Therapeutic Targets Database
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TTD Target ID: TTDS00393

Target Information
NameMelatonin receptor type 1A    
Type of targetSuccessful target    
DiseaseChronic Primary Insomnia    [1]
Insomnia    [1]
Major Depressive Disorder    [1]
Drug(s)MelatoninApprovedInsomnia[2][3]
RamelteonApprovedInsomnia[4]
VEC-162Phase III completedTransient insomnia[5]
LY-156735Phase II completedCircadian rhythm disorders[6]
AgomelatineWithdrawn in MAAMajor depressive disorder[5]
RamelteonDiscontinuedCircadian rhythm sleep disorder(CRSD)[7]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP48039
SequenceMQGNGSALPNASQPVLRGDGARPSWLASALACVLIFTIVVDILGNLLVILSVYRNKKLRN AGNIFVVSLAVADLVVAIYPYPLVLMSIFNNGWNLGYLHCQVSGFLMGLSVIGSIFNITG IAINRYCYICHSLKYDKLYSSKNSLCYVLLIWLLTLAAVLPNLRAGTLQYDPRIYSCTFA QSVSSAYTIAVVVFHFLVPMIIVIFCYLRIWILVLQVRQRVKPDRKPKLKPQDFRNFVTM FVVFVLFAICWAPLNFIGLAVASDPASMVPRIPEWLFVASYYMAYFNSCLNAIIYGLLNQ NFRKEYRRIIVSLCTARVFFVDSSNDVADRVKWKPSPLMTNNNVVKVDSV
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[8]
5-methoxycarbonylamino-N-acetyltryptamine[9]
IODOMELATONIN[10]
N- (2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide[11]
N- (2,3-Dihydro-1H-phenalen-2-yl)-acetamide[12]
N- (2-[9]
N- (3-[13]
N- (3-[13]
N- (3-[13]
N- (3-[14]
N- (3-[13]
N- (3-[13]
N- (3-[13]
N- (3-[13]
N-[2- (5-Hydroxy-1H-indol-3-yl)-ethyl]-acetamide[12]
UCM-454[14]
beta,beta-dimethylmelatonin[15]
beta-methylmelatonin[15]
AgonistAgomelatine[5]
LY-156735[6]
Ramelteon[4]
Ramelteon[7]
VEC-162[5]
BinderMelatonin[2][3]
MultitargetRamelteon[4]
Ramelteon[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Tasimelteon, a melatonin agonist for the treatment of insomnia and circadian rhythm sleep disorders. Curr Opin Investig Drugs. 2009 Jul;10(7):691-701. To Reference
Ref 2The 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. To Reference
Ref 3Coexpression of MT1 and RORalpha1 melatonin receptors in the Syrian hamster Harderian gland. J Pineal Res. 2005 Aug;39(1):21-6. To Reference
Ref 4Ramelteon: a review of its therapeutic potential in sleep disorders. Adv Ther. 2009 Jun;26(6):613-26. Epub 2009 Jun 30. To Reference
Ref 5Curr Top Med Chem. 2008;8(11):954-68.Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders. To Reference
Ref 6Melatonin and sleep in aging population. Exp Gerontol. 2005 Dec;40(12):911-25. Epub 2005 Sep 23. To Reference
Ref 7Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 8J Med Chem. 2010 Sep 9;53(17):6386-97.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 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 9Bioorg Med Chem. 2008 May 1;16(9):4954-62. Epub 2008 Mar 17.Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3. To Reference
Ref 10J Med Chem. 2002 Apr 25;45(9):1853-9.Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3). To Reference
Ref 11Bioorg. Med. Chem. Lett. 4(13):1559-1564 (1994) To Reference
Ref 12J Med Chem. 1996 Aug 2;39(16):3089-95.Synthesis of 2-amido-2,3-dihydro-1H-phenalene derivatives as new conformationally restricted ligands for melatonin receptors. To Reference
Ref 13Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5. Epub 2010 Feb 25.Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands. To Reference
Ref 14J Med Chem. 2009 Feb 12;52(3):826-33.2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists. To Reference
Ref 15J Med Chem. 2006 Jun 15;49(12):3509-19.Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines. To Reference



 

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