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

Vasopressin 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-162394
    Vasopressin V2 receptor antagonist 2
    		Antagonist
    Vasopressin V2 receptor antagonist 2 (Compound 33) is an antagonist of the arginine vasopressin V2 receptor (V2R) with a Ki value of 6.2 nM. Vasopressin V2 receptor antagonist 2 can effectively reduce cAMP levels, thereby inhibiting the growth of renal cysts[1].
    Vasopressin V2 receptor antagonist 2
  • HY-P4678
    (Phe2,Orn8)-Oxytocin
    		Agonist
    (Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM.
    (Phe2,Orn8)-Oxytocin
  • 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-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
  • HY-P0041
    F992
    		Inhibitor
    F992 is an antidiuretic peptide and vasopressin (antidiuretic hormone) analogue.
    F992
  • HY-P3213
    Dp[Tyr(methyl)2,Arg8]-Vasopressin
    		Antagonist
    Dp[Tyr(methyl)2,Arg8]-Vasopressin is a non-selective peptide arginine vasopressin Vlb receptor antagonist.
    Dp[Tyr(methyl)2,Arg8]-Vasopressin
  • HY-W104304
    2-(3-Trifluoromethylphenyl)glycine hydrochloride
    		Antagonist
    2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research.
    2-(3-Trifluoromethylphenyl)glycine hydrochloride
  • HY-P5010
    (D-Arg8)-Inotocin
    		Antagonist
    (D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R.
    (D-Arg8)-Inotocin
  • HY-P1163
    D[LEU4,LYS8]-VP
    		Agonist
    D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
    D[LEU4,LYS8]-VP
  • HY-P4678A
    (Phe2,Orn8)-Oxytocin acetate
    		Agonist
    (Phe2,Orn8)-Oxytocin acetate is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin acetate induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM.
    (Phe2,Orn8)-Oxytocin acetate
  • HY-N12638
    Endolide F
    		Antagonist
    Endolide F (Compound 2) is a proline-containing lactone. Endolide F is a moderate antagonist of the arginine antidiuretic hormone V1A receptor.
    Endolide F
  • HY-W539944
    Argipressin acetate
    		Agonist
    Argipressin (Arg8-vasopressin) (acetate) binds to the V1, V2, V3-vascular arginine vasopressin receptor, with a Kd value of 1.31 nM in A7r5 rat aortic smooth muscle cells for V1.
    Argipressin acetate
Vasopressin Receptor Isoform Comparison

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