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

Vasopressin Receptor

Vasopressin receptors are a family of tissue-specific G protein-coupled receptors, which classified into V1, V2 and V3 subtypes. These three subtypes differ in localization, function and signal transduction mechanisms. Although all three of these proteins are G-protein coupled receptors (GPCRs), activation of AVPR1A and AVPR1B stimulate phospholipase C, while activation of AVPR2 stimulates adenylate cyclase. These three receptors for vasopressin have unique tissue distributions. AVPR1A are expressed in vascular smooth muscle cells, hepatocytes, platelets, brain cells, and uterus cells. AVPR1B are expressed in cells of the anterior pituitary and throughout the brain, especially in the pyramidal neurons of the hippocampal CA2 field. AVPR2 are expressed in the kidney tubule, predominantly in the distal convoluted tubule and collecting ducts, in fetal lung tissue and lung cancer, the last two being associated with alternative splicing. AVPR2 is also expressed in the liver where stimulation releases a variety of clotting factors into the bloodstream.

Vasopressin Receptor Related Products (27):

Cat. No. Product Name Effect Purity
  • HY-P0049
    Argipressin Agonist 99.82%
    Argipressin 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 is a selective V2 agonist.
  • HY-17572
    Atosiban Antagonist 99.09%
    Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
  • HY-17000
    Tolvaptan Antagonist 99.92%
    Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.
  • HY-18347A
    Conivaptan hydrochloride Antagonist 99.92%
    Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.
  • HY-A0182
    Felypressin Agonist 99.68%
    Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.
  • HY-17572A
    Atosiban acetate Antagonist 99.92%
    Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
  • HY-P1390A
    d[Cha4]-AVP TFA Agonist
    d[Cha4]-AVP TFA is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP TFA stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
  • 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.
  • HY-14185
    Lixivaptan Antagonist 99.90%
    Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.
  • HY-109024
    Balovaptan Antagonist 99.18%
    Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
  • HY-15009
    Fuscoside Antagonist >98.0%
    Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
  • HY-12554
    Terlipressin Agonist
    Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
  • HY-12554A
    Terlipressin acetate Agonist 99.76%
    Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
  • HY-18346
    Mozavaptan Antagonist 99.89%
    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.
  • HY-105685
    SRX246 Antagonist 99.69%
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
  • HY-12981
    RG7713 Antagonist 99.79%
    RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
  • HY-14887
    Fedovapagon Agonist 99.03%
    Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia.
  • HY-15010
    L-371,257 Antagonist >99.0%
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
  • HY-A0182A
    Felypressin acetate Agonist
    Felypressin acetate (PLV-2 acetate) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin acetate is widely used in dental procedures.
  • HY-P1163A
    D[LEU4,LYS8]-VP TFA Agonist
    D[LEU4,LYS8]-VP TFA 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 TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
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