Target Information
Target General Information | Top | |||||
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Target ID |
T66237
(Former ID: TTDS00111)
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Target Name |
Vasopressin V2 receptor (V2R)
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Synonyms |
Renal-type arginine vasopressin receptor; DIR3; DIR; Antidiuretic hormone receptor; AVPR V2; ADHR
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Gene Name |
AVPR2
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 6 Target-related Diseases | + | ||||
1 | Acute diabete complication [ICD-11: 5A2Y] | |||||
2 | Autism spectrum disorder [ICD-11: 6A02] | |||||
3 | Enuresis [ICD-11: 6C00] | |||||
4 | Hypo-osmolality/hyponatraemia [ICD-11: 5C72] | |||||
5 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
6 | Polyuria [ICD-11: MF55] | |||||
Function |
The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Involved in renal water reabsorption. Receptor for arginine vasopressin.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLA
ALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQM VGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQ RNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGP SERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEA PLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTT ASSSLAKDTSS Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
1 | Conivaptan | Drug Info | Approved | Euvolemic hyponatremia | [2], [3] | |
2 | Desmopressin | Drug Info | Approved | Diabetic complication | [4], [5], [6] | |
3 | Mozavaptan | Drug Info | Approved | Hyponatraemia | [5], [7], [8] | |
4 | Oxytocin | Drug Info | Approved | Autism spectrum disorder | [9] | |
5 | Tolvaptan | Drug Info | Approved | Hyponatraemia | [10], [11] | |
6 | Vasopressin | Drug Info | Approved | Diabetes insipidus | [12], [13] | |
Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
1 | Lixivaptan | Drug Info | Phase 3 | Hyponatraemia | [14], [15] | |
2 | Satavaptan | Drug Info | Phase 3 | Acute and chronic heart failure | [16], [17] | |
3 | ASP-7035 | Drug Info | Phase 2 | Nocturia | [18] | |
4 | SPD-556 | Drug Info | Phase 2 | Heart failure | [19] | |
5 | SSR149415 | Drug Info | Phase 2 | Anxiety disorder | [20], [21], [22] | |
6 | VA-106483 | Drug Info | Phase 2 | Nocturia | [23] | |
Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
1 | OPC-51803 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [24], [25] | |
2 | OX 19 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [26] | |
3 | VNA-932 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [27], [28] | |
4 | JTV-605 | Drug Info | Terminated | Dysmenorrhea | [29] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Modulator | [+] 1 Modulator drugs | + | ||||
1 | Conivaptan | Drug Info | [30], [31] | |||
Agonist | [+] 9 Agonist drugs | + | ||||
1 | Desmopressin | Drug Info | [32], [33], [34], [35], [36] | |||
2 | Oxytocin | Drug Info | [41] | |||
3 | Vasopressin | Drug Info | [1] | |||
4 | ASP-7035 | Drug Info | [45] | |||
5 | OPC-51803 | Drug Info | [48] | |||
6 | OX 19 | Drug Info | [49] | |||
7 | VNA-932 | Drug Info | [50], [5] | |||
8 | [Phe3]OT | Drug Info | [58] | |||
9 | [Val4]AVP | Drug Info | [59] | |||
Inhibitor | [+] 28 Inhibitor drugs | + | ||||
1 | Mozavaptan | Drug Info | [37], [38], [39], [40] | |||
2 | ATOSIBAN | Drug Info | [43] | |||
3 | SSR149415 | Drug Info | [46] | |||
4 | VA-106483 | Drug Info | [47] | |||
5 | ARGENINE VASOPRESSIN | Drug Info | [51] | |||
6 | D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT | Drug Info | [53] | |||
7 | DVDAVP | Drug Info | [51] | |||
8 | D[Arg4,Dab8]VP | Drug Info | [51] | |||
9 | D[Arg4,Lys8]VP | Drug Info | [51] | |||
10 | D[Arg4,Orn8]VP | Drug Info | [51] | |||
11 | D[Arg4]AVP | Drug Info | [51] | |||
12 | D[Cha4,Dab8]VP | Drug Info | [51] | |||
13 | D[Cha4,Dap8]VP | Drug Info | [51] | |||
14 | D[Cha4,Lys8]VP | Drug Info | [51] | |||
15 | D[Cha4,Orn8]VP | Drug Info | [51] | |||
16 | D[Cha4]AVP | Drug Info | [51] | |||
17 | D[D-3-Pal2]AVP | Drug Info | [51] | |||
18 | D[Leu4,Dab8]VP | Drug Info | [51] | |||
19 | D[Leu4,Dap8]VP | Drug Info | [51] | |||
20 | D[Leu4,Lys8]VP | Drug Info | [51] | |||
21 | D[Leu4,Orn8]VP | Drug Info | [51] | |||
22 | D[Leu4]AVP | Drug Info | [51] | |||
23 | D[Orn4,Lys8]VP | Drug Info | [51] | |||
24 | D[Orn4,Orn8]VP | Drug Info | [51] | |||
25 | D[Orn4]AVP | Drug Info | [51] | |||
26 | D[Val4]AVP | Drug Info | [51] | |||
27 | L-372662 | Drug Info | [54] | |||
28 | YM-35278 | Drug Info | [57] | |||
Antagonist | [+] 13 Antagonist drugs | + | ||||
1 | Tolvaptan | Drug Info | [42], [11] | |||
2 | Lixivaptan | Drug Info | [44] | |||
3 | Satavaptan | Drug Info | [17], [39], [33] | |||
4 | SPD-556 | Drug Info | [41] | |||
5 | JTV-605 | Drug Info | [37] | |||
6 | CL-385004 | Drug Info | [37] | |||
7 | d(CH2)5[D-Ile2,Ile4]AVP | Drug Info | [52] | |||
8 | d(CH2)5[Tyr(Me)2]AVP | Drug Info | [52] | |||
9 | d[Pen1,Tyr(Me)2]AVP | Drug Info | [52] | |||
10 | FR161282 | Drug Info | [37] | |||
11 | VP-343 | Drug Info | [37] | |||
12 | YM 218 | Drug Info | [55] | |||
13 | YM 471 | Drug Info | [56] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
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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
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KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Phospholipase D signaling pathway | hsa04072 | Affiliated Target |
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Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Vasopressin-regulated water reabsorption | hsa04962 | Affiliated Target |
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Class: Organismal Systems => Excretory system | Pathway Hierarchy |
Degree | 5 | Degree centrality | 5.37E-04 | Betweenness centrality | 3.84E-04 |
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Closeness centrality | 2.07E-01 | Radiality | 1.36E+01 | Clustering coefficient | 2.00E-01 |
Neighborhood connectivity | 2.46E+01 | Topological coefficient | 2.78E-01 | Eccentricity | 12 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"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 | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
2 | Vasopressin-regulated water reabsorption | |||||
Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
1 | Vasopressin Regulation of Water Homeostasis | |||||
PID Pathway | [+] 1 PID Pathways | + | ||||
1 | Arf6 trafficking events | |||||
Reactome | [+] 3 Reactome Pathways | + | ||||
1 | Vasopressin-like receptors | |||||
2 | G alpha (s) signalling events | |||||
3 | Vasopressin regulates renal water homeostasis via Aquaporins | |||||
WikiPathways | [+] 5 WikiPathways | + | ||||
1 | GPCRs, Class A Rhodopsin-like | |||||
2 | Regulation of Water Balance by Renal Aquaporins | |||||
3 | Peptide GPCRs | |||||
4 | GPCR ligand binding | |||||
5 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Vasopressin receptors: structure/function relationships and signal transduction in target cells. J Soc Biol. 2005;199(4):351-9. | |||||
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: 2203). | |||||
REF 3 | Emerging diuretics for the treatment of heart failure. Expert Opin Emerg Drugs. 2009 Mar;14(1):195-204. | |||||
REF 4 | 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 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 6 | ClinicalTrials.gov (NCT00748072) 1-deamino 8-d-arginine Vasopressin (DDAVP) in Percutaneous Ultrasound-guided Renal Biopsy. U.S. National Institutes of Health. | |||||
REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001739) | |||||
REF 8 | 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: 2197). | |||||
REF 9 | 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 10 | 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: 2226). | |||||
REF 11 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | |||||
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: 2168). | |||||
REF 13 | New topics in vasopressin receptors and approach to novel drugs: research and development of conivaptan hydrochloride (YM087), a drug for the treatment of hyponatremia. J Pharmacol Sci. 2009 Jan;109(1):53-9. | |||||
REF 14 | 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: 2238). | |||||
REF 15 | Physical state of kappa-carrageenan modulates the mode of action of kappa-carrageenase from Pseudoalteromonas carrageenovora. Biochem J. 2009 May 1;419(3):545-53. | |||||
REF 16 | 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: 2199). | |||||
REF 17 | Post-translational import of protein into the endoplasmic reticulum of a trypanosome: an in vitro system for discovery of anti-trypanosomal chemical entities. Biochem J. 2009 Apr 15;419(2):507-17. | |||||
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 800030285) | |||||
REF 19 | ClinicalTrials.gov (NCT01179607) Study of Efficacy of a Vasopressin 2 Receptor Antagonist M0002 for Treatment of Ascites in Cirrhotic Subjects With Hypo- or Normonatraemia. U.S. National Institutes of Health. | |||||
REF 20 | 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 21 | 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 22 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
REF 23 | ClinicalTrials.gov (NCT01038843) Efficacy Study of VA106483 in Males With Nocturia.. U.S. National Institutes of Health. | |||||
REF 24 | 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: 2173). | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010599) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021110) | |||||
REF 27 | 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: 3537). | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013621) | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010443) | |||||
REF 30 | Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation. 2001 Nov 13;104(20):2417-23. | |||||
REF 31 | Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79. | |||||
REF 32 | 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 33 | Vasopressin-induced von Willebrand factor secretion from endothelial cells involves V2 receptors and cAMP. J Clin Invest. 2000 Jul;106(1):107-16. | |||||
REF 34 | The abnormal quinine drinking aversion in the Brattleboro rat with diabetes insipidus is reversed by the vasopressin agonist DDAVP: a possible role for vasopressin in the motivation to drink. PhysiolBehav. 1994 Mar;55(3):407-12. | |||||
REF 35 | Hydronephrosis: prevention by restoration of urinary concentrating ability using desamino-8D-arginine vasopressin (DDAVP) in Brattleboro rats. Int J Exp Pathol. 1991 Oct;72(5):581-7. | |||||
REF 36 | An extracellular residue determines the agonist specificity of V2 vasopressin receptors. FEBS Lett. 1995 Mar 27;362(1):19-23. | |||||
REF 37 | Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Prog Brain Res. 2002;139:197-210. | |||||
REF 38 | Effects of an oral vasopressin receptor antagonist (OPC-31260) in a dog with syndrome of inappropriate secretion of antidiuretic hormone. Aust Vet J. 2000 Dec;78(12):825-30. | |||||
REF 39 | Nonpeptide vasopressin antagonists: a new group of hormone blockers entering the scene. Exp Clin Endocrinol Diabetes. 1999;107(3):157-65. | |||||
REF 40 | New analgesic drugs derived from phencyclidine. J Med Chem. 1981 May;24(5):496-9. | |||||
REF 41 | 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: 368). | |||||
REF 42 | Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor. Biochem J. 2009 May 1;419(3):577-84. | |||||
REF 43 | The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. | |||||
REF 44 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | |||||
REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030285) | |||||
REF 46 | Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. | |||||
REF 47 | New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. J Med Chem. 2008 Dec 25;51(24):8124-34. | |||||
REF 48 | Effects of OPC-51803, a novel, nonpeptide vasopressin V2-receptor agonist, on micturition frequency in Brattleboro and aged rats. J Pharmacol Sci. 2003 Dec;93(4):484-8. | |||||
REF 49 | Investigation of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors: molecular dynamics simulation of the agonist-bound state in the membrane-aqueous system. Biopolymers. 2006 Apr 5;81(5):321-38. | |||||
REF 50 | Biased Agonist Pharmacochaperones of the AVP V2 Receptor May Treat Congenital Nephrogenic Diabetes Insipidus. J Am Soc Nephrol. 2009 October; 20(10): 2190-2203. | |||||
REF 51 | 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 52 | Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463. Kidney Int. 2000 Oct;58(4):1613-22. | |||||
REF 53 | 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 54 | Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38. | |||||
REF 55 | Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res. 2005 Mar;51(3):275-81. | |||||
REF 56 | Effects of YM471, a nonpeptide AVP V(1A) and V(2) receptor antagonist, on human AVP receptor subtypes expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells. Br J Pharmacol. 2001 Jul;133(5):746-54. | |||||
REF 57 | Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists. Bioorg Med Chem. 2008 Nov 1;16(21):9524-35. | |||||
REF 58 | Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J. 1995 May 15;14(10):2176-82. | |||||
REF 59 | [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology. 2002 Dec;143(12):4655-64. |
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