General Information of DTT (ID: TT0WAIE)

DTT Name Melatonin receptor type 1A (MTNR1A) DTT Info
Gene Name MTNR1A

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
3 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Melatonin DMKWFBT Depression 6A70-6A7Z Approved [1]
Ramelteon DM7IW9J Insomnia 7A00-7A0Z Approved [2]
Tasimelteon DMLOQ1V Insomnia 7A00-7A0Z Approved [3]
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2 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
LY-156735 DM5IX9M Anxiety disorder 6B00-6B0Z Phase 2 [4]
Neu-P11 DMIQDFW Alzheimer disease 8A20 Phase 2 [5]
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6 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Agomelatine DMXYA5K Major depressive disorder 6A70.3 Withdrawn from market [6]
GR-131663 DMKAGLV Anxiety disorder 6B00-6B0Z Terminated [7]
GR-133347 DMNRJA0 Anxiety disorder 6B00-6B0Z Terminated [8]
Luzindole DMXRJQV Sleep-wake disorder 7A00-7B2Z Terminated [9]
S-20928 DMQDWMJ Sleep-wake disorder 7A00-7B2Z Terminated [10]
SL-18.1616 DMI1WNF Insomnia 7A00-7A0Z Terminated [11]
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⏷ Show the Full List of 6 Discontinued Drug(s)
51 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(hydroxymethylphenyl)agomelatine DMOJUEC Discovery agent N.A. Investigative [12]
2-(indolin-1yl)-melatonin DMOVYXT Discovery agent N.A. Investigative [13]
2-iodo-melatonin DMSEIUP Discovery agent N.A. Investigative [14]
2-methoxy-alpha,beta-didehydro-agomelatine DM4G3FS Discovery agent N.A. Investigative [15]
2-[125I]melatonin DMFJOHG Discovery agent N.A. Investigative [16]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [17]
4P-PDOT DMEMN0W Discovery agent N.A. Investigative [18]
5-HEAT DMKUT6A Discovery agent N.A. Investigative [19]
5-methoxy-luzindole DMUXTWC Discovery agent N.A. Investigative [16]
5-methoxycarbonylamino-N-acetyltryptamine DMCZSP3 Discovery agent N.A. Investigative [20]
6-Cl-MLT DMKNOLV Discovery agent N.A. Investigative [14]
6-hydroxymelatonin DM89YV7 Discovery agent N.A. Investigative [14]
AAE-M-PBP-amine DMNO51B Discovery agent N.A. Investigative [21]
Beta,beta-dimethylmelatonin DM6FHQD Discovery agent N.A. Investigative [22]
Beta-methylmelatonin DMKH32S Discovery agent N.A. Investigative [22]
BOMPPA DMI75A3 Discovery agent N.A. Investigative [23]
CBOBNEA DMITY0H Discovery agent N.A. Investigative [24]
CIFEA DMP35OM Discovery agent N.A. Investigative [25]
DH97 DM7UVOD Discovery agent N.A. Investigative [26]
difluoroagomelatine DM8AZQ3 Discovery agent N.A. Investigative [27]
EFPPEA DMZ2XOH Discovery agent N.A. Investigative [28]
GR 128107 DMAI9Y0 Discovery agent N.A. Investigative [29]
GR 196429 DMHAWYJ Discovery agent N.A. Investigative [30]
IIK7 DMLYIBO Discovery agent N.A. Investigative [31]
isoamyl-agomelatine DMGNFXY Discovery agent N.A. Investigative [27]
K185 DME65H8 Discovery agent N.A. Investigative [31]
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide DMWC70I Discovery agent N.A. Investigative [32]
N-(2,3-Dihydro-1H-phenalen-2-yl)-acetamide DMPL26K Discovery agent N.A. Investigative [33]
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide DM4V7AS Discovery agent N.A. Investigative [20]
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide DM4ZTF1 Discovery agent N.A. Investigative [34]
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide DMLWGPC Discovery agent N.A. Investigative [34]
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide DMI452E Discovery agent N.A. Investigative [34]
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide DMH0LOT Discovery agent N.A. Investigative [13]
N-(3-(3-methoxyphenyl)propyl)acetamide DMSZ03N Discovery agent N.A. Investigative [34]
N-(3-(3-methoxyphenyl)propyl)propionamide DMKSM5A Discovery agent N.A. Investigative [34]
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide DMILWPS Discovery agent N.A. Investigative [34]
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide DMHM0WI Discovery agent N.A. Investigative [34]
N-acetylserotonin DMJ4SBM Discovery agent N.A. Investigative [33]
S22153 DM4S5TQ Discovery agent N.A. Investigative [35]
S24014 DM9RU46 Discovery agent N.A. Investigative [35]
S24773 DM1HAD0 Discovery agent N.A. Investigative [35]
S26131 DMCJ86U Discovery agent N.A. Investigative [35]
S26284 DMLJITC Discovery agent N.A. Investigative [35]
UCM 549 DM9JG1L Discovery agent N.A. Investigative [36]
UCM 724 DMCKSYQ Discovery agent N.A. Investigative [36]
UCM 765 DMD16MH Discovery agent N.A. Investigative [37]
UCM 793 DM8J41W Discovery agent N.A. Investigative [37]
UCM-454 DMSVJFG Discovery agent N.A. Investigative [13]
[125I]DIV880 DMEPT8H Discovery agent N.A. Investigative [38]
[125I]S70254 DMHC6KX Discovery agent N.A. Investigative [38]
[125I]SD6 DM285MQ Discovery agent N.A. Investigative [38]
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⏷ Show the Full List of 51 Investigative Drug(s)
Molecule Interaction Atlas

References

1 The human MT1 melatonin receptor stimulates cAMP production in the human neuroblastoma cell line SH-SY5Y cells via a calcium-calmodulin signal transduction pathway. J Neuroendocrinol. 2005 Mar;17(3):170-8.
2 MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014 Apr 24;57(8):3161-85.
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7393).
4 Melatonin and sleep in aging population. Exp Gerontol. 2005 Dec;40(12):911-25.
5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 288).
6 Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders. Curr Top Med Chem. 2008;8(11):954-68.
7 Novel non-indolic melatonin receptor agonists differentially entrain endogenous melatonin rhythm and increase its amplitude. Eur J Pharmacol. 1999 Oct 15;382(3):157-66.
8 US patent application no. 5,151,446, Substituted 2-amidotetralins as melatonin agonists and antagonists.
9 Luzindole (N-0774): a novel melatonin receptor antagonist. J Pharmacol Exp Ther. 1988 Sep;246(3):902-10.
10 Effects of two melatonin analogues, S-20098 and S-20928, on melatonin receptors in the pars tuberalis of the rat. J Pineal Res. 1998 Oct;25(3):172-6.
11 US patent application no. 2005,016,4987, Melatonin combination therapy for improving sleep quality.
12 Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands. Bioorg Med Chem. 2008 Sep 15;16(18):8339-48.
13 2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists. J Med Chem. 2009 Feb 12;52(3):826-33.
14 Characterization of a retinal melatonin receptor. J Pharmacol Exp Ther. 1985 Aug;234(2):395-401.
15 Synthesis of new N-(arylcyclopropyl)acetamides and N-(arylvinyl)acetamides as conformationally-restricted ligands for melatonin receptors. Bioorg Med Chem Lett. 2013 Jan 15;23(2):430-4.
16 Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):365-75.
17 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
18 Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms. FASEB J. 1998 Sep;12(12):1211-20.
19 A new melatonin receptor ligand with mt1-agonist and MT2-antagonist properties. J Pineal Res. 2000 Nov;29(4):234-40.
20 Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3. Bioorg Med Chem. 2008 May 1;16(9):4954-62.
21 MT1-selective melatonin receptor ligands: synthesis, pharmacological evaluation, and molecular dynamics investigation of N-{[(3-O-substituted)anilino]alkyl}amides. ChemMedChem. 2012 Nov;7(11):1954-64.
22 Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-me... J Med Chem. 2006 Jun 15;49(12):3509-19.
23 Development of substituted N-[3-(3-methoxylphenyl)propyl] amides as MT(2)-selective melatonin agonists: improving metabolic stability. Bioorg Med Chem. 2013 Jan 15;21(2):547-52.
24 Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands. Bioorg Med Chem. 2010 May 15;18(10):3426-36.
25 1,6-Dihydro-2H-indeno[5,4-b]furan derivatives: design, synthesis, and pharmacological characterization of a novel class of highly potent MT selective agonists. J Med Chem. 2011 May 12;54(9):3436-44.
26 Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores. Naunyn Schmiedebergs Arch Pharmacol. 1998 Nov;358(5):522-8.
27 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. 2012 Mar;49:310-23.
28 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. 2011 Jun 23;54(12):4207-18.
29 The putative melatonin receptor antagonist GR128107 is a partial agonist on Xenopus laevis melanophores. Br J Pharmacol. 1999 Mar;126(5):1237-45.
30 GR196429: a nonindolic agonist at high-affinity melatonin receptors. J Pharmacol Exp Ther. 1998 Jun;285(3):1239-45.
31 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. 2000 Mar 23;43(6):1050-61.
32 Mapping the melatonin receptor. 2. synthesis and biological activity of indole derived melatonin analogues with restricted conformations of the C-3 amidoethane side chain, Bioorg. Med. Chem. Lett. 4(13):1559-1564 (1994).
33 Synthesis of 2-amido-2,3-dihydro-1H-phenalene derivatives as new conformationally restricted ligands for melatonin receptors. J Med Chem. 1996 Aug 2;39(16):3089-95.
34 Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5.
35 New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jun;367(6):553-61.
36 Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists. ChemMedChem. 2007 Dec;2(12):1741-9.
37 N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands. J Med Chem. 2007 Dec 27;50(26):6618-26.
38 New radioligands for describing the molecular pharmacology of MT1 and MT2 melatonin receptors. Int J Mol Sci. 2013 Apr 25;14(5):8948-62.