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-114594
    Khusimol
    		Ligand
    Khusimol is a compound used in chemotherapy for oral squamous cell carcinoma.
    Khusimol
  • 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-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-133173
    Niravoline
    Niravoline (RU51599) is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. Niravoline has a pure water diuresis effect without associated electrolyte excretion. Niravoline can reduce brain oedema following transient forebrain ischaemia in rats.
    Niravoline
  • 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-105652
    Ambucetamide
    		Inhibitor
    Ambucetamide is an antispasmodic agent. Ambucetamide alleviates menstrual pain.
    Ambucetamide
  • 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-18344
    Satavaptan
    		Antagonist
    Satavaptan (SR 121463) is an antagonist for vasopressin V2 receptor. Satavaptan regulates the vasopressin regulated phosphopeptides and vasopressin-mediated signaling pathway. Satavaptan is potential in ameliorating hyponatremia.
    Satavaptan
  • 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-A0182R
    Felypressin (Standard)
    		Agonist
    Felypressin (Standard) is the analytical standard of Felypressin. This product is intended for research and analytical applications. Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.
    Felypressin (Standard)
  • 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-111225
    VA-111913
    		Antagonist
    VA-111913 (VT-913) is a vasopressin receptor V1A antagonist (Ki = 1.74 nM). VA-111913 reduces uterine contractions and improves uterine blood flow by inhibiting vasopressin, thereby alleviating dysmenorrhea. VA-111913 can be used for research on menstrual pain.
    VA-111913
  • HY-180142
    XYDC2050
    		Antagonist
    XYDC2050 (Compound 29) is a selective vasopressin V2 receptor (V2R) antagonist with an IC50 of 27 nM and a Ki of 2.8 nM. XYDC2050 shows a Ki of 420.7 nM (SI = 162 fold) for V1R. XYDC2050 can inhibit Vasopressin (HY-B1811)-induced intracellular cyclic adenosine monophosphate (cAMP) accumulation with an IC50 of 12 nM. XYDC2050 can inhibit the growth of renal cysts, reduce the ratio of kidney weight to body weight and decrease the area of cysts and the cystic index. XYDC2050 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).
    XYDC2050
  • 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
Vasopressin Receptor Isoform Comparison

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