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Identification
NameTerlipressin
Accession NumberDB02638  (EXPT03310)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionTerlipressin is an analogue of vasopressin used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help. [Wikipedia]
Structure
Thumb
Synonyms
Terlipressin
Terlipressina
Terlipressine
Terlipressinum
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
GlypressinFerring Pharmaceuticals
LucassinNot Available
TeripressNew Medicon Pharma
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7Z5X49W53P
CAS number14636-12-5
WeightAverage: 1227.372
Monoisotopic: 1226.496097158
Chemical FormulaC52H74N16O15S2
InChI KeyInChIKey=BENFXAYNYRLAIU-QSVFAHTRSA-N
InChI
InChI=1S/C52H74N16O15S2/c53-17-5-4-9-31(45(76)60-23-41(57)72)63-51(82)38-10-6-18-68(38)52(83)37-27-85-84-26-36(61-44(75)25-59-43(74)24-58-42(73)22-54)50(81)65-34(20-29-11-13-30(69)14-12-29)48(79)64-33(19-28-7-2-1-3-8-28)47(78)62-32(15-16-39(55)70)46(77)66-35(21-40(56)71)49(80)67-37/h1-3,7-8,11-14,31-38,69H,4-6,9-10,15-27,53-54H2,(H2,55,70)(H2,56,71)(H2,57,72)(H,58,73)(H,59,74)(H,60,76)(H,61,75)(H,62,78)(H,63,82)(H,64,79)(H,65,81)(H,66,77)(H,67,80)/t31-,32-,33-,34-,35-,36-,37-,38-/m0/s1
IUPAC Name
(2S)-6-amino-2-{[(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-{2-[2-(2-aminoacetamido)acetamido]acetamido}-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
NCCCC[[email protected]](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[[email protected]](NC(=O)CNC(=O)CNC(=O)CN)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.
KingdomOrganic compounds
Super ClassOrganic Polymers
ClassPolypeptides
Sub ClassNot Available
Direct ParentPolypeptides
Alternative Parents
Substituents
  • Polypeptide
  • Cyclic alpha peptide
  • N-acyl-alpha amino acid or derivatives
  • Macrolactam
  • Alpha-amino acid amide
  • Alpha-amino acid or derivatives
  • N-substituted-alpha-amino acid
  • Pyrrolidine-2-carboxamide
  • Pyrrolidine carboxylic acid or derivatives
  • N-acylpyrrolidine
  • Phenol
  • Fatty acyl
  • Benzenoid
  • N-acyl-amine
  • Fatty amide
  • Monocyclic benzene moiety
  • Tertiary carboxylic acid amide
  • Pyrrolidine
  • Cyclic alcohol
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Primary carboxylic acid amide
  • Organic disulfide
  • Lactam
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationCommonly used to stop bleeding of varices in the food pipe (oesophagus).
PharmacodynamicsTerlipressin is a medicine similar to a naturally occurring hormone present in the body, known as antidiuretic hormone (ADH) or vasopressin. ADH has two main effects in the body. Firstly, it causes narrowing of blood vessels (vasoconstriction), thereby limiting blood flow to a particular area of the body. It also acts on receptors in the kidney to retain water in the body, which helps to prevent excessive loss of water in the urine.
Mechanism of actionTerlipressin, an analogue of 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 terlipressin 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.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingApproximately 30%
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7085
Blood Brain Barrier-0.8855
Caco-2 permeable-0.7797
P-glycoprotein substrateSubstrate0.7307
P-glycoprotein inhibitor INon-inhibitor0.8042
P-glycoprotein inhibitor IINon-inhibitor0.8977
Renal organic cation transporterNon-inhibitor0.8004
CYP450 2C9 substrateNon-substrate0.8292
CYP450 2D6 substrateNon-substrate0.7878
CYP450 3A4 substrateNon-substrate0.5247
CYP450 1A2 substrateNon-inhibitor0.9358
CYP450 2C9 inhibitorNon-inhibitor0.766
CYP450 2D6 inhibitorNon-inhibitor0.8606
CYP450 2C19 inhibitorNon-inhibitor0.7565
CYP450 3A4 inhibitorNon-inhibitor0.7185
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8301
Ames testNon AMES toxic0.736
CarcinogenicityNon-carcinogens0.8513
BiodegradationNot ready biodegradable0.9261
Rat acute toxicity2.9218 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8955
hERG inhibition (predictor II)Inhibitor0.6764
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.167 mg/mLALOGPS
logP-1.6ALOGPS
logP-10ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)9.43ChemAxon
pKa (Strongest Basic)10.26ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count17ChemAxon
Hydrogen Donor Count16ChemAxon
Polar Surface Area512.85 Å2ChemAxon
Rotatable Bond Count25ChemAxon
Refractivity305.18 m3·mol-1ChemAxon
Polarizability123.88 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Pesaturo AB, Jennings HR, Voils SA: Terlipressin: vasopressin analog and novel drug for septic shock. Ann Pharmacother. 2006 Dec;40(12):2170-7. Epub 2006 Dec 5. [PubMed:17148649 ]
  2. Klein M, Weksler N, Borer A, Koyfman L, Kesslin J, Gurman GM: Terlipressin facilitates transport of septic patients treated with norepinephrine. Isr Med Assoc J. 2006 Oct;8(10):691-3. [PubMed:17125115 ]
  3. Leone M, Charvet A, Delmas A, Albanese J, Martin C, Boyle WA: Terlipressin: a new therapeutic for calcium-channel blockers overdose. J Crit Care. 2005 Mar;20(1):114-5. [PubMed:16015526 ]
  4. Matok I, Vard A, Efrati O, Rubinshtein M, Vishne T, Leibovitch L, Adam M, Barzilay Z, Paret G: Terlipressin as rescue therapy for intractable hypotension due to septic shock in children. Shock. 2005 Apr;23(4):305-10. [PubMed:15803052 ]
  5. Kam PC, Williams S, Yoong FF: Vasopressin and terlipressin: pharmacology and its clinical relevance. Anaesthesia. 2004 Oct;59(10):993-1001. [PubMed:15488059 ]
External Links
ATC CodesH01BA04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Terlipressin.
AcebutololAcebutolol may increase the hypotensive activities of Terlipressin.
AlfuzosinAlfuzosin may increase the hypotensive activities of Terlipressin.
AliskirenTerlipressin may increase the hypotensive activities of Aliskiren.
AlprenololAlprenolol may increase the hypotensive activities of Terlipressin.
AmbrisentanTerlipressin may increase the hypotensive activities of Ambrisentan.
AmifostineTerlipressin may increase the hypotensive activities of Amifostine.
AmlodipineAmlodipine may increase the hypotensive activities of Terlipressin.
AtenololAtenolol may increase the hypotensive activities of Terlipressin.
BenazeprilBenazepril may increase the hypotensive activities of Terlipressin.
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Terlipressin.
BenmoxinBenmoxin may increase the hypotensive activities of Terlipressin.
BepridilBepridil may increase the hypotensive activities of Terlipressin.
BetaxololBetaxolol may increase the hypotensive activities of Terlipressin.
BethanidineBethanidine may increase the hypotensive activities of Terlipressin.
BimatoprostBimatoprost may increase the hypotensive activities of Terlipressin.
BisoprololBisoprolol may increase the hypotensive activities of Terlipressin.
BosentanBosentan may increase the hypotensive activities of Terlipressin.
BretyliumBretylium may increase the hypotensive activities of Terlipressin.
BrimonidineTerlipressin may increase the hypotensive activities of Brimonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Terlipressin.
BupranololTerlipressin may increase the hypotensive activities of Bupranolol.
CandesartanCandesartan may increase the hypotensive activities of Terlipressin.
CandoxatrilCandoxatril may increase the hypotensive activities of Terlipressin.
CaptoprilCaptopril may increase the hypotensive activities of Terlipressin.
CaroxazoneCaroxazone may increase the hypotensive activities of Terlipressin.
CarteololCarteolol may increase the hypotensive activities of Terlipressin.
CarvedilolCarvedilol may increase the hypotensive activities of Terlipressin.
CeliprololTerlipressin may increase the hypotensive activities of Celiprolol.
ChlorothiazideChlorothiazide may increase the hypotensive activities of Terlipressin.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Terlipressin.
CilazaprilCilazapril may increase the hypotensive activities of Terlipressin.
ClonidineClonidine may increase the hypotensive activities of Terlipressin.
CryptenamineCryptenamine may increase the hypotensive activities of Terlipressin.
CyclothiazideCyclothiazide may increase the hypotensive activities of Terlipressin.
DebrisoquinTerlipressin may increase the hypotensive activities of Debrisoquin.
DeserpidineTerlipressin may increase the hypotensive activities of Deserpidine.
DiazoxideDiazoxide may increase the hypotensive activities of Terlipressin.
DiltiazemDiltiazem may increase the hypotensive activities of Terlipressin.
DorzolamideDorzolamide may increase the hypotensive activities of Terlipressin.
DoxazosinDoxazosin may increase the hypotensive activities of Terlipressin.
EfonidipineTerlipressin may increase the hypotensive activities of Efonidipine.
EnalaprilEnalapril may increase the hypotensive activities of Terlipressin.
EnalaprilatTerlipressin may increase the hypotensive activities of Enalaprilat.
EpoprostenolEpoprostenol may increase the hypotensive activities of Terlipressin.
EprosartanEprosartan may increase the hypotensive activities of Terlipressin.
FelodipineFelodipine may increase the hypotensive activities of Terlipressin.
FenoldopamFenoldopam may increase the hypotensive activities of Terlipressin.
FosinoprilFosinopril may increase the hypotensive activities of Terlipressin.
FurazolidoneFurazolidone may increase the hypotensive activities of Terlipressin.
GuanabenzGuanabenz may increase the hypotensive activities of Terlipressin.
GuanadrelGuanadrel may increase the hypotensive activities of Terlipressin.
GuanethidineGuanethidine may increase the hypotensive activities of Terlipressin.
GuanfacineGuanfacine may increase the hypotensive activities of Terlipressin.
HexamethoniumTerlipressin may increase the hypotensive activities of Hexamethonium.
HydracarbazineHydracarbazine may increase the hypotensive activities of Terlipressin.
HydralazineHydralazine may increase the hypotensive activities of Terlipressin.
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Terlipressin.
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Terlipressin.
IloprostIloprost may increase the hypotensive activities of Terlipressin.
IndapamideIndapamide may increase the hypotensive activities of Terlipressin.
IndenololTerlipressin may increase the hypotensive activities of Indenolol.
IndoraminTerlipressin may increase the hypotensive activities of Indoramin.
IproclozideIproclozide may increase the hypotensive activities of Terlipressin.
IproniazidIproniazid may increase the hypotensive activities of Terlipressin.
IrbesartanIrbesartan may increase the hypotensive activities of Terlipressin.
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Terlipressin.
IsradipineIsradipine may increase the hypotensive activities of Terlipressin.
LabetalolLabetalol may increase the hypotensive activities of Terlipressin.
LacidipineTerlipressin may increase the hypotensive activities of Lacidipine.
LatanoprostLatanoprost may increase the hypotensive activities of Terlipressin.
LercanidipineLercanidipine may increase the hypotensive activities of Terlipressin.
LisinoprilLisinopril may increase the hypotensive activities of Terlipressin.
LofexidineTerlipressin may increase the hypotensive activities of Lofexidine.
LosartanLosartan may increase the hypotensive activities of Terlipressin.
MacitentanTerlipressin may increase the hypotensive activities of Macitentan.
ManidipineTerlipressin may increase the hypotensive activities of Manidipine.
MebanazineMebanazine may increase the hypotensive activities of Terlipressin.
MecamylamineMecamylamine may increase the hypotensive activities of Terlipressin.
MethyldopaMethyldopa may increase the hypotensive activities of Terlipressin.
Methylene blueMethylene blue may increase the hypotensive activities of Terlipressin.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Terlipressin.
MetipranololMetipranolol may increase the hypotensive activities of Terlipressin.
MetolazoneMetolazone may increase the hypotensive activities of Terlipressin.
MetoprololMetoprolol may increase the hypotensive activities of Terlipressin.
MibefradilMibefradil may increase the hypotensive activities of Terlipressin.
MinaprineMinaprine may increase the hypotensive activities of Terlipressin.
MinoxidilMinoxidil may increase the hypotensive activities of Terlipressin.
MoclobemideMoclobemide may increase the hypotensive activities of Terlipressin.
MoexiprilMoexipril may increase the hypotensive activities of Terlipressin.
MolsidomineMolsidomine may increase the hypotensive activities of Terlipressin.
MoxonidineTerlipressin may increase the hypotensive activities of Moxonidine.
NadololNadolol may increase the hypotensive activities of Terlipressin.
NebivololTerlipressin may increase the hypotensive activities of Nebivolol.
NialamideNialamide may increase the hypotensive activities of Terlipressin.
NicardipineNicardipine may increase the hypotensive activities of Terlipressin.
NicorandilTerlipressin may increase the hypotensive activities of Nicorandil.
NiguldipineTerlipressin may increase the hypotensive activities of Niguldipine.
NilvadipineTerlipressin may increase the hypotensive activities of Nilvadipine.
NimodipineNimodipine may increase the hypotensive activities of Terlipressin.
NisoldipineNisoldipine may increase the hypotensive activities of Terlipressin.
NitrendipineNitrendipine may increase the hypotensive activities of Terlipressin.
NitroprussideNitroprusside may increase the hypotensive activities of Terlipressin.
ObinutuzumabTerlipressin may increase the hypotensive activities of Obinutuzumab.
OctamoxinOctamoxin may increase the hypotensive activities of Terlipressin.
OlmesartanOlmesartan may increase the hypotensive activities of Terlipressin.
OmapatrilatOmapatrilat may increase the hypotensive activities of Terlipressin.
OxprenololOxprenolol may increase the hypotensive activities of Terlipressin.
PargylinePargyline may increase the hypotensive activities of Terlipressin.
PenbutololPenbutolol may increase the hypotensive activities of Terlipressin.
PentoliniumPentolinium may increase the hypotensive activities of Terlipressin.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Terlipressin.
PerindoprilPerindopril may increase the hypotensive activities of Terlipressin.
PhenelzinePhenelzine may increase the hypotensive activities of Terlipressin.
PheniprazinePheniprazine may increase the hypotensive activities of Terlipressin.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Terlipressin.
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Terlipressin.
PhentolaminePhentolamine may increase the hypotensive activities of Terlipressin.
PinacidilTerlipressin may increase the hypotensive activities of Pinacidil.
PindololPindolol may increase the hypotensive activities of Terlipressin.
PirlindolePirlindole may increase the hypotensive activities of Terlipressin.
PivhydrazinePivhydrazine may increase the hypotensive activities of Terlipressin.
PolythiazidePolythiazide may increase the hypotensive activities of Terlipressin.
PrazosinPrazosin may increase the hypotensive activities of Terlipressin.
PropranololPropranolol may increase the hypotensive activities of Terlipressin.
QuinaprilQuinapril may increase the hypotensive activities of Terlipressin.
QuinineQuinine may increase the hypotensive activities of Terlipressin.
RamiprilRamipril may increase the hypotensive activities of Terlipressin.
RasagilineRasagiline may increase the hypotensive activities of Terlipressin.
RemikirenRemikiren may increase the hypotensive activities of Terlipressin.
RescinnamineTerlipressin may increase the hypotensive activities of Rescinnamine.
ReserpineReserpine may increase the hypotensive activities of Terlipressin.
RiociguatTerlipressin may increase the hypotensive activities of Riociguat.
RituximabTerlipressin may increase the hypotensive activities of Rituximab.
SafrazineSafrazine may increase the hypotensive activities of Terlipressin.
SaprisartanSaprisartan may increase the hypotensive activities of Terlipressin.
SelegilineSelegiline may increase the hypotensive activities of Terlipressin.
SelexipagTerlipressin may increase the hypotensive activities of Selexipag.
SildenafilSildenafil may increase the antihypertensive activities of Terlipressin.
SitaxentanTerlipressin may increase the hypotensive activities of Sitaxentan.
SpiraprilSpirapril may increase the hypotensive activities of Terlipressin.
TadalafilTadalafil may increase the antihypertensive activities of Terlipressin.
TelmisartanTelmisartan may increase the hypotensive activities of Terlipressin.
TemocaprilTerlipressin may increase the hypotensive activities of Temocapril.
TiboloneTerlipressin may increase the hypotensive activities of Tibolone.
TicrynafenTerlipressin may increase the hypotensive activities of Ticrynafen.
TimololTimolol may increase the hypotensive activities of Terlipressin.
TolazolineTolazoline may increase the hypotensive activities of Terlipressin.
ToloxatoneToloxatone may increase the hypotensive activities of Terlipressin.
TorasemideTorasemide may increase the hypotensive activities of Terlipressin.
TrandolaprilTrandolapril may increase the hypotensive activities of Terlipressin.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Terlipressin.
TranylcypromineTranylcypromine may increase the hypotensive activities of Terlipressin.
TravoprostTravoprost may increase the hypotensive activities of Terlipressin.
TreprostinilTreprostinil may increase the hypotensive activities of Terlipressin.
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Terlipressin.
TrimazosinTerlipressin may increase the hypotensive activities of Trimazosin.
TrimethaphanTrimethaphan may increase the hypotensive activities of Terlipressin.
UdenafilUdenafil may increase the antihypertensive activities of Terlipressin.
UnoprostoneTerlipressin may increase the hypotensive activities of Unoprostone.
ValsartanValsartan may increase the hypotensive activities of Terlipressin.
VardenafilVardenafil may increase the antihypertensive activities of Terlipressin.
XylometazolineTerlipressin may increase the hypotensive activities of Xylometazoline.
YohimbineYohimbine may decrease the antihypertensive activities of Terlipressin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
stimulator
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 behaviors, including affiliation and attachment.
Gene Name:
AVPR1A
Uniprot ID:
P37288
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. [PubMed:17275806 ]
  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. [PubMed:16532916 ]
  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. [PubMed:16511036 ]
  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. [PubMed:16011575 ]
  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:17303660 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
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
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. [PubMed:17020465 ]
  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:16333859 ]
  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:16563128 ]
  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. [PubMed:17287200 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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
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. [PubMed:17027167 ]
  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. [PubMed:16720725 ]
  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. [PubMed:17284170 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23