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

Vasopressin Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-116567
    OPC-51803
    Agonist
    OPC-51803 is an orally active nonpeptide vasopressin V2 receptor agonist. OPC-51803 can be used for the research of micturition disorders that result in frequent micturition, such as that from polyuria, nocturnal polyuria, and some kinds of urinary incontinence.
    OPC-51803
  • HY-157220
    Tolvaptan phosphate ester sodium
    Antagonist
    Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation.
    Tolvaptan phosphate ester sodium
  • 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-172427
    Elsovaptan
    Antagonist
    Elsovaptan is the antagonist for vasopressin receptor that can be used in researchs of Alzheimer disease.
    Elsovaptan
  • 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
  • HY-P1162
    (d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin
    Antagonist
    (d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin (SKF 100273) is a vasopressin V1 receptor selective antagonist.
    (d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin
  • HY-109133
    Pecavaptan
    Inhibitor
    Pecavaptan is an orally active and dual antagonist of V1a/V2 receptor (Ki=0.5 nM and 0.6 nM for human, respectively). Pecavaptan promotes an increase in urine production, which reduces the associated symptoms of water retention and edema.
    Pecavaptan
  • HY-P10046
    [Deamino-Pen1,Val4,D-Arg8]-vasopressin
    Inhibitor
    [Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an arginine-vasopressin (AVP) antagonist. AVP-A can significantly lower plasma aldosterone concentration in rats. AVP-A can be used for the research of the growth and steroidogenic capacity of rat adrenal zona glomerulosa.
    [Deamino-Pen1,Val4,D-Arg8]-vasopressin

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