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Showing drug card for Vasopressin (DB00067)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-05-26 19:20:55
Primary Accession Number DB00067
Secondary Accession Number
  • BIOD00110
  • BTD00110
Name Vasopressin
Drug Type
  • Approved
  • Biotech
Description Antidiuretic hormone, also known as vasopressin, is a nine amino acid peptide secreted from the posterior pituitary. Antidiuretic hormone binds to receptors in the distal or collecting tubules of the kidney and promotes reabsorbtion of water back into the circulation
Synonyms
  1. 3-Isoleucyl vasopressin
  2. Arginine oxytocin
  3. Arginine vasotocin
  4. Argiprestocin
  5. Pitressin tannate
  6. Vasopressin, isoleucyl
  7. Vasopressin, non-mammalian
  8. Vasotocin
Brand Names
  1. Pitressin
  2. Pressyn
Brand Mixtures Not Available
Chemical IUPAC Name 1-[19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-butan-2-yl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pyrrolidine-2-carboxamide
Chemical Formula C43H67N15O12S2
Chemical Structure Structure
Protein Sequence(s) >DE = Vasopressin 
CYFQNCPRG
CAS Registry Number 11000-17-2
InChI Identifier InChI=1/C43H67N15O12S2/c1-3-21(2)34-41(69)53-26(12-13-31(45)60)37(65)55-28(17-32(46)61)38(66)56-29(20-72-71-19-24(44)35(63)54-27(39(67)57-34)16-22-8-10-23(59)11-9-22)42(70)58-15-5-7-30(58)40(68)52-25(6-4-14-50-43(48)49)36(64)51-18-33(47)62/h8-11,21,24-30,34,59H,3-7,12-20,44H2,1-2H3,(H2,45,60)(H2,46,61)(H2,47,62)(H,51,64)(H,52,68)(H,53,69)(H,54,63)(H,55,65)(H,56,66)(H,57,67)(H4,48,49,50)/f/h51-57H,45-49H2
InChI Key OXDZADMCOWPSOC-UPLISBMOCV
KEGG Drug D00101 Link Image
KEGG Compound C00840 Link Image
PubChem Compound 24774 Link Image
PubChem Substance 167533 Link Image
ChEBI ID Not Available
PharmGKB ID PA451858 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 00693820 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/vasopressin.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Vasopressin Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 1050.2150
Monoisotopic Molecular Weight 1049.4535
State Solid
Melting Point Not Available
Experimental Water Solubility Soluble Source: PhysProp
Predicted Water Solubility 2.78e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity -4.9 Source: PhysProp
Predicted LogP -1.66 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -3.58 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CC[C@H](C)[C@H]1NC(=O)[C@@H](CC2=CC=C(O)C=C2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O)C(=O)N1CCC[C@@H]1C(=O)N[C@H](CCC\N=C(/N)N)C(=O)NCC(N)=O
Canonical SMILES CCC(C)C1NC(=O)C(CC2=CC=C(O)C=C2)NC(=O)C(N)CSSCC(NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC1=O)C(=O)N1CCCC1C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O
Drug Category
  • Antidiuretics
  • Oxytocics
  • Vasoconstrictor Agents
ATC Codes
AHFS Codes
  • 68:28.00
Indication For the treatment of enuresis, polyuria, diabetes insipidus, polydipsia and oesophageal varices with bleeding
Pharmacology Vasopressin is an antidiuretic hormone indicated for the prevention and treatment of postoperative abdominal distention, in abdominal roentgenography to dispel interfering gas shadows, and in diabetes insipidus. Vasopressin can cause contraction of smooth muscle of the gastrointestinal tract and of all parts of the vascular bed, especially the capillaries, small arterioles and venules. It has less effect on the smooth musculature of the large veins. Vasopressin may also be used to control bleeding in some forms of von Willebrand disease and to treat extreme cases of bed wetting in children. It may also play a role in memory formation although the mechanism is unknown.
Mechanism of Action Vasopressin acts on three different receptors, vasopressin receptor V1a (which initiates vasoconstriction, liver gluconeogenesis, platelet aggregation and release of factor VIII), vasopressin receptor V1b (which mediates corticotrophin secretion from the pituitary) and vasopressin receptor V2 which controls free water reabsorption in the renal medullar. The binding of vasopressin to the V2 receptor activates adenylate cyclase which causes the release of aquaporin 2 channels into the cells lining the renal medullar duct. This allows water to be reabsorbed down an osmotic gradient so the urine is more concentrated.
Absorption Not Available
Toxicity Not Available
Protein Binding 1%
Biotransformation The majority of a dose of vasopressin is metabolized and rapidly destroyed in the liver and kidneys.
Half Life 10-20 minutes
Dosage Forms
Form Route
Liquid Intramuscular
Solution Intramuscular
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Bielsky IF, Hu SB, Szegda KL, Westphal H, Young LJ: Profound impairment in social recognition and reduction in anxiety-like behavior in vasopressin V1a receptor knockout mice. Neuropsychopharmacology. 2004 Mar;29(3):483-93. [PubMed Link Image]
  2. Wersinger SR, Kelliher KR, Zufall F, Lolait SJ, O'Carroll AM, Young WS 3rd: Social motivation is reduced in vasopressin 1b receptor null mice despite normal performance in an olfactory discrimination task. Horm Behav. 2004 Dec;46(5):638-45. [PubMed Link Image]
  3. Wersinger SR, Caldwell HK, Martinez L, Gold P, Hu SB, Young WS 3rd: Vasopressin 1a receptor knockout mice have a subtle olfactory deficit but normal aggression. Genes Brain Behav. 2007 Aug;6(6):540-51. Epub 2006 Nov 3. [PubMed Link Image]
  4. Lolait SJ, Stewart LQ, Jessop DS, Young WS 3rd, O'Carroll AM: The hypothalamic-pituitary-adrenal axis response to stress in mice lacking functional vasopressin V1b receptors. Endocrinology. 2007 Feb;148(2):849-56. Epub 2006 Nov 22. [PubMed Link Image]
  5. Kanwar S, Woodman RC, Poon MC, Murohara T, Lefer AM, Davenpeck KL, Kubes P: Desmopressin induces endothelial P-selectin expression and leukocyte rolling in postcapillary venules. Blood. 1995 Oct 1;86(7):2760-6. [PubMed Link Image]
  6. Drugs.com Link Image
  7. Wikipedia Link Image
  8. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Vasopressin V1a receptor
  2. Vasopressin V2 receptor
  3. Vasopressin V1b receptor
Drug Target 1 [top]
Target 1 ID 185
Target 1 Name Vasopressin V1a receptor
Target 1 Synonyms
  1. AVPR V1a
  2. Antidiuretic hormone receptor 1a
  3. V1aR
  4. Vascular/hepatic-type arginine vasopressin receptor
Target 1 Gene Name AVPR1A
Target 1 Protein Sequence >Vasopressin V1a receptor 
MRLSAGPDAGPSGNSSPWWPLATGAGNTSREAEALGEGNGPPRDVRNEELAKLEIAVLAV
TFAVAVLGNSSVLLALHRTPRKTSRMHLFIRHLSLADLAVAFFQVLPQMCWDITYRFRGP
DWLCRVVKHLQVFGMFASAYMLVVMTADRYIAVCHPLKTLQQPARRSRLMIAAAWVLSFV
LSTPQYFVFSMIEVNNVTKARDCWATFIQPWGSRAYVTWMTGGIFVAPVVILGTCYGFIC
YNIWCNVRGKTASRQSKGAEQAGVAFQKGFLLAPCVSSVKSISRAKIRTVKMTFVIVTAY
IVCWAPFFIIQMWSVWDPMSVWTESENPTITITALLGSLNSCCNPWIYMFFSGHLLQDCV
QSFPCCQNMKEKFNKEDTDSMSRRQTFYSNNRSPTNSTGMWKDSPKSSKSIKFIPVST
Target 1 Number of Residues 424
Target 1 Molecular Weight 46800
Target 1 Theoretical pI 9.67
Target 1 GO Classification
Function
peptide receptor activity, G-protein coupled
vasopressin-like receptor activity
vasopressin receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl- inositol-calcium second messenger system. Has been involved in social behaviors, including affiliation and attachment
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 53-76
  • 89-110
  • 126-147
  • 169-190
  • 219-239
  • 294-313
  • 332-351
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 667068 Link Image
Target 1 UniProtKB/Swiss-Prot ID P37288 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name V1AR_HUMAN Link Image
Target 1 PDB ID 1YTV Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1257 bp 
ATGCGTCTCTCCGCCGGTCCCGACGCGGGGCCCTCGGGCAACTCCAGCCCATGGTGGCCT
CTGGCCACCGGCGCTGGCAACACAAGCCGGGAGGCCGAAGCCCTCGGGGAGGGCAACGGC
CCACCGAGGGACGTGCGCAACGAGGAGCTGGCCAAACTGGAGATCGCCGTGCTGGCGGTG
ACTTTCGCGGTGGCCGTGCTGGGCAACAGCAGCGTACTGCTGGCTCTGCACCGGACGCCG
CGCAAGACGTCCCGCATGCACCTCTTCATCCGACACCTCAGCCTGGCCGACCTGGCCGTG
GCATTCTTCCAGGTGCTGCCGCAAATGTGCTGGGACATCACCTACCGCTTCCGCGGCCCC
GACTGGCTGTGCCGCGTGGTGAAGCACCTGCAGGTGTTCGGCATGTTTGCGTCGGCCTAC
ATGCTGGTAGTCATGACAGCCGACCGCTACATCGCGGTGTGCCACCCGCTCAAGACTCTG
CAACAGCCCGCGCGCCGCTCGCGCCTCATGATCGCGGCCGCCTGGGTGCTGAGCTTCGTG
CTGAGCACGCCGCAGTACTTCGTCTTCTCCATGATCGAGGTGAACAATGTCACCAAGGCC
CGCGACTGCTGGGCCACCTTCATCCAGCCCTGGGGTTCTCGTGCCTACGTGACCTGGATG
ACGGGCGGCATCTTTGTGGCGCCCGTGGTCATCTTGGGTACCTGCTACGGCTTCATCTGC
TACAACATCTGGTGCAACGTCCGCGGGAAGACGGCGTCGCGCCAGAGCAAGGGTGCAGAG
CAAGCGGGTGTGGCCTTCCAAAAGGGGTTCCTGCTCGCACCCTGTGTCAGCAGCGTGAAG
TCCATTTCCCGGGCCAAGATCCGCACGGTGAAGATGACTTTTGTGATCGTGACGGCTTAC
ATCGTCTGCTGGGCGCCTTTCTTCATCATCCAGATGTGGTCTGTCTGGGATCCCATGTCC
GTCTGGACCGAATCGGAAAACCCTACCATCACCATCACTGCATTACTGGGTTCCTTGAAT
AGCTGCTGTAATCCCTGGATATACATGTTTTTTAGTGGCCATCTCCTTCAAGACTGTGTT
CAAAGCTTCCCATGCTGCCAAAACATGAAGGAAAAATTCAACAAAGAAGATACTGACAGT
ATGAGCAGAAGACAGACTTTTTATTCTAACAATCGAAGCCCAACAAACAGTACGGGTATG
TGGAAGGACTCGCCTAAATCTTCCAAGTCCATCAAATTCATTCCTGTTTCAACTTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID AVPR1A Link Image
Target 1 GenAtlas ID AVPR1A Link Image
Target 1 HGNC ID HGNC:895 Link Image
Target 1 Chromosome Location 12
Target 1 Locus 12q14-q15
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Hirasawa A, Shibata K, Kotosai K, Tsujimoto G: Cloning, functional expression and tissue distribution of human cDNA for the vascular-type vasopressin receptor. Biochem Biophys Res Commun. 1994 Aug 30;203(1):72-9. [PubMed Link Image]
  2. Thibonnier M, Auzan C, Madhun Z, Wilkins P, Berti-Mattera L, Clauser E: Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor. J Biol Chem. 1994 Feb 4;269(5):3304-10. [PubMed Link Image]
  3. North WG, Fay MJ, Longo K, Du J: Functional vasopressin V1 type receptors are present in variant as well as classical forms of small-cell carcinoma. Peptides. 1997;18(7):985-93. [PubMed Link Image]
  4. North WG, Fay MJ, Longo KA, Du J: Expression of all known vasopressin receptor subtypes by small cell tumors implies a multifaceted role for this neuropeptide. Cancer Res. 1998 May 1;58(9):1866-71. [PubMed Link Image]
Target 1 Drug References
  1. Hammock EA, Lim MM, Nair HP, Young LJ: Association of vasopressin 1a receptor levels with a regulatory microsatellite and behavior. Genes Brain Behav. 2005 Jul;4(5):289-301. [PubMed Link Image]
  2. Adikesavan NV, Mahmood SS, Stanley N, Xu Z, Wu N, Thibonnier M, Shoham M: A C-terminal segment of the V1R vasopressin receptor is unstructured in the crystal structure of its chimera with the maltose-binding protein. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005 Apr 1;61(Pt 4):341-5. Epub 2005 Mar 24. [PubMed Link Image]
  3. Liedman R, Grant L, Igidbashian S, James I, McLeod A, Skillern L, Akerlund M: Intrauterine pressure, ischemia markers, and experienced pain during administration of a vasopressin V1a receptor antagonist in spontaneous and vasopressin-induced dysmenorrhea. Acta Obstet Gynecol Scand. 2006;85(2):207-11. [PubMed Link Image]
  4. Hiroyama M, Wang S, Aoyagi T, Oikawa R, Sanbe A, Takeo S, Tanoue A: Vasopressin promotes cardiomyocyte hypertrophy via the vasopressin V1A receptor in neonatal mice. Eur J Pharmacol. 2007 Mar 22;559(2-3):89-97. Epub 2006 Dec 29. [PubMed Link Image]
  5. Aoyagi T, Birumachi J, Hiroyama M, Fujiwara Y, Sanbe A, Yamauchi J, Tanoue A: Alteration of glucose homeostasis in V1a vasopressin receptor-deficient mice. Endocrinology. 2007 May;148(5):2075-84. Epub 2007 Feb 15. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 322
Target 2 Name Vasopressin V2 receptor
Target 2 Synonyms
  1. AVPR V2
  2. Antidiuretic hormone receptor
  3. Renal-type arginine vasopressin receptor
Target 2 Gene Name AVPR2
Target 2 Protein Sequence >Vasopressin V2 receptor 
MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLA
ALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQM
VGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQ
RNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGP
SERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEA
PLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTT
ASSSLAKDTSS
Target 2 Number of Residues 377
Target 2 Molecular Weight 40279
Target 2 Theoretical pI 9.41
Target 2 GO Classification
Function
peptide receptor activity, G-protein coupled
vasopressin-like receptor activity
vasopressin receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in rhodopsin-like receptor activity
Target 2 Specific Function Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 39-63
  • 78-98
  • 114-135
  • 160-180
  • 201-220
  • 272-293
  • 309-328
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 28418 Link Image
Target 2 UniProtKB/Swiss-Prot ID P30518 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name V2R_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1116 bp 
ATGCTCATGGCGTCCACCACTTCCGCTGTGCCTGGGCATCCCTCTCTGCCCAGCCTGCCC
AGCAACAGCAGCCAGGAGAGGCCACTGGACACCCGGGACCCGCTGCTAGCCCGGGCGGAG
CTGGCGCTGCTCTCCATAGTCTTTGTGGCTGTGGCCCTGAGCAATGGCCTGGTGCTGGCG
GCCCTAGCTCGGCGGGGCCGGCGGGGCCACTGGGCACCCATACACGTCTTCATTGGCCAC
TTGTGCCTGGCCGACCTGGCCGTGGCTCTGTTCCAAGTGCTGCCCCAGCTGGCCTGGAAG
GCCACCGACCGCTTCCGTGGGCCAGATGCCCTGTGTCGGGCCGTGAAGTATCTGCAGATG
GTGGGCATGTATGCCTCCTCCTACATGATCCTGGCCATGACGCTGGACCGCCACCGTGCC
ATCTGCCGTCCCATGCTGGCGTACCGCCATGGAAGTGGGGCTCACTGGAACCGGCCGGTG
CTAGTGGCTTGGGCCTTCTCGCTCCTTCTCAGCCTGCCCCAGCTCTTCATCTTCGCCCAG
CGCAACGTGGAAGGTGGCAGCGGGGTCACTGACTGCTGGGCCTGCTTTGCGGAGCCCTGG
GGCCGTCGCACCTATGTCACCTGGATTGCCCTGATGGTGTTCGTGGCACCTACCCTGGGT
ATCGCCGCCTGCCAGGTGCTCATCTTCCGGGAGATTCATGCCAGTCTGGTGCCAGGGCCA
TCAGAGAGGCCTGGGGGGCGCCGCAGGGGACGCCGGACAGGCAGCCCCGGTGAGGGAGCC
CACGTGTCAGCAGCTGTGGCCAAGACTGTGAGGATGACGCTAGTGATTGTGGTCGTCTAT
GTGCTGTGCTGGGCACCCTTCTTCCTGGTGCAGCTGTGGGCCGCGTGGGACCCGGAGGCA
CCTCTGGAAGGGGCGCCCTTTGTGCTACTCATGTTGCTGGCCAGCCTCAACAGCTGCACC
AACCCCTGGATCTATGCATCTTTCAGCAGCAGCGTGTCCTCAGAGCTGCGAAGCTTGCTC
TGCTGTGCCCGGGGACGCACCCCACCCAGCCTGGGTCCCCAAGATGAGTCCTGCACCACC
GCCAGCTCCTCCCTGGCCAAGGACACTTCATCGTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID AVPR2 Link Image
Target 2 GenAtlas ID AVPR2 Link Image
Target 2 HGNC ID HGNC:897 Link Image
Target 2 Chromosome Location X
Target 2 Locus Xq28
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Pasel K, Schulz A, Timmermann K, Linnemann K, Hoeltzenbein M, Jaaskelainen J, Gruters A, Filler G, Schoneberg T: Functional characterization of the molecular defects causing nephrogenic diabetes insipidus in eight families. J Clin Endocrinol Metab. 2000 Apr;85(4):1703-10. [PubMed Link Image]
  2. Postina R, Ufer E, Pfeiffer R, Knoers NV, Fahrenholz F: Misfolded vasopressin V2 receptors caused by extracellular point mutations entail congential nephrogenic diabetes insipidus. Mol Cell Endocrinol. 2000 Jun;164(1-2):31-9. [PubMed Link Image]
  3. Inaba S, Hatakeyama H, Taniguchi N, Miyamori I: The property of a novel v2 receptor mutant in a patient with nephrogenic diabetes insipidus. J Clin Endocrinol Metab. 2001 Jan;86(1):381-5. [PubMed Link Image]
  4. Chen CH, Chen WY, Liu HL, Liu TT, Tsou AP, Lin CY, Chao T, Qi Y, Hsiao KJ: Identification of mutations in the arginine vasopressin receptor 2 gene causing nephrogenic diabetes insipidus in Chinese patients. J Hum Genet. 2002;47(2):66-73. [PubMed Link Image]
  5. Pan Y, Metzenberg A, Das S, Jing B, Gitschier J: Mutations in the V2 vasopressin receptor gene are associated with X-linked nephrogenic diabetes insipidus. Nat Genet. 1992 Oct;2(2):103-6. [PubMed Link Image]
  6. van den Ouweland AM, Dreesen JC, Verdijk M, Knoers NV, Monnens LA, Rocchi M, van Oost BA: Mutations in the vasopressin type 2 receptor gene (AVPR2) associated with nephrogenic diabetes insipidus. Nat Genet. 1992 Oct;2(2):99-102. [PubMed Link Image]
  7. Rosenthal W, Seibold A, Antaramian A, Lonergan M, Arthus MF, Hendy GN, Birnbaumer M, Bichet DG: Molecular identification of the gene responsible for congenital nephrogenic diabetes insipidus. Nature. 1992 Sep 17;359(6392):233-5. [PubMed Link Image]
  8. Birnbaumer M, Seibold A, Gilbert S, Ishido M, Barberis C, Antaramian A, Brabet P, Rosenthal W: Molecular cloning of the receptor for human antidiuretic hormone. Nature. 1992 May 28;357(6376):333-5. [PubMed Link Image]
  9. Tsukaguchi H, Matsubara H, Taketani S, Mori Y, Seido T, Inada M: Binding-, intracellular transport-, and biosynthesis-defective mutants of vasopressin type 2 receptor in patients with X-linked nephrogenic diabetes insipidus. J Clin Invest. 1995 Oct;96(4):2043-50. [PubMed Link Image]
  10. Faa V, Ventruto ML, Loche S, Bozzola M, Podda R, Cao A, Rosatelli MC: Mutations in the vasopressin V2-receptor gene in three families of Italian descent with nephrogenic diabetes insipidus. Hum Mol Genet. 1994 Sep;3(9):1685-6. [PubMed Link Image]
  11. 7984150 Birnbaumer M, Gilbert S, Rosenthal W: An extracellular congenital nephrogenic diabetes insipidus mutation of the vasopressin receptor reduces cell surface expression, affinity for ligand, and coupling to the Gs/adenylyl cyclase system. Mol Endocrinol. 1994 Jul;8(7):886-94.
  12. 7987330 Wenkert D, Merendino JJ Jr, Shenker A, Thambi N, Robertson GL, Moses AM, Spiegel AM: Novel mutations in the V2 vasopressin receptor gene of patients with X-linked nephrogenic diabetes insipidus. Hum Mol Genet. 1994 Aug;3(8):1429-30.
  13. 7999078 Oksche A, Dickson J, Schulein R, Seyberth HW, Muller M, Rascher W, Birnbaumer M, Rosenthal W: Two novel mutations in the vasopressin V2 receptor gene in patients with congenital nephrogenic diabetes insipidus. Biochem Biophys Res Commun. 1994 Nov 30;205(1):552-7.
  14. 8037205 Bichet DG, Birnbaumer M, Lonergan M, Arthus MF, Rosenthal W, Goodyer P, Nivet H, Benoit S, Giampietro P, Simonetti S, et al.: Nature and recurrence of AVPR2 mutations in X-linked nephrogenic diabetes insipidus. Am J Hum Genet. 1994 Aug;55(2):278-86.
  15. 8045948 Yuasa H, Ito M, Oiso Y, Kurokawa M, Watanabe T, Oda Y, Ishizuka T, Tani N, Ito S, Shibata A, et al.: Novel mutations in the V2 vasopressin receptor gene in two pedigrees with congenital nephrogenic diabetes insipidus. J Clin Endocrinol Metab. 1994 Aug;79(2):361-5.
  16. 8078903 Friedman E, Bale AE, Carson E, Boson WL, Nordenskjold M, Ritzen M, Ferreira PC, Jammal A, De Marco L: Nephrogenic diabetes insipidus: an X chromosome-linked dominant inheritance pattern with a vasopressin type 2 receptor gene that is structurally normal. Proc Natl Acad Sci U S A. 1994 Aug 30;91(18):8457-61.
  17. 8267567 Tsukaguchi H, Matsubara H, Aritaki S, Kimura T, Abe S, Inada M: Two novel mutations in the vasopressin V2 receptor gene in unrelated Japanese kindreds with nephrogenic diabetes insipidus. Biochem Biophys Res Commun. 1993 Dec 15;197(2):1000-10.
  18. 8479490 Holtzman EJ, Harris HW Jr, Kolakowski LF Jr, Guay-Woodford LM, Botelho B, Ausiello DA: Brief report: a molecular defect in the vasopressin V2-receptor gene causing nephrogenic diabetes insipidus. N Engl J Med. 1993 May 27;328(21):1534-7.
  19. 8514744 Rosenthal W, Antaramian A, Gilbert S, Birnbaumer M: Nephrogenic diabetes insipidus. A V2 vasopressin receptor unable to stimulate adenylyl cyclase. J Biol Chem. 1993 Jun 25;268(18):13030-3.
  20. 8735975 Fay MJ, Du J, Yu X, North WG: Evidence for expression of vasopressin V2 receptor mRNA in human lung. Peptides. 1996;17(3):477-81.
  21. 9224808 Sadeghi HM, Innamorati G, Dagarag M, Birnbaumer M: Palmitoylation of the V2 vasopressin receptor. Mol Pharmacol. 1997 Jul;52(1):21-9.
  22. 9402087 Vargas-Poussou R, Forestier L, Dautzenberg MD, Niaudet P, Dechaux M, Antignac C: Mutations in the vasopressin V2 receptor and aquaporin-2 genes in 12 families with congenital nephrogenic diabetes insipidus. J Am Soc Nephrol. 1997 Dec;8(12):1855-62.
  23. 9452109 Shoji Y, Takahashi T, Suzuki Y, Suzuki T, Komatsu K, Hirono H, Shoji Y, Yokoyama T, Kito H, Takada G: Mutational analyses of AVPR2 gene in three Japanese families with X-linked nephrogenic diabetes insipidus: two recurrent mutations, R137H and deltaV278, caused by the hypermutability at CpG dinucleotides. Hum Mutat. 1998;Suppl 1:S278-83.
  24. 9581826 North WG, Fay MJ, Longo KA, Du J: Expression of all known vasopressin receptor subtypes by small cell tumors implies a multifaceted role for this neuropeptide. Cancer Res. 1998 May 1;58(9):1866-71.
  25. 9711877 Schoneberg T, Schulz A, Biebermann H, Gruters A, Grimm T, Hubschmann K, Filler G, Gudermann T, Schultz G: V2 vasopressin receptor dysfunction in nephrogenic diabetes insipidus caused by different molecular mechanisms. Hum Mutat. 1998;12(3):196-205.
Target 2 Drug References
  1. Bouley R, Hawthorn G, Russo LM, Lin HY, Ausiello DA, Brown D: Aquaporin 2 (AQP2) and vasopressin receptor (V2R) endocytosis in kidney epithelial cells: AQP2 is located in "endocytosis-resistant" membrane domains after vasopressin treatment. Biol Cell. 2005 Aug 12;. [PubMed Link Image]
  2. Slusarz MJ, Slusarz R, Ciarkowski J: 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. [PubMed Link Image]
  3. Bouley R, Hawthorn G, Russo LM, Lin HY, Ausiello DA, Brown D: Aquaporin 2 (AQP2) and vasopressin type 2 receptor (V2R) endocytosis in kidney epithelial cells: AQP2 is located in 'endocytosis-resistant' membrane domains after vasopressin treatment. Biol Cell. 2006 Apr;98(4):215-32. [PubMed Link Image]
  4. Boson WL, Della Manna T, Damiani D, Miranda DM, Gadelha MR, Liberman B, Correa H, Romano-Silva MA, Friedman E, Silva FF, Ribeiro PA, De Marco L: Novel vasopressin type 2 (AVPR2) gene mutations in Brazilian nephrogenic diabetes insipidus patients. Genet Test. 2006 Fall;10(3):157-62. [PubMed Link Image]
  5. Yi X, Bouley R, Lin HY, Bechoua S, Sun TX, Del Re E, Shioda T, Raychowdhury MK, Lu HA, Abou-Samra AB, Brown D, Ausiello DA: Alix (AIP1) is a vasopressin receptor (V2R)-interacting protein that increases lysosomal degradation of the V2R. Am J Physiol Renal Physiol. 2007 May;292(5):F1303-13. Epub 2007 Feb 6. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 850
Target 3 Name Vasopressin V1b receptor
Target 3 Synonyms
  1. AVPR V1b
  2. AVPR V3
  3. Antidiuretic hormone receptor 1b
  4. V1bR
  5. Vasopressin V3 receptor
Target 3 Gene Name AVPR1B
Target 3 Protein Sequence >Vasopressin V1b receptor 
MDSGPLWDANPTPRGTLSAPNATTPWLGRDEELAKVEIGVLATVLVLATGGNLAVLLTLG
QLGRKRSRMHLFVLHLALTDLAVALFQVLPQLLWDITYRFQGPDLLCRAVKYLQVLSMFA
STYMLLAMTLDRYLAVCHPLRSLQQPGQSTYLLIAAPWLLAAIFSLPQVFIFSLREVIQG
SGVLDCWADFGFPWGPRAYLTWTTLAIFVLPVTMLTACYSLICHEICKNLKVKTQAWRVG
GGGWRTWDRPSPSTLAATTRGLPSRVSSINTISRAKIRTVKMTFVIVLAYIACWAPFFSV
QMWSVWDKNAPDEDSTNVAFTISMLLGNLNSCCNPWIYMGFNSHLLPRPLRHLACCGGPQ
PRMRRRLSDGSLSSRHTTLLTRSSCPATLSLSLSLTLSGRPRPEESPRDLELADGEGTAE
TIIF
Target 3 Number of Residues 431
Target 3 Molecular Weight 46971
Target 3 Theoretical pI 9.05
Target 3 GO Classification
Function
peptide receptor activity, G-protein coupled
vasopressin-like receptor activity
vasopressin receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 3 General Function Involved in rhodopsin-like receptor activity
Target 3 Specific Function Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl- inositol-calcium second messenger system
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 36-59
  • 72-93
  • 109-130
  • 152-173
  • 202-222
  • 284-303
  • 322-341
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 563982 Link Image
Target 3 UniProtKB/Swiss-Prot ID P47901 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name V1BR_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1275 bp 
ATGGATTCTGGGCCTCTGTGGGATGCCAACCCCACCCCTCGGGGCACCCTCTCTGCCCCC
AATGCCACAACACCCTGGCTGGGCCGGGATGAGGAGCTGGCCAAGGTGGAGATCGGAGTC
CTGGCCACTGTCCTGGTGCTGGCGACCGGGGGCAACCTGGCTGTGCTGCTGACCCTGGGC
CAGCTGGGCCGCAAGCGCTCCCGCATGCACCTGTTCGTGCTGCACTTAGCCCTGACAGAC
CTGGCCGTGGCGCTCTTCCAGGTGCTGCCACAGCTGCTGTGGGACATCACCTACCGCTTC
CAGGGCCCCGACCTCCTGTGCAGGGCCGTCAAGTACCTGCAGGTGCTCAGCATGTTTGCC
TCCACCTACATGCTGCTGGCCATGACGCTGGACCGCTACCTGGCTGTCTGTCACCCCCTG
CGCAGCCTCCAGCAGCCAGGCCAGTCCACCTACCTGCTCATCGCTGCTCCCTGGCTGCTG
GCCGCCATCTTCAGCCTCCCTCAAGTCTTCATTTTTTCCCTGCGGGAGGTGATCCAGGGC
TCAGGGGTGCTGGACTGCTGGGCAGACTTCGGCTTCCCTTGGGGGCCACGGGCCTACCTC
ACCTGGACCACCCTGGCTATCTTCGTTCTGCCGGTGACCATGCTCACGGCCTGCTACAGC
CTCATCTGCCATGAGATCTGTAAAAACCTAAAAGTCAAGACACAGGCCTGGCGGGTGGGA
GGAGGGGGCTGGAGGACTTGGGACAGGCCCTCACCTTCCACCTTAGCTGCCACCACTCGG
GGGCTGCCATCTCGGGTCAGCAGCATCAACACCATCTCACGGGCCAAGATCCGAACAGTG
AAGATGACCTTTGTCATCGTGCTGGCCTACATCGCTTGCTGGGCTCCCTTCTTCAGTGTC
CAGATGTGGTCCGTGTGGGACAAGAATGCCCCTGATGAAGATTCCACCAATGTGGCTTTC
ACCATCTCTATGCTTTTGGGCAACCTCAACAGCTGCTGCAACCCCTGGATCTACATGGGC
TTCAACAGCCACCTGTTACCGCGGCCCCTGCGTCACCTTGCCTGCTGTGGGGGTCCCCAG
CCCAGGATGCGCCGGCGGCTCTCCGACGGCAGCCTCTCGAGCCGCCACACCACGCTGCTG
ACCCGCTCCAGCTGCCCGGCCACCCTCAGCCTCAGCCTCAGCCTAACCCTCAGTGGGAGG
CCCAGGCCTGAAGAGTCACCAAGGGACTTGGAGCTGGCAGATGGGGAAGGCACCGCTGAG
ACCATCATCTTTTAG
Target 3 GenBank Gene ID
Target 3 GeneCard ID AVPR1B Link Image
Target 3 GenAtlas ID AVPR1B Link Image
Target 3 HGNC ID HGNC:896 Link Image
Target 3 Chromosome Location 1
Target 3 Locus 1q32
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Rene P, Lenne F, Ventura MA, Bertagna X, de Keyzer Y: Nucleotide sequence and structural organization of the human vasopressin pituitary receptor (V3) gene. Gene. 2000 Jan 4;241(1):57-64. [PubMed Link Image]
  2. de Keyzer Y, Auzan C, Lenne F, Beldjord C, Thibonnier M, Bertagna X, Clauser E: Cloning and characterization of the human V3 pituitary vasopressin receptor. FEBS Lett. 1994 Dec 19;356(2-3):215-20. [PubMed Link Image]
  3. Sugimoto T, Saito M, Mochizuki S, Watanabe Y, Hashimoto S, Kawashima H: Molecular cloning and functional expression of a cDNA encoding the human V1b vasopressin receptor. J Biol Chem. 1994 Oct 28;269(43):27088-92. [PubMed Link Image]
  4. North WG, Fay MJ, Longo K, Du J: Functional vasopressin V1 type receptors are present in variant as well as classical forms of small-cell carcinoma. Peptides. 1997;18(7):985-93. [PubMed Link Image]
  5. North WG, Fay MJ, Longo KA, Du J: Expression of all known vasopressin receptor subtypes by small cell tumors implies a multifaceted role for this neuropeptide. Cancer Res. 1998 May 1;58(9):1866-71. [PubMed Link Image]
Target 3 Drug References
  1. Jurkevich A, Berghman LR, Cornett LE, Kuenzel WJ: Characterization and immunohistochemical visualization of the vasotocin VT2 receptor in the pituitary gland of the chicken, Gallus gallus. Gen Comp Endocrinol. 2005 Aug;143(1):82-91. Epub 2005 Mar 23. [PubMed Link Image]
  2. Slusarz MJ, Gieldon A, Slusarz R, Ciarkowski J: Analysis of interactions responsible for vasopressin binding to human neurohypophyseal hormone receptors-molecular dynamics study of the activated receptor-vasopressin-G(alpha) systems. J Pept Sci. 2006 Mar;12(3):180-9. [PubMed Link Image]
  3. Volpi S, Liu Y, Aguilera G: Vasopressin increases GAGA binding activity to the V1b receptor promoter through transactivation of the MAP kinase pathway. J Mol Endocrinol. 2006 Jun;36(3):581-90. [PubMed Link Image]
  4. Young WS, Li J, Wersinger SR, Palkovits M: The vasopressin 1b receptor is prominent in the hippocampal area CA2 where it is unaffected by restraint stress or adrenalectomy. Neuroscience. 2006 Dec 28;143(4):1031-9. Epub 2006 Oct 4. [PubMed Link Image]
  5. Wersinger SR, Caldwell HK, Christiansen M, Young WS 3rd: Disruption of the vasopressin 1b receptor gene impairs the attack component of aggressive behavior in mice. Genes Brain Behav. 2007 Oct;6(7):653-60. Epub 2006 Dec 20. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.