Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T84486
(Former ID: TTDS00264)
|
|||||
| Target Name |
Oxytocin receptor (OTR)
|
|||||
| Synonyms |
OT-R
Click to Show/Hide
|
|||||
| Gene Name |
OXTR
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Acute diabete complication [ICD-11: 5A2Y] | |||||
| 2 | Autism spectrum disorder [ICD-11: 6A02] | |||||
| 3 | Postpartum haemorrhage [ICD-11: JA43] | |||||
| Function |
The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. Receptor for oxytocin.
Click to Show/Hide
|
|||||
| BioChemical Class |
GPCR rhodopsin
|
|||||
| UniProt ID | ||||||
| Sequence |
MEGALAANWSAEAANASAAPPGAEGNRTAGPPRRNEALARVEVAVLCLILLLALSGNACV
LLALRTTRQKHSRLFFFMKHLSIADLVVAVFQVLPQLLWDITFRFYGPDLLCRLVKYLQV VGMFASTYLLLLMSLDRCLAICQPLRSLRRRTDRLAVLATWLGCLVASAPQVHIFSLREV ADGVFDCWAVFIQPWGPKAYITWITLAVYIVPVIVLAACYGLISFKIWQNLRLKTAAAAA AEAPEGAAAGDGGRVALARVSSVKLISKAKIRTVKMTFIIVLAFIVCWTPFFFVQMWSVW DANAPKEASAFIIVMLLASLNSCCNPWIYMLFTGHLFHELVQRFLCCSASYLKGRRLGET SASKKSNSSSFVLSHRSSSQRSCSQPSTA Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A01759 ; BADD_A05900 | |||||
| HIT2.0 ID | T76GZS | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Carbetocin | Drug Info | Approved | Postpartum haemorrhage | [5] | |
| 2 | Oxytocin | Drug Info | Approved | Autism spectrum disorder | [6] | |
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | Retosiban | Drug Info | Phase 3 | Preterm labour | [7], [8] | |
| 2 | Barusiban | Drug Info | Phase 2 | Androgen deficiency | [9] | |
| 3 | FE-202767 | Drug Info | Phase 2 | Erectile dysfunction | [10] | |
| 4 | GSK-557296 | Drug Info | Phase 2 | Premature ejaculation | [11] | |
| 5 | SSR149415 | Drug Info | Phase 2 | Anxiety disorder | [12], [13], [14] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | L-368899 | Drug Info | Discontinued in Phase 1 | Miscarriage | [15], [16] | |
| 2 | PF-3274167 | Drug Info | Discontinued in Phase 1 | Female sexual arousal dysfunction | [17] | |
| 3 | TT-235 | Drug Info | Discontinued in Phase 1 | Miscarriage | [18] | |
| 4 | AS-602305 | Drug Info | Terminated | Androgen deficiency | [19] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 3 Agonist drugs | + | ||||
| 1 | Carbetocin | Drug Info | [1], [20], [21] | |||
| 2 | FE-202767 | Drug Info | [22] | |||
| 3 | [Thr4,Gly7]OT | Drug Info | [44] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Oxytocin | Drug Info | [22], [23] | |||
| 2 | Retosiban | Drug Info | [25] | |||
| Inhibitor | [+] 46 Inhibitor drugs | + | ||||
| 1 | ATOSIBAN | Drug Info | [24] | |||
| 2 | SSR149415 | Drug Info | [28] | |||
| 3 | PF-3274167 | Drug Info | [31] | |||
| 4 | L-371257 | Drug Info | [31] | |||
| 5 | ARGENINE VASOPRESSIN | Drug Info | [34] | |||
| 6 | D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT | Drug Info | [35] | |||
| 7 | DesGly-NH2,d(CH2)5[D-Tyr2,Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 8 | D[Arg4,Lys8]VP | Drug Info | [34] | |||
| 9 | D[Arg4,Orn8]VP | Drug Info | [34] | |||
| 10 | D[Arg4]AVP | Drug Info | [34] | |||
| 11 | D[Cha4,Dab8]VP | Drug Info | [34] | |||
| 12 | D[Cha4,Dap8]VP | Drug Info | [34] | |||
| 13 | D[Cha4,Lys8]VP | Drug Info | [34] | |||
| 14 | D[Cha4,Orn8]VP | Drug Info | [34] | |||
| 15 | D[Cha4]AVP | Drug Info | [34] | |||
| 16 | D[Leu4,Dab8]VP | Drug Info | [34] | |||
| 17 | D[Leu4,Dap8]VP | Drug Info | [34] | |||
| 18 | D[Leu4,Lys8]VP | Drug Info | [34] | |||
| 19 | D[Leu4]AVP | Drug Info | [34] | |||
| 20 | D[Lys8(5/6-Flu)]VT | Drug Info | [35] | |||
| 21 | D[Orn4,Lys8]VP | Drug Info | [34] | |||
| 22 | D[Orn8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 23 | D[Thr4,Lys8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 24 | D[Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 25 | L-372662 | Drug Info | [31] | |||
| 26 | [Aib7]OT | Drug Info | [42] | |||
| 27 | [D-Tic7]OT | Drug Info | [42] | |||
| 28 | [Gly(But)7]OT | Drug Info | [42] | |||
| 29 | [HO1][Lys8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 30 | [HO1][Orn8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 31 | [HO1][Orn8(5/6C-Rhm)]VT | Drug Info | [35] | |||
| 32 | [HO1][Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [35] | |||
| 33 | [L-Tic7]OT | Drug Info | [42] | |||
| 34 | [Lys8(Alexa 488) ]PVA | Drug Info | [43] | |||
| 35 | [Lys8(Alexa 546) ]PVA | Drug Info | [43] | |||
| 36 | [Mpa1, D-Tic7]OT | Drug Info | [42] | |||
| 37 | [Mpa1, D-Tyr(Et)2, Aib7, D-Tic9]OT | Drug Info | [42] | |||
| 38 | [Mpa1, D-Tyr(Et)2, Aib7]OT | Drug Info | [42] | |||
| 39 | [Mpa1, D-Tyr(Et)2, D-Tic7, D-Tic9]OT | Drug Info | [42] | |||
| 40 | [Mpa1, D-Tyr(Et)2, D-Tic7]OT | Drug Info | [42] | |||
| 41 | [Mpa1, D-Tyr(Et)2, Gly(But)3, Gly(But)7]OT | Drug Info | [42] | |||
| 42 | [Mpa1, D-Tyr(Et)2, Gly(But)7]OT | Drug Info | [42] | |||
| 43 | [Mpa1, D-Tyr(Et)2, L-Tic7]OT | Drug Info | [42] | |||
| 44 | [Mpa1, D-Tyr(Et)2, Pip7]OT | Drug Info | [42] | |||
| 45 | [Mpa1, L-Tic7]OT | Drug Info | [42] | |||
| 46 | [Pip7]OT | Drug Info | [42] | |||
| Antagonist | [+] 27 Antagonist drugs | + | ||||
| 1 | Barusiban | Drug Info | [26] | |||
| 2 | GSK-557296 | Drug Info | [27] | |||
| 3 | PMID28906174-Compound-figure1g | Drug Info | [29] | |||
| 4 | Pyrrolidine derivative 10 | Drug Info | [29] | |||
| 5 | Pyrrolidine derivative 11 | Drug Info | [29] | |||
| 6 | Pyrrolidine derivative 12 | Drug Info | [29] | |||
| 7 | Pyrrolidine derivative 13 | Drug Info | [29] | |||
| 8 | Pyrrolidine derivative 9 | Drug Info | [29] | |||
| 9 | Triazole derivative 4 | Drug Info | [29] | |||
| 10 | Triazole derivative 5 | Drug Info | [29] | |||
| 11 | Triazole derivative 6 | Drug Info | [29] | |||
| 12 | Triazole derivative 7 | Drug Info | [29] | |||
| 13 | L-368899 | Drug Info | [30] | |||
| 14 | TT-235 | Drug Info | [32], [3] | |||
| 15 | AS-602305 | Drug Info | [33] | |||
| 16 | d(CH2)5[Tyr(Me)2]AVP | Drug Info | [36] | |||
| 17 | L-365,209 | Drug Info | [36] | |||
| 18 | L-366,509 | Drug Info | [36] | |||
| 19 | L-366,682 | Drug Info | [36] | |||
| 20 | L-366,948 | Drug Info | [36] | |||
| 21 | L-367,773 | Drug Info | [36] | |||
| 22 | L023103 | Drug Info | [37] | |||
| 23 | LS-192629 | Drug Info | [38] | |||
| 24 | PF-271836 | Drug Info | [22] | |||
| 25 | PMID16250654C37 | Drug Info | [39] | |||
| 26 | SSR126768A | Drug Info | [40] | |||
| 27 | [35S]-non-peptide OT antagonist | Drug Info | [41] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Retosiban | Ligand Info | |||||
| Structure Description | Crystal structure of the human oxytocin receptor | PDB:6TPK | ||||
| Method | X-ray diffraction | Resolution | 3.20 Å | Mutation | No | [45] |
| PDB Sequence |
NEALARVEVA
44 VLCLILLLAL54 SGNACVLLAL64 HHSRLFFFMK79 HLSIADLVVA89 VFQVLPQLLW 99 DITFRFYGPD109 LLCRLVKYLQ119 LVGMFASTYL129 LLLMSLDRCL139 AICQPLRSLR 149 RRTARLAVLA159 TWLGCLVVSA169 PQVHIFSLRE179 VADGVFDCWA189 VFIRPWGPKA 199 YITWITLAVY209 IVPVIVLATC219 YGLIAFKIWQ229 NLISKAKIRT273 VKMTFIIVLA 283 FIVCWTPFFF293 VQMWSVWDAN303 APKEASAFII313 VMLLASLNCC323 CKPWIYMLFM 333 GHLFHGIDSF344 WNESYLTGSR356 DERKKSLLSK366 FGMDEGVTFM376 FIGRFDRGQK 386 GVDVLLKAIE396 ILSSKKEFQE406 MRFIIIGKGD416 PELEGWARSL426 EEKHGNVKVI 436 TEMLSREFVR446 ELYGSVDFVI456 IPSYFEPFGL466 VALEAMCLGA476 IPIASAVGGL 486 RDIITNETGI496 LVKAGDPGEL506 ANAILKALEL516 SRSDLSKFRE526 NCKKRAMSFS 536
|
|||||
|
|
VAL88
4.251
GLN92
3.250
GLN96
4.382
LYS116
3.423
GLN119
3.458
LEU120
4.814
MET123
3.603
GLN171
2.439
PHE175
3.768
TRP188
4.934
PHE191
4.971
|
|||||
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Crystal structure of the human oxytocin receptor | PDB:6TPK | ||||
| Method | X-ray diffraction | Resolution | 3.20 Å | Mutation | No | [45] |
| PDB Sequence |
NEALARVEVA
44 VLCLILLLAL54 SGNACVLLAL64 HHSRLFFFMK79 HLSIADLVVA89 VFQVLPQLLW 99 DITFRFYGPD109 LLCRLVKYLQ119 LVGMFASTYL129 LLLMSLDRCL139 AICQPLRSLR 149 RRTARLAVLA159 TWLGCLVVSA169 PQVHIFSLRE179 VADGVFDCWA189 VFIRPWGPKA 199 YITWITLAVY209 IVPVIVLATC219 YGLIAFKIWQ229 NLISKAKIRT273 VKMTFIIVLA 283 FIVCWTPFFF293 VQMWSVWDAN303 APKEASAFII313 VMLLASLNCC323 CKPWIYMLFM 333 GHLFHGIDSF344 WNESYLTGSR356 DERKKSLLSK366 FGMDEGVTFM376 FIGRFDRGQK 386 GVDVLLKAIE396 ILSSKKEFQE406 MRFIIIGKGD416 PELEGWARSL426 EEKHGNVKVI 436 TEMLSREFVR446 ELYGSVDFVI456 IPSYFEPFGL466 VALEAMCLGA476 IPIASAVGGL 486 RDIITNETGI496 LVKAGDPGEL506 ANAILKALEL516 SRSDLSKFRE526 NCKKRAMSFS 536
|
|||||
|
|
||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
|
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Calcium signaling pathway | hsa04020 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| cAMP signaling pathway | hsa04024 | Affiliated Target |
|
| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Oxytocin signaling pathway | hsa04921 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Degree | 3 | Degree centrality | 3.22E-04 | Betweenness centrality | 2.38E-04 |
|---|---|---|---|---|---|
| Closeness centrality | 1.89E-01 | Radiality | 1.32E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 2.13E+01 | Topological coefficient | 3.45E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | cAMP signaling pathway | |||||
| 3 | Neuroactive ligand-receptor interaction | |||||
| 4 | Oxytocin signaling pathway | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | TGF_beta_Receptor Signaling Pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Oxytocin receptor mediated signaling pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Vasopressin-like receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| WikiPathways | [+] 7 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Myometrial Relaxation and Contraction Pathways | |||||
| 3 | Oxytocin signaling | |||||
| 4 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 5 | Peptide GPCRs | |||||
| 6 | GPCR ligand binding | |||||
| 7 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | 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 2 | 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: 2182). | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | ClinicalTrials.gov (NCT00748072) 1-deamino 8-d-arginine Vasopressin (DDAVP) in Percutaneous Ultrasound-guided Renal Biopsy. U.S. National Institutes of Health. | |||||
| REF 5 | Clinical Textbook of Dental Hygiene and Therapy. 2006, P237. By Robert Ireland. | |||||
| REF 6 | 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: 2174). | |||||
| REF 7 | 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: 8403). | |||||
| REF 8 | 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 9 | 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 10 | ClinicalTrials.gov (NCT02545127) Trial Exploring the Efficacy and Safety of FE 202767. | |||||
| REF 11 | 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 12 | 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: 2202). | |||||
| REF 13 | Anxiolytic- and antidepressant-like effects of the non-peptide vasopressin V1b receptor antagonist, SSR149415, suggest an innovative approach for t... Proc Natl Acad Sci U S A. 2002 Apr 30;99(9):6370-5. | |||||
| REF 14 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
| REF 15 | 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: 2249). | |||||
| REF 16 | 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 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025596) | |||||
| REF 18 | 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 19 | 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 20 | Structural organization of the human oxytocin receptor gene. J Biol Chem. 1994 Dec 23;269(51):32451-6. | |||||
| REF 21 | Structure and expression of a human oxytocin receptor. Nature. 1992 Apr 9;356(6369):526-9. | |||||
| REF 22 | 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: 369). | |||||
| REF 23 | Oxytocin receptors and human parturition: a dual role for oxytocin in the initiation of labor. Science. 1982 Mar 12;215(4538):1396-8. | |||||
| REF 24 | Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9. | |||||
| REF 25 | The Effect of an Oxytocin Receptor Antagonist (Retosiban, GSK221149A) on the Response of Human Myometrial Explants to Prolonged Mechanical Stretch.Endocrinology.2015 Oct;156(10):3511-6. | |||||
| REF 26 | 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 27 | 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 28 | Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. | |||||
| REF 29 | A patent review of oxytocin receptor antagonists 2013-2017.Expert Opin Ther Pat. 2017 Dec;27(12):1287-1290. | |||||
| REF 30 | 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 31 | Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38. | |||||
| REF 32 | In vivo activity of the potent oxytocin antagonist on uterine activity in the rat. In Vivo. 2004 Nov-Dec;18(6):763-6. | |||||
| REF 33 | Clinical pipeline report, company report or official report of darkpharma. | |||||
| REF 34 | Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasop... J Med Chem. 2007 Feb 22;50(4):835-47. | |||||
| REF 35 | Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. J Med Chem. 2002 Jun 6;45(12):2579-88. | |||||
| REF 36 | Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells. Life Sci. 1995;57(24):2253-61. | |||||
| REF 37 | 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 38 | Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a ... J Pharmacol Exp Ther. 2003 Jul;306(1):253-61. | |||||
| REF 39 | 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 40 | 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, ... J Pharmacol Exp Ther. 2004 Apr;309(1):414-24. | |||||
| REF 41 | A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors. Eur J Pharmacol. 2002 Aug 16;450(1):19-28. | |||||
| REF 42 | Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7. Eur J Med Chem. 2007 Jun;42(6):799-806. | |||||
| REF 43 | Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. J Med Chem. 2007 Oct 4;50(20):4976-85. | |||||
| REF 44 | [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 45 | Crystal structure of the human oxytocin receptor. Sci Adv. 2020 Jul 15;6(29):eabb5419. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.