Target Information
Target General Infomation | |||||
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Target ID |
T84486
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Former ID |
TTDS00264
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Target Name |
Oxytocin receptor
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Gene Name |
OXTR
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Synonyms |
OT-R; OXTR
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Target Type |
Successful
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Disease | Androgen decline [ICD10: E20-E35] | ||||
Autism [ICD9: 299; ICD10: F84.0] | |||||
Erectile dysfunction [ICD9: 302.72, 607.84; ICD10: F52.2, N48.4] | |||||
Female sexual dysfunction [ICD9: 302.7; ICD10: F52] | |||||
Miscarriage [ICD10: O03] | |||||
Postpartum haemorrhage [ICD9: 666; ICD10: O72] | |||||
Premature ejaculation [ICD9: 302.75; ICD10: F52.4] | |||||
Threatened pre-term labour [ICD10: O60.1, P07.3] | |||||
Function |
Receptor for oxytocin. The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol- calcium second messenger system.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T84486
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UniProt ID | |||||
Sequence |
MEGALAANWSAEAANASAAPPGAEGNRTAGPPRRNEALARVEVAVLCLILLLALSGNACV
LLALRTTRQKHSRLFFFMKHLSIADLVVAVFQVLPQLLWDITFRFYGPDLLCRLVKYLQV VGMFASTYLLLLMSLDRCLAICQPLRSLRRRTDRLAVLATWLGCLVASAPQVHIFSLREV ADGVFDCWAVFIQPWGPKAYITWITLAVYIVPVIVLAACYGLISFKIWQNLRLKTAAAAA AEAPEGAAAGDGGRVALARVSSVKLISKAKIRTVKMTFIIVLAFIVCWTPFFFVQMWSVW DANAPKEASAFIIVMLLASLNSCCNPWIYMLFTGHLFHELVQRFLCCSASYLKGRRLGET SASKKSNSSSFVLSHRSSSQRSCSQPSTA |
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Drugs and Mode of Action | |||||
Drug(s) | Carbetocin | Drug Info | Approved | Postpartum haemorrhage | [544501] |
Oxytocin | Drug Info | Approved | Autism | [539377] | |
ATOSIBAN | Drug Info | Phase 4 | Discovery agent | [524034], [539407] | |
GSK221149 | Drug Info | Phase 3 | Threatened pre-term labour | [548262] | |
Retosiban | Drug Info | Phase 3 | Threatened pre-term labour | [525102], [543110] | |
Barusiban | Drug Info | Phase 2 | Androgen decline | [521712] | |
FE-202767 | Drug Info | Phase 2 | Erectile dysfunction | [525314] | |
GSK-557296 | Drug Info | Phase 2 | Premature ejaculation | [522869] | |
L-368899 | Drug Info | Discontinued in Phase 1 | Miscarriage | [539423], [546833] | |
PF-3274167 | Drug Info | Discontinued in Phase 1 | Female sexual dysfunction | [548448] | |
TT-235 | Drug Info | Discontinued in Phase 1 | Miscarriage | [546859] | |
AS-602305 | Drug Info | Terminated | Androgen decline | [547962] | |
L-371257 | Drug Info | Terminated | Discovery agent | [539425], [546463] | |
Inhibitor | 1'-tosylspiro[indene-1,4'-piperidine] | Drug Info | [530975] | ||
ARGENINE VASOPRESSIN | Drug Info | [528674] | |||
ATOSIBAN | Drug Info | [527874] | |||
D(CH2)5[Tyr(Me)2,Thr4,Orn8(5/6C-Flu),Tyr-NH29]VT | Drug Info | [526347] | |||
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT | Drug Info | [526347] | |||
DesGly-NH2,d(CH2)5[D-Tyr2,Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Arg4,Dab8]VP | Drug Info | [528674] | |||
D[Arg4,Lys8]VP | Drug Info | [528674] | |||
D[Arg4,Orn8]VP | Drug Info | [528674] | |||
D[Arg4]AVP | Drug Info | [528674] | |||
D[Cha4,Dab8]VP | Drug Info | [528674] | |||
D[Cha4,Dap8]VP | Drug Info | [528674] | |||
D[Cha4,Lys8]VP | Drug Info | [528674] | |||
D[Cha4,Orn8]VP | Drug Info | [528674] | |||
D[Cha4]AVP | Drug Info | [528674] | |||
D[Leu4,Dab8]VP | Drug Info | [528674] | |||
D[Leu4,Dap8]VP | Drug Info | [528674] | |||
D[Leu4,Lys8]VP | Drug Info | [528674] | |||
D[Leu4,Orn8]VP | Drug Info | [528674] | |||
D[Leu4]AVP | Drug Info | [528674] | |||
D[Lys8(5/6-Flu)]VT | Drug Info | [526347] | |||
D[Orn4,Lys8]VP | Drug Info | [528674] | |||
D[Orn4,Orn8]VP | Drug Info | [528674] | |||
D[Orn4]AVP | Drug Info | [528674] | |||
D[Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Thr4,Lys8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Val4]AVP | Drug Info | [528674] | |||
L-371257 | Drug Info | [530975] | |||
L-372662 | Drug Info | [530975] | |||
PF-3274167 | Drug Info | [530975] | |||
SR-149415 | Drug Info | [530420] | |||
[Aib7]OT | Drug Info | [528693] | |||
[D-Tic7]OT | Drug Info | [528693] | |||
[Gly(But)7]OT | Drug Info | [528693] | |||
[HO1][Lys8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[HO1][Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[HO1][Orn8(5/6C-Rhm)]VT | Drug Info | [526347] | |||
[HO1][Thr4,Lys8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[HO1][Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[L-Tic7]OT | Drug Info | [528693] | |||
[Lys8(Alexa 488) ]PVA | Drug Info | [529036] | |||
[Lys8(Alexa 546) ]PVA | Drug Info | [529036] | |||
[Mpa1, D-Tic2, Aib7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tic7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, Aib7, D-Tic9]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, Aib7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, D-Tic7, Aib9]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, D-Tic7, D-Tic9]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, D-Tic7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, Gly(But)3, Gly(But)7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, Gly(But)7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, L-Tic7]OT | Drug Info | [528693] | |||
[Mpa1, D-Tyr(Et)2, Pip7]OT | Drug Info | [528693] | |||
[Mpa1, L-Tic7]OT | Drug Info | [528693] | |||
[Pip7]OT | Drug Info | [528693] | |||
Antagonist | AS-602305 | Drug Info | [550592] | ||
Barusiban | Drug Info | [530031] | |||
compound 37 | Drug Info | [527824] | |||
d(CH2)5[Tyr(Me)2]AVP | Drug Info | [533590] | |||
GSK-557296 | Drug Info | [532286] | |||
GSK221149 | Drug Info | [550963] | |||
L-365,209 | Drug Info | [533590] | |||
L-366,509 | Drug Info | [533590] | |||
L-366,682 | Drug Info | [533590] | |||
L-366,948 | Drug Info | [533590] | |||
L-367,773 | Drug Info | [533590] | |||
L-368899 | Drug Info | [534480] | |||
L023103 | Drug Info | [527891] | |||
LS-192629 | Drug Info | [526585] | |||
PF-271836 | Drug Info | [543799] | |||
SSR126768A | Drug Info | [526928] | |||
TT-235 | Drug Info | [527375], [551871] | |||
[35S]-non-peptide OT antagonist | Drug Info | [526401] | |||
Agonist | Carbetocin | Drug Info | [535799], [536790], [537867] | ||
dAVP | Drug Info | [527042] | |||
FE-202767 | Drug Info | [543799] | |||
[3H]OT (human, mouse, rat) | Drug Info | [533541] | |||
[Phe3]OT | Drug Info | [534289] | |||
[Thr4,Gly7]OT | Drug Info | [533355] | |||
Modulator | Oxytocin | Drug Info | [543799] | ||
Retosiban | Drug Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
cAMP signaling pathway | |||||
Neuroactive ligand-receptor interaction | |||||
Oxytocin signaling pathway | |||||
NetPath Pathway | TGF_beta_Receptor Signaling Pathway | ||||
PANTHER Pathway | Oxytocin receptor mediated signaling pathway | ||||
Reactome | Vasopressin-like receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Myometrial Relaxation and Contraction Pathways | |||||
Oxytocin signaling | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 521712 | ClinicalTrials.gov (NCT00209326) A Proof of Concept Study Assessing the Effect of Four Different Single Bolus Intravenous Doses of FE200440 and Placebo on Stopping Preterm Labor. U.S. National Institutes of Health. | ||||
Ref 522869 | ClinicalTrials.gov (NCT01021553) A Study To Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Two Oral Doses of GSK557296 in a Study in Men With Premature Ejaculation. U.S. National Institutes of Health. | ||||
Ref 524034 | ClinicalTrials.gov (NCT01673399) Oxytocin Antagonist in Patients With Repeated Failure of Implantation. U.S. National Institutes of Health. | ||||
Ref 525102 | ClinicalTrials.gov (NCT02377466) A Phase III Efficacy and Safety Study of Intravenous Retosiban Versus Placebo for Women in Spontaneous Preterm Labor. U.S. National Institutes of Health. | ||||
Ref 539377 | (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: 2174). | ||||
Ref 539407 | (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: 2213). | ||||
Ref 539423 | (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: 2249). | ||||
Ref 539425 | (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: 2252). | ||||
Ref 543110 | (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: 8403). | ||||
Ref 546463 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008273) | ||||
Ref 546833 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010521) | ||||
Ref 546859 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010692) | ||||
Ref 547962 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020775) | ||||
Ref 526347 | J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. | ||||
Ref 526401 | A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors. Eur J Pharmacol. 2002 Aug 16;450(1):19-28. | ||||
Ref 526585 | Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor. J Pharmacol Exp Ther. 2003 Jul;306(1):253-61. Epub 2003 Mar 26. | ||||
Ref 526928 | SSR126768A (4-chloro-3-[(3R)-(+)-5-chloro-1-(2,4-dimethoxybenzyl)-3-methyl-2-oxo-2,3-dihydro-1H-indol-3-yl]-N-ethyl-N-(3-pyridylmethyl)-benzamide, hydrochloride): a new selective and orally active oxytocin receptor antagonist for the prevention of preterm labor. J Pharmacol Exp Ther. 2004 Apr;309(1):414-24. Epub 2004 Jan 13. | ||||
Ref 527042 | Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88. | ||||
Ref 527375 | In vivo activity of the potent oxytocin antagonist on uterine activity in the rat. In Vivo. 2004 Nov-Dec;18(6):763-6. | ||||
Ref 527824 | 2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics. J Med Chem. 2005 Nov 3;48(22):6956-69. | ||||
Ref 527874 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9. Epub 2005 Nov 15.Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. | ||||
Ref 527891 | Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists. J Med Chem. 2005 Dec 1;48(24):7882-905. | ||||
Ref 528674 | J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8. | ||||
Ref 528693 | Eur J Med Chem. 2007 Jun;42(6):799-806. Epub 2007 Jan 10.Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7. | ||||
Ref 529036 | J Med Chem. 2007 Oct 4;50(20):4976-85. Epub 2007 Sep 12.Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. | ||||
Ref 530031 | The effect of barusiban, a selective oxytocin antagonist, in threatened preterm labor at late gestational age: a randomized, double-blind, placebo-controlled trial. Am J Obstet Gynecol. 2009 Jun;200(6):627.e1-10. | ||||
Ref 530420 | Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. | ||||
Ref 532286 | Inhibition of ejaculation by the non-peptide oxytocin receptor antagonist GSK557296: a multi-level site of action. Br J Pharmacol. 2013 Aug;169(7):1477-85. | ||||
Ref 533355 | [3H]-[Thr4,Gly7]OT: a highly selective ligand for central and peripheral OT receptors. Am J Physiol. 1988 Jan;254(1 Pt 1):E31-8. | ||||
Ref 533541 | Oxytocin receptors and human parturition: a dual role for oxytocin in the initiation of labor. Science. 1982 Mar 12;215(4538):1396-8. | ||||
Ref 533590 | Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells. Life Sci. 1995;57(24):2253-61. | ||||
Ref 534289 | Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin. FEBS Lett. 1996 Nov 18;397(2-3):201-6. | ||||
Ref 534480 | Pharmacokinetics and disposition of the oxytocin receptor antagonist L-368,899 in rats and dogs. Drug Metab Dispos. 1997 Oct;25(10):1113-8. | ||||
Ref 535799 | Structure and expression of a human oxytocin receptor. Nature. 1992 Apr 9;356(6369):526-9. | ||||
Ref 536790 | Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res. 2008;170:473-512. | ||||
Ref 537867 | Structural organization of the human oxytocin receptor gene. J Biol Chem. 1994 Dec 23;269(51):32451-6. |
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