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-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
  • 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-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-107037
    Tolmesoxide
    		Antagonist
    Tolmesoxide (RX71107) is a peripheral vascular dilator with blood pressure lowering activity. Tolmesoxide has shown direct vasodilation in the human forearm arterial bed and dorsal hand vein. Tolmesoxide can dose-dependently increase blood flow in the forearm and produce dilation during contraction of the dorsal hand veins. Tolmesoxide can be used to study high blood pressure and angina.
    Tolmesoxide
  • 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
  • HY-P4009
    [Lys8] Vasopressin Desglycinamide
    [Lys8] Vasopressin Desglycinamide is a vasopressin analog, used for the maintenance of active and passive avoidance behavior. [Lys8] Vasopressin Desglycinamide facilitates memory consolidation processes.
    [Lys8] Vasopressin Desglycinamide
  • HY-18346S
    Mozavaptan-d6
    		Antagonist
    Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
    Mozavaptan-d<sub>6</sub>
  • HY-P1185A
    Antagonist G TFA
    		Antagonist
    Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
    Antagonist G TFA
Vasopressin Receptor Isoform Comparison

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