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.

Vasopressin Receptor Related Products (38):

Cat. No. Product Name Effect Purity
  • HY-P0049
    Argipressin
    Agonist 99.82%
    Argipressin (Arg8-vasopressin) 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.
  • HY-17572A
    Atosiban acetate
    Antagonist 99.56%
    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-17000
    Tolvaptan
    Antagonist 99.96%
    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 induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia.
  • 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-14185
    Lixivaptan
    Antagonist 99.46%
    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-18345
    SR 49059
    Antagonist ≥98.0%
    SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM.
  • HY-105239
    Selepressin
    Agonist
    Selepressin (FE 202158) is a selective vasopressin V1A receptor agonist. Selepressin is a potent vasopressor. Selepressin can be used in the research of septic shock.
  • 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.
  • HY-109024
    Balovaptan
    Antagonist 99.25%
    Balovaptan (RG7314) is an orally available, 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-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-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-105685
    SRX246
    Antagonist 98.77%
    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-123593
    Mozavaptan hydrochloride
    Antagonist 98.16%
    Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride 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 hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.
  • 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-14887
    Fedovapagon
    Agonist 99.14%
    Fedovapagon (VA106483) is a selective and orally active vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM. Fedovapagon can be used in the research of nocturia.
  • 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-A0182
    Felypressin
    Agonist
    Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.
  • 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-18346
    Mozavaptan
    Antagonist 99.64%
    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-19381
    WAY-151932
    Agonist 99.73%
    WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay.