, Kosugi Y, Nakashima M, Yoshikubo S, Hirai K, Uchikawa O. (2011) Synthesis of a novel series of tricyclic dihydrofuran derivatives: discovery of 8,9-dihydrofuro[3,2-c]pyrazolo[1,5-a]pyridines as melatonin receptor (MT1/MT2) ligands. J. Med. Chem., 54 (12): 4207-18. [PMID:21568291]

41. Krause DN, Barrios VE, Duckles SP. (1995) Melatonin receptors mediate potentiation of contractile responses to adrenergic nerve stimulation in rat caudal artery. Eur J Pharmacol, 276: 207-213. [PMID:7601206]

42. Lardone PJ, Rubio A, Cerrillo I, Gómez-Corvera A, Carrillo-Vico A, Sanchez-Hidalgo M, Guerrero JM, Fernandez-Riejos P, Sanchez-Margalet V, Molinero P. (2010) Blocking of melatonin synthesis and MT(1) receptor impairs the activation of Jurkat T cells. Cell. Mol. Life Sci., 67 (18): 3163-72. [PMID:20440532]

43. Legros C, Matthey U, Grelak T, Pedragona-Moreau S, Hassler W, Yous S, Thomas E, Suzenet F, Folleas B, Lefoulon F et al.. (2013) New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors. Int J Mol Sci, 14 (5): 8948-62. [PMID:23698757]

44. Levoye A, Dam J, Ayoub MA, Guillaume JL, Couturier C, Delagrange P, Jockers R. (2006) The orphan GPR50 receptor specifically inhibits MT1 melatonin receptor function through heterodimerization. EMBO J., 25 (13): 3012-23. [PMID:16778767]

45. Liu C, Weaver DR, Jin X, Shearman LP, Pieschl RL, Gribkoff VK, Reppert SM. (1997) Molecular dissection of two distinct actions of melatonin on the suprachiasmatic circadian clock. Neuron, 19: 91-102. [PMID:9247266]

46. Lucini V, Pannacci M, Scaglione F, Fraschini F, Rivara S, Mor M, Bordi F, Plazzi PV, Spadoni G, Bedini A et al.. (2004) Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity. J. Med. Chem., 47 (17): 4202-12. [PMID:15293992]

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Ralf Jockers, Philippe Delagrange, Margarita L. Dubocovich, Regina Pekelmann Markus, Nicolas Renault, Gianluca Tosini, Darius Paul Zlotos, Daniel P. Cardinali, Diana N. Krause, James Olcese, David Sugden.
Melatonin receptors: MT1 receptor. Last modified on 20/02/2018. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=287.