Identification

Summary

Vasopressin is a peptide hormone used to increase blood pressure in patients with vasodilatory shock who are resistant to fluid and catecholamine therapy.

Brand Names
Vasostrict
Generic Name
Vasopressin
DrugBank Accession Number
DB00067
Background

Vasopressin (arginine-vasopressin or antidiuretic hormone) is a nonapeptide primarily produced in the hypothalamus that exhibits diverse physiological functions related to diuresis, hemodynamic modulation, and behaviour.1,2,3,4,6 Vasopressin is very similar to oxytocin, differing in the third and eighth amino acids.7 Despite a wide variety of functions, exogenous vasopressin is primarily used to control blood pressure during systemic shock by increasing vasoconstriction and renal fluid reuptake by acting through V1 and V2 cellular receptors.6,7,8,10

The vasopressive effect of posterior pituitary gland extracts was noted in 1895, while vasopressin itself was not purified until 1951. It has been used for more than five decades for varying conditions, including variceal bleeding, diabetes insipidus, and, more recently, vasodilatory shock.7 It is currently marketed under the trademark VASOSTRICT® by PAR Pharmaceuticals.10

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 2140.46
Monoisotopic: 2138.869561874
Chemical Formula
C92H130N28O24S4
Synonyms
  • Vasopressin, unspecified
  • Vasopressina

Pharmacology

Indication

Vasopressin is indicated to increase blood pressure in adults in vasodilatory shock refractory to the application of fluids and catecholamines.10

Pharmacology
Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
Pharmacodynamics

Vasopressin is a nonapeptide antidiuretic hormone involved in modulating various physiological processes, including autonomic signalling, stress response, behaviour, and memory; the most well-known modulation is of blood pressure.1,2,3,4,10 Vasopressin acts both within the brain and in the periphery to modulate blood pressure through sympathetic outflow, baroreflex modulation, vasoconstriction, and renal fluid retention.6,7,8 These mechanisms vary by location and physiological state, leading to occasionally contradictory responses to vasopressin. Although generally safe, vasopressin may worsen cardiac output in patients with impaired cardiac function. The cessation of vasopressin therapy may result in transient reversible diabetes insipidus, which may require additional desmopressin or vasopressin to manage.10

Mechanism of action

Vasopressin, Cyclo (1-6) L-Cysteinyl-L-Tyrosyl-L-PhenylalanylL-Glutaminyl-L-Asparaginyl-L-Cysteinyl-L-Prolyl-L-Arginyl-L-Glycinamide, is a cyclic nonapeptide hormone primarily produced by the supraoptic and periventricular nuclei of the hypothalamus.6,10 Vasopressin release is mediated by sensory pathways, in which either a 2% increase in plasma osmolarity or a 10% decrease in blood pressure causes the release of endogenous vasopressin.7 Upon release, vasopressin mediates a variety of physiological effects, both centrally and systemically, primarily by binding to G-protein-coupled receptors termed V1 (V1A), V2, and V3 (V1B).

V1 receptors are abundantly expressed in the brain whereby vasopressin binding can increase blood pressure through autonomic pathways.6 Peripherally, V1 is localized in the blood vessels (vascular smooth muscle), platelets, adrenal glands, kidneys, and liver.6,8 Vasopressin binding to V1 causes hydrolysis of phosphatidylinositol-4,5-bisphosphate into inositol triphosphate (IP3) and diacylglycerol (DAG) by phospholipase C, which in turn release intracellular calcium and activate protein kinase C (PKC) to open voltage-gated calcium channels (VGCCs) while closing potassium channels. Overall, intracellular calcium levels rise, which bind calmodulin and cause muscular contraction, resulting in vasoconstriction.7 This is balanced by the apparent ability of vasopressin to induce vasodilation through binding oxytocin receptors and activating endothelial nitric oxide (NO) synthase; NO acts antagonistically to reduce muscle contraction.7 It is also thought that vasopressin, acting through both V1 and oxytocin receptors, causes the cardiac release of atrial natriuretic peptide (ANP), which has a negative inotropic effect; indeed, vasopressin tends to decrease heart rate and cardiac output, although the opposite effect has been noted with low doses.7,10

V2 receptors are abundantly expressed in the distal convoluted tubules and the collecting ducts of the kidneys.8,9 Vasopressin binding to V2 causes activation of a Gs protein that subsequently activates protein kinase A (PKA) through adenylyl cyclase-mediated increase in cyclic adenosine monophosphate (cAMP), which leads to phosphorylation of the water channel aquaporin-2 (AQP2) and its trafficking to the cell surface.8,9 Increased AQP2 levels lead to increased water reabsorption and explains vasopressin's antidiuretic effects.8

V3 (formerly V1B) receptors are primarily located in the anterior pituitary and brain.6,8 Vasopressin released during acute stress causes adrenocorticotropic hormone (ACTH) release from the pituitary through V3 and by potentiating the effects of corticotrophin-releasing factor. Within the brain itself, V3 activation modulates various effects, including recognition, memory, aggression, anxiety, and depression.6

Thus, vasopressin can affect a wide variety of physiological processes, often in apparently contradictory ways depending on the patient's dose and physiological state. Vasodilatory shock causes an immediate release of vasopressin from 20 to 200 times its normal serum concentration, which falls again to normal levels in prolonged shock; in this context, normal serum levels are insufficient to control the pathologic vasodilation.7,8 In these cases, vasopressin acts to depolarize hyperpolarized vascular smooth muscle cells, restore sensitivity to catecholamines, and inhibit excessive nitric oxide production, primarily through acting through V1 receptors. Therefore, vasopressin helps decrease the dose requirement for norepinephrine and is routinely administered together with norepinephrine to restore normal blood pressure in shock states.8,10

TargetActionsOrganism
AVasopressin V2 receptor
agonist
Humans
AVasopressin V1a receptor
agonist
Humans
AVasopressin V1b receptor
agonist
Humans
AOxytocin receptor
agonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Animal studies suggest that vasopressin is metabolized by serine proteases, carboxypeptidases, and disulphide oxidoreductases, primarily in the liver and kidneys. These cleavage events occur at sites important for vasopressin's activity, and hence the metabolites are expected to be inactive.10

Route of elimination

Vasopressin is primarily eliminated in the urine, where only 6% of the dose is excreted unchanged.10

Half-life

Vasopressin administered at 0.01-0.1 U/min has an apparent t1/2 of ≤10 minutes,10 although half-lives of up to 44 minutes have been reported in the literature.

Clearance

Vasopressin has a clearance of 9-25 mL/min/kg in patients with vasodilatory shock receiving 0.01-0.1 U/min of vasopressin.10

Adverse Effects
Adverseeffects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Vasopressin overdose is expected to present with consequences related to excessive vasoconstriction of peripheral, mesenteric, coronary vascular beds, hyponatremia, and possibly with ventricular tachyarrhythmias, rhabdomyolysis, and gastrointestinal symptoms. As vasopressin is rapidly metabolized and cleared, symptoms will resolve with cessation of vasopressin administration.10

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AmitriptylineAmitriptyline may increase the fluid retaining and vasopressor activities of Vasopressin.
AmitriptylinoxideAmitriptylinoxide may increase the fluid retaining and vasopressor activities of Vasopressin.
AmoxapineAmoxapine may increase the fluid retaining and vasopressor activities of Vasopressin.
ArdeparinThe therapeutic efficacy of Vasopressin can be decreased when used in combination with Ardeparin.
BemiparinThe therapeutic efficacy of Vasopressin can be decreased when used in combination with Bemiparin.
Botulinum toxin type ABotulinum toxin type A may increase the hypertensive activities of Vasopressin.
Botulinum toxin type BBotulinum toxin type B may increase the hypertensive activities of Vasopressin.
ButriptylineButriptyline may increase the fluid retaining and vasopressor activities of Vasopressin.
CarbamazepineThe risk or severity of water intoxication can be increased when Carbamazepine is combined with Vasopressin.
CarbidopaVasopressin may increase the hypertensive activities of Carbidopa.
Interactions
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
Not Available

Products

Products2
Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Product Ingredients
IngredientUNIICASInChI Key
ArgipressinY4907O6MFD113-79-1KBZOIRJILGZLEJ-LGYYRGKSSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PitressinInjection20 [USP'U]/1mLIntramuscular; SubcutaneousPar Pharmaceutical2007-10-012016-06-30US flag
PitressinInjection, solution20 [USP'U]/1mLIntramuscular; SubcutaneousPhysicians Total Care, Inc.2011-05-172011-09-30US flag
PitressinInjection20 [USP'U]/1mLIntramuscular; SubcutaneousCardinal Health2007-10-012016-05-31US flag
Pitressin Inj 10 Unit/0.5mlLiquid10 unit / .5 mLIntramuscular; SubcutaneousParke Davis Division, Warner Lambert Canada Inc.1971-12-311997-08-25Canada flag
Pressyn ArLiquid20 unit / 1 mLIntramuscular; SubcutaneousFerring Pharmaceuticals2002-11-042017-03-10Canada flag
VasopressinInjection, solution20 [USP'U]/1mLIntramuscular; SubcutaneousGeneral Injectables & Vaccines2013-12-17Not applicableUS flag
VasopressinInjection, solution20 [USP'U]/1mLIntramuscular; SubcutaneousAmerican Regent1992-10-012013-06-01US flag
VasopressinInjection, solution20 [USP'U]/1mLIntravenous; SubcutaneousPhysicians Total Care, Inc.2007-01-022013-01-15US flag
VasopressinInjection, solution20 [USP'U]/1mLIntramuscular; SubcutaneousGeneral Injectables & Vaccines2010-03-012013-02-01US flag
VasopressinInjection, solution20 [USP'U]/1mLIntramuscular; SubcutaneousFresenius Kabi USA, LLC2001-07-17Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
PitressinVasopressin (20 [USP'U]/1mL)InjectionIntramuscular; SubcutaneousPar Pharmaceutical2007-10-012016-06-30US flag
PitressinVasopressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousPhysicians Total Care, Inc.2011-05-172011-09-30US flag
PitressinVasopressin (20 [USP'U]/1mL)InjectionIntramuscular; SubcutaneousCardinal Health2007-10-012016-05-31US flag
VasopressinVasopressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousGeneral Injectables & Vaccines2013-12-17Not applicableUS flag
VasopressinArgipressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousAmerican Regent1992-10-012013-06-01US flag
VasopressinArgipressin (20 [USP'U]/1mL)Injection, solutionIntravenous; SubcutaneousPhysicians Total Care, Inc.2007-01-022013-01-15US flag
VasopressinArgipressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousGeneral Injectables & Vaccines2010-03-012013-02-01US flag
VasopressinVasopressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousFresenius Kabi USA, LLC2001-07-17Not applicableUS flag
VasopressinArgipressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousAmerican Regent1992-10-012013-05-01US flag
VasopressinArgipressin (20 [USP'U]/1mL)Injection, solutionIntramuscular; SubcutaneousGeneral Injectables & Vaccines2010-08-012013-03-01US flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
Y87Y826H08
CAS number
11000-17-2
InChI Key
JLTCWSBVQSZVLT-UHFFFAOYSA-N
InChI
InChI=1S/C46H65N15O12S2.C46H65N13O12S2/c47-27-22-74-75-23-33(45(73)61-17-5-9-34(61)44(72)56-28(8-4-16-53-46(51)52)39(67)54-21-37(50)65)60-43(71)32(20-36(49)64)59-40(68)29(14-15-35(48)63)55-41(69)31(18-24-6-2-1-3-7-24)58-42(70)30(57-38(27)66)19-25-10-12-26(62)13-11-25;47-17-5-4-9-29(40(65)52-22-38(51)63)54-45(70)35-10-6-18-59(35)46(71)34-24-73-72-23-28(48)39(64)55-31(20-26-11-13-27(60)14-12-26)43(68)56-32(19-25-7-2-1-3-8-25)42(67)53-30(15-16-36(49)61)41(66)57-33(21-37(50)62)44(69)58-34/h1-3,6-7,10-13,27-34,62H,4-5,8-9,14-23,47H2,(H2,48,63)(H2,49,64)(H2,50,65)(H,54,67)(H,55,69)(H,56,72)(H,57,66)(H,58,70)(H,59,68)(H,60,71)(H4,51,52,53);1-3,7-8,11-14,28-35,60H,4-6,9-10,15-24,47-48H2,(H2,49,61)(H2,50,62)(H2,51,63)(H,52,65)(H,53,67)(H,54,70)(H,55,64)(H,56,68)(H,57,66)(H,58,69)
IUPAC Name
2-({1-[19-amino-13-benzyl-10-(2-carbamoylethyl)-7-(carbamoylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl]pyrrolidin-2-yl}formamido)-N-(carbamoylmethyl)-5-[(diaminomethylidene)amino]pentanamide; 6-amino-2-({1-[19-amino-13-benzyl-10-(2-carbamoylethyl)-7-(carbamoylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl]pyrrolidin-2-yl}formamido)-N-(carbamoylmethyl)hexanamide
SMILES
NCCCCC(NC(=O)C1CCCN1C(=O)C1CSSCC(N)C(=O)NC(CC2=CC=C(O)C=C2)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(N)=O)C(=O)N1)C(=O)NCC(N)=O.NC1CSSCC(NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC2=CC=C(O)C=C2)NC1=O)C(=O)N1CCCC1C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O

References

Synthesis Reference

Nedumparambil A. Abraham, Hans U. Immer, Kazimir Sestanj, "Process for producing triglycyl-lysine vasopressin and intermediates therefor." U.S. Patent US4093610, issued June, 1963.

US4093610
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. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  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. [Article]
  6. Lozic M, Sarenac O, Murphy D, Japundzic-Zigon N: Vasopressin, Central Autonomic Control and Blood Pressure Regulation. Curr Hypertens Rep. 2018 Feb 26;20(2):11. doi: 10.1007/s11906-018-0811-0. [Article]
  7. Pelletier JS, Dicken B, Bigam D, Cheung PY: Cardiac effects of vasopressin. J Cardiovasc Pharmacol. 2014 Jul;64(1):100-7. doi: 10.1097/FJC.0000000000000092. [Article]
  8. Wagener G, Bakker J: Vasopressin in cirrhosis and sepsis: physiology and clinical implications. Minerva Anestesiol. 2015 Dec;81(12):1377-83. Epub 2014 Nov 11. [Article]
  9. Ranieri M, Di Mise A, Tamma G, Valenti G: Vasopressin-aquaporin-2 pathway: recent advances in understanding water balance disorders. F1000Res. 2019 Feb 4;8. doi: 10.12688/f1000research.16654.1. eCollection 2019. [Article]
  10. FDA Approved Drug Products: VASOSTRICT (vasopressin) injection [Link]
KEGG Drug
D00101
KEGG Compound
C00840
PubChem Substance
46505933
ChemSpider
10152658
RxNav
11149
ChEMBL
CHEMBL373742
Therapeutic Targets Database
DAP000018
PharmGKB
PA451858
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Vasopressin
MSDS
Download (143 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceEndotoxaemia1
4CompletedPreventionHemorrhage1
4CompletedPreventionKidney Failure1
4CompletedTreatmentBlood Loss During Vaginal Hysterectomy1
4CompletedTreatmentCardiac Arrest1
4CompletedTreatmentSurgical Blood Loss1
4Not Yet RecruitingPreventionAcute Kidney Injury (AKI) / Cirrhosis of the Liver / End-stage Liver Disease (ESLD) / Liver Transplant; Complications1
4RecruitingBasic ScienceGeneral Anesthesia / Major Abdominal Surgeries / Vasopressin Infusion / Ventilations, Mechanical1
4RecruitingPreventionAcute Kidney Injury (AKI)1
4RecruitingTreatmentShock1

Pharmacoeconomics

Manufacturers
  • Parke davis div warner lambert co
Packagers
  • American Regent
  • APP Pharmaceuticals
  • APPD
  • A-S Medication Solutions LLC
  • Cardinal Health
  • JHP Pharmaceuticals LLC
  • Luitpold Pharmaceuticals Inc.
  • Monarch Pharmacy
  • PD-Rx Pharmaceuticals Inc.
Dosage Forms
FormRouteStrength
SolutionIntramuscular; Subcutaneous20 IU
Injection, solution, concentrateIntravenous
Injection, solution, concentrateIntravenous40 U.I./2ML
Injection
InjectionIntramuscular; Subcutaneous20 [USP'U]/1mL
Injection, solutionIntramuscular; Subcutaneous20 [USP'U]/1mL
LiquidIntramuscular; Subcutaneous10 unit / .5 mL
LiquidIntramuscular; Subcutaneous20 unit / 1 mL
SolutionIntravenous20 IU
InjectionIntravenous20 IU/mL
SolutionIntramuscular; Intravenous; Subcutaneous20 U
Injection, solutionIntramuscular20 [USP'U]/1mL
Injection, solutionIntravenous; Subcutaneous20 [USP'U]/1mL
LiquidIntramuscular; Nasal; Subcutaneous20 unit / mL
LiquidIntramuscular; Subcutaneous20 unit / mL
SolutionIntramuscular; Subcutaneous20 unit / mL
InjectionIntramuscular; Subcutaneous20 u/ml
Injection, solutionIntravenous
InjectionIntravenous20 [USP'U]/1mL
InjectionIntravenous40 [USP'U]/100mL
InjectionIntravenous60 [USP'U]/100mL
Prices
Unit descriptionCostUnit
Pitressin 20 unit/ml vial7.68USD ml
Vasopressin 10 unit/0.5 ml vial2.88USD vial
Vasopressin 20 unit/ml vial1.86USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9687526No2017-06-272035-01-30US flag
US9375478No2016-06-282035-01-30US flag
US9744209No2017-08-292035-01-30US flag
US9744239No2017-08-292035-01-30US flag
US9750785No2017-09-052035-01-30US flag
US9937223No2018-04-102035-01-30US flag
US10010575No2018-07-032035-01-30US flag
US9925233No2018-03-272035-01-30US flag
US9974827No2018-05-222035-01-30US flag
US9968649No2018-05-152035-01-30US flag
US9962422No2018-05-082035-01-30US flag
US9925234No2018-03-272035-01-30US flag
US9981006No2018-05-292035-01-30US flag
US9919026No2018-03-202035-01-30US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.124 mg/mLALOGPS
logP-1.4ALOGPS
logP-7.2ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)7.65ChemAxon
pKa (Strongest Basic)11.5ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count16ChemAxon
Hydrogen Donor Count14ChemAxon
Polar Surface Area463.93 Å2ChemAxon
Rotatable Bond Count38ChemAxon
Refractivity272.59 m3·mol-1ChemAxon
Polarizability108.29 Å3ChemAxon
Number of Rings8ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Vasopressin receptor activity
Specific Function
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Involved in renal water reabsorption.
Gene Name
AVPR2
Uniprot ID
P30518
Uniprot Name
Vasopressin V2 receptor
Molecular Weight
40278.57 Da
References
  1. 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. [Article]
  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. [Article]
  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. [Article]
  4. 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. [Article]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  6. Lozic M, Sarenac O, Murphy D, Japundzic-Zigon N: Vasopressin, Central Autonomic Control and Blood Pressure Regulation. Curr Hypertens Rep. 2018 Feb 26;20(2):11. doi: 10.1007/s11906-018-0811-0. [Article]
  7. FDA Approved Drug Products: VASOSTRICT (vasopressin) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Vasopressin receptor activity
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 behavi...
Gene Name
AVPR1A
Uniprot ID
P37288
Uniprot Name
Vasopressin V1a receptor
Molecular Weight
46799.105 Da
References
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  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. [Article]
  6. Lozic M, Sarenac O, Murphy D, Japundzic-Zigon N: Vasopressin, Central Autonomic Control and Blood Pressure Regulation. Curr Hypertens Rep. 2018 Feb 26;20(2):11. doi: 10.1007/s11906-018-0811-0. [Article]
  7. FDA Approved Drug Products: VASOSTRICT (vasopressin) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Vasopressin receptor activity
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.
Gene Name
AVPR1B
Uniprot ID
P47901
Uniprot Name
Vasopressin V1b receptor
Molecular Weight
46970.345 Da
References
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. Lozic M, Sarenac O, Murphy D, Japundzic-Zigon N: Vasopressin, Central Autonomic Control and Blood Pressure Regulation. Curr Hypertens Rep. 2018 Feb 26;20(2):11. doi: 10.1007/s11906-018-0811-0. [Article]
  7. FDA Approved Drug Products: VASOSTRICT (vasopressin) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Vasopressin receptor activity
Specific Function
Receptor for oxytocin. The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system.
Gene Name
OXTR
Uniprot ID
P30559
Uniprot Name
Oxytocin receptor
Molecular Weight
42770.99 Da
References
  1. Pelletier JS, Dicken B, Bigam D, Cheung PY: Cardiac effects of vasopressin. J Cardiovasc Pharmacol. 2014 Jul;64(1):100-7. doi: 10.1097/FJC.0000000000000092. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
This interaction is based on animal studies.
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Madon J, Hagenbuch B, Landmann L, Meier PJ, Stieger B: Transport function and hepatocellular localization of mrp6 in rat liver. Mol Pharmacol. 2000 Mar;57(3):634-41. [Article]

Drug created at June 13, 2005 13:24 / Updated at November 28, 2021 11:56