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-18347A
    Conivaptan hydrochloride
    		Antagonist 99.88%
    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.
    Conivaptan hydrochloride
  • 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.
    Argipressin
  • HY-17000
    Tolvaptan
    		Antagonist 99.95%
    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.
    Tolvaptan
  • HY-17572A
    Atosiban acetate
    		Antagonist 99.88%
    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.
    Atosiban acetate
  • HY-18345
    SR 49059
    		Antagonist 99.92%
    SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM.
    SR 49059
  • HY-168742
    V1a/V2 antagonist 1
    		Antagonist
    V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice.
    V1a/V2 antagonist 1
  • 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-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-17572
    Atosiban
    		Antagonist 99.55%
    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.
    Atosiban
  • HY-14185
    Lixivaptan
    		Antagonist 99.30%
    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.
    Lixivaptan
  • HY-12554A
    Terlipressin diacetate
    		Agonist 99.76%
    Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
    Terlipressin diacetate
  • HY-A0182A
    Felypressin acetate
    		Agonist 98.31%
    Felypressin acetate (PLV-2 acetate) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin acetate is widely used in dental procedures.
    Felypressin acetate
  • 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.
    Mozavaptan
  • HY-15010
    L-371,257
    		Antagonist 99.90%
    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).
    L-371,257
  • HY-123593
    Mozavaptan hydrochloride
    		Antagonist 99.89%
    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.
    Mozavaptan hydrochloride
  • 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.
    SRX246
  • 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.
    Fedovapagon
  • HY-117820
    TASP0390325
    		Antagonist ≥99.0%
    TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.
    TASP0390325
  • HY-109024
    Balovaptan
    		Antagonist 99.89%
    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.
    Balovaptan
  • HY-10066
    Nelivaptan
    		Antagonist 98.35%
    Nelivaptan (SSR-149415) is a selective and orally active vasopressin V1b Receptor antagonist (Ki: 3.7 and 1.3 nM for native and recombinant rat V1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca2+ increase and corticotropin secretion. Nelivaptan can be used for research of stress and anxiety.
    Nelivaptan
Vasopressin Receptor Isoform Comparison

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