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  2. Signaling Pathways
  3. GPCR/G Protein
  4. Vasopressin Receptor

Vasopressin Receptor

Receptor

Vasopressin Receptor

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The neurohypophysial hormone arginine vasopressin (AVP) is involved in diverse functions including regulation of body fluid homeostasis, vasoconstriction, and adrenocorticotropic hormone release. These physiological effects are mediated by three subtypes of vasopressin receptors, designated V1a, V1b (or V3), and V2. They all belong to the large rhodopsin-like G-protein-coupled receptor family.

The V1a receptor is expressed in both neuronal and non-neuronal tissues including the heart and elicits a variety of physiological effects including cell contraction and proliferation, stimulation of hepatic glycogenolysis, platelet aggregation and coagulation factor release. The V1b receptor subtype is found predominantly in the pituitary gland where it stimulates adrenocorticotropic hormone release. Both the V1a and V1b AVP receptors act through a G protein alpha-subunit of the Gαq family (αq, q11, q14, α15/16) to activate phospholipase C-β, and, thus enhance cellular IP3 and calcium levels. By contrast, the V2 receptor subtype is localized predominantly to the kidney where it mediates the anti-diuretic effects of AVP through the heterotrimeric G protein Gs and activation of adenylyl cyclase.

Vasopressin Receptor Isoform Specific Products:

Vasopressin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P4683A
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate
    		Antagonist 99.81%
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats.
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate
  • HY-P2538
    Big Endothelin-1 (1-38), human
    		Agonist
    Big Endothelin-1 (1-38), human is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide.
    Big Endothelin-1 (1-38), human
  • HY-P4683
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
    		Antagonist
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats.
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
  • HY-108678
    TC OT 39
    		Antagonist
    TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models.
    TC OT 39
  • HY-P1810
    c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm
    		Agonist
    c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.25 and 0.05 nM for hV2R and rV2R, respectively.
    c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm
  • HY-P1809
    Velmupressin
    		Agonist
    Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively.
    Velmupressin
  • HY-159507
    Brezivaptan
    		Antagonist
    Brezivaptan (Brezivaptanum; TH1773; TS-121) is a vasopressin receptor antagonist.
    Brezivaptan
  • HY-P0049A
    Argipressin diacetate
    		Agonist
    Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)) is a 9 amino acid neuropeptide secreted by the posterior pituitary. Argipressin (diacetate) (AVP (diacetate)) can regulate the biological effects of fluid balance, osmolality and cardiovascular through three separate G-protein coupled receptors (GPCRs), namely Avpr1a (V1a), Avpr1b (V1b) and Avpr2 (V2). Argipressin (diacetate) (AVP (diacetate)) also have potentially important effects on centrally regulated metabolic processes.
    Argipressin diacetate
  • HY-P1390A
    d[Cha4]-AVP TFA
    		Agonist
    d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP TFA shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors.
    d[Cha4]-AVP TFA
  • HY-146272
    Vasopressin V2 receptor antagonist 1
    		Antagonist
    Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM. Vasopressin V2 receptor antagonist 1 can be used for autosomal dominant polycystic kidney disease (ADPKD) research.
    Vasopressin V2 receptor antagonist 1
  • HY-P4201
    JKC 301
    		Antagonist
    JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking.
    JKC 301
  • HY-139572
    Enuvaptan
    		Antagonist
    Enuvaptan (BAY-2327949) is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases.
    Enuvaptan
  • HY-P2539
    Big Endothelin-1 (1-39), porcine
    		Agonist
    Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide. Big Endothelin-1 (1-39), porcine has similar pressor effects in vivo.
    Big Endothelin-1 (1-39), porcine
  • HY-P5006
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin
    		Antagonist
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin (d(CH2)5[Tyr(Me)2, Dab5]AVP) is a specific antagonist of vasopressin V1a receptor, with a pA2 of 6.71.
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin
  • HY-P5535
    Invopressin
    		99.40%
    Invopressin (Compound 42) is a vasopressin V1A receptor partial agonist (EC50: 1.0 nM). Invopressin can be used for research of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.
    Invopressin
  • HY-P5214
    Vasopressin Dimer (anti-parallel) (TFA)
    		Activator
    Vasopressin Dimer (anti-parallel) TFA is an anti-parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (anti-parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR.
    Vasopressin Dimer (anti-parallel) (TFA)
  • HY-W583271
    Zn(II) Deuteroporphyrin IX 2,4 bis ethylene glycol
    		Inhibitor
    Zn(II) Deuteroporphyrin IX 2,4 bis ethylene glycol is a heme oxygenase (HO) inhibitor, and inhibiting HO activity can reduce the release of hypothalamic hormones like AVP, OT, and ANP caused by hyperosmolarity. Zn(II) Deuteroporphyrin IX 2,4 bis ethylene glycol can be used for research on hyperbilirubinemia.
    Zn(II) Deuteroporphyrin IX 2,4 bis ethylene glycol
  • HY-P4008
    [Deamino-4-valine, 8-D-arginine]-Vasopressin
    [Deamino-4-valine, 8-D-arginine]-Vasopressin (dVDAVP) is a highly potent and specific antidiuretic agent possessing protracted effects.
    [Deamino-4-valine, 8-D-arginine]-Vasopressin
  • HY-162118
    RGH-122
    RGH-122 (compound 43) is an orally active, potent, selective, and hV1a receptor antagonist with Ki value of 0.3 nM and IC50 of 0.9 nM. RGH-122 showes microsomal stability with CLint value of 13/28/25 μL/min/mg.
    RGH-122
  • HY-P4012
    [Asu1,6-Arg8]Vasopressin
    		Agonist
    [Asu1,6-Arg8]Vasopressin is an vasopressin agonist which potentiates cyclic AMP accumulation and ACTH release induced by corticotropin-releasing factor (CRF) in rat anterior pituitary cells in culture.
    [Asu1,6-Arg8]Vasopressin
Vasopressin Receptor Isoform Comparison

V1a Receptor 

V1b Receptor 

V2 Receptor 

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Please try each isoform separately.

Vasopressin Receptor Inhibitors, Agonists, Antagonists & Activators
Product NameV1a Receptor V1b Receptor V2 Receptor Purity    
Conivaptan hydrochloride  
V2 Receptor 
99.89%
Argipressin  
V2 Receptor 
99.82%
Tolvaptan  
V2 Receptor 
99.95%
V1a/V2 antagonist 1
human V1a Receptor, Ki: 0.13 nM
human V1a Receptor, IC50: 2.2 nM
 
human V2 Receptor, Ki: 0.53 nM
Lixivaptan  
V2 Receptor 
99.67%
Mozavaptan  
V2 Receptor 
99.71%
Mozavaptan hydrochloride  
V2 Receptor 
99.89%
Fedovapagon  
V2 Receptor , EC50: 24 nM
99.43%
Vasopressin Dimer (parallel) (TFA)  
V2 Receptor 
99.55%
TC OT 39
Avprla vasopressin receptor, Ki: 300 nM
  
Vasopressin Dimer (anti-parallel) (TFA)  
V2 Receptor 
Mozavaptan-d6  
V2 Receptor 
Pecavaptan
human V1a Receptor, IC50: 3.6 nM
canine V1a Receptor, IC50: 4.4 nM
 
human V2 Receptor, IC50: 1.7 nM
canine V2 Receptor, IC50: 1.3 nM
Conivaptan  
V2 Receptor 
L-364918  
V2 Receptor , Ki: 2400 nM
YM218 free base
Rat liver V1a Receptor, Ki: 0.5 nM
Rat pituitary V1b receptor, Ki: 1510 nM
Rat kidney V2 receptor, Ki: 72.2 nM
Tolvaptan-d7  
V2 Receptor