Target Information

Target General Infomation
Target ID
T48268
Former ID
TTDS00422
Target Name
Melatonin receptor type 1B
Gene Name
MTNR1B
Synonyms
Mel-1B-R; Mel1b melatonin receptor; MTNR1B
Target Type
Successful
Disease Circadian rhythm sleep disorder [ICD9: 327.3, 780.55; ICD10: G47.2]
Epilepsy [ICD10: G40]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Function
High affinityreceptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity.
BioChemical Class
GPCR rhodopsin
Target Validation
T48268
UniProt ID
P49286
Sequence
MSENGSFANCCEAGGWAVRPGWSGAGSARPSRTPRPPWVAPALSAVLIVTTAVDVVGNLL
VILSVLRNRKLRNAGNLFLVSLALADLVVAFYPYPLILVAIFYDGWALGEEHCKASAFVM
GLSVIGSVFNITAIAINRYCYICHSMAYHRIYRRWHTPLHICLIWLLTVVALLPNFFVGS
LEYDPRIYSCTFIQTASTQYTAAVVVIHFLLPIAVVSFCYLRIWVLVLQARRKAKPESRL
CLKPSDLRSFLTMFVVFVIFAICWAPLNCIGLAVAINPQEMAPQIPEGLFVTSYLLAYFN
SCLNAIVYGLLNQNFRREYKRILLALWNPRHCIQDASKGSHAEGLQSPAPPIIGVQHQAD
AL
Drugs and Mode of Action
Drug(s) Ramelteon Drug Info Approved Insomnia [1], [2]
Tasimelteon Drug Info Approved Insomnia [3], [4]
VLB-01 Drug Info Phase 3 Epilepsy [5]
Ramelteon Drug Info Terminated Circadian rhythm sleep disorder [1], [2]
Inhibitor 5-methoxycarbonylamino-N-acetyltryptamine Drug Info [6]
Beta,beta-dimethylmelatonin Drug Info [7]
Beta-methylmelatonin Drug Info [7]
IODOMELATONIN Drug Info [8]
N-(2,3,4,9-Tetrahydro-1H-carbazol-3-yl)-acetamide Drug Info [9]
N-(2-(5-methoxybenzofuran-3-yl)ethyl)acetamide Drug Info [6]
N-(3-(2,5-dimethoxyphenyl)propyl)acetamide Drug Info [10]
N-(3-(2-ethoxy-5-methoxyphenyl)propyl)acetamide Drug Info [10]
N-(3-(2-hydroxy-5-methoxyphenyl)propyl)acetamide Drug Info [10]
N-(3-(3-methoxyphenyl)-3-phenylallyl)acetamide Drug Info [11]
N-(3-(3-methoxyphenyl)propyl)acetamide Drug Info [10]
N-(3-(3-methoxyphenyl)propyl)propionamide Drug Info [10]
N-(3-(4-hydroxy-3-methoxyphenyl)propyl)acetamide Drug Info [10]
N-(3-(5-methoxy-2-propoxyphenyl)propyl)acetamide Drug Info [10]
N-(3-Benzooxazol-7-yl-propyl)-acetamide Drug Info [12]
N-(3-Benzooxazol-7-yl-propyl)-butyramide Drug Info [12]
N-(3-Benzooxazol-7-yl-propyl)-propionamide Drug Info [12]
N-[3-(2-Ethyl-benzooxazol-7-yl)-propyl]-acetamide Drug Info [12]
UCM-454 Drug Info [11]
Modulator Ramelteon Drug Info [13], [14]
VLB-01 Drug Info [15]
Agonist Tasimelteon Drug Info [3]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Circadian entrainment
Reactome Class A/1 (Rhodopsin-like receptors)
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Small Ligand GPCRs
GPCR ligand binding
GPCR downstream signaling
References
REF 1Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
REF 2(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: 1356).
REF 3(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).
REF 4Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032715)
REF 6Bioorg 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.
REF 7J 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.
REF 8J Med Chem. 2002 Apr 25;45(9):1853-9.Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).
REF 9Mapping 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).
REF 10Bioorg 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.
REF 11J 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.
REF 12Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
REF 13Ramelteon: a melatonin receptor agonist for the treatment of insomnia. J Postgrad Med. 2008 Jan-Mar;54(1):45-8.
REF 14MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014 Apr 24;57(8):3161-85.
REF 15Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.