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-123593R
    Mozavaptan hydrochloride (Standard)
    		Antagonist
    Mozavaptan (hydrochloride) (Standard) is the analytical standard of Mozavaptan (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-P5006
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin
    		Antagonist
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin (d(CH2)5[Tyr(Me)2, Dab5]AVP) is a specific antagonist of vasopressin V1a receptor, with a pA2 of 6.71.
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin
  • HY-19880
    RWJ-676070
    		Antagonist
    RWJ-676070 is a dual vasopressin V(1A)/V(2) receptor antagonist with an Ki value of 1.4 nM and 14 nM respectly.
    RWJ-676070
  • HY-172814A
    OT-R agonist 1 TFA
    		Antagonist
    OT-R agonist 1 TFA (compound 5) is an oxytocin receptor agonist with an EC50 of 0.39 nM. OT-R agonist 1 TFA shows V1A antagonist activity with an EC50 of 2432 nM and can be used for study of CNS disorders.
    OT-R agonist 1 TFA
  • HY-118918
    YM218 free base
    		Antagonist
    YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease.
    YM218 free base
  • HY-18346R
    Mozavaptan (Standard)
    		Antagonist
    Mozavaptan (Standard) is the analytical standard of Mozavaptan. This product is intended for research and analytical applications. 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 (Standard)
  • HY-14185R
    Lixivaptan (Standard)
    		Antagonist
    Lixivaptan (Standard) is the analytical standard of Lixivaptan. This product is intended for research and analytical applications. 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 (Standard)
  • HY-109024R
    Balovaptan (Standard)
    		Antagonist
    Balovaptan (Standard) is the analytical standard of Balovaptan (HY-109024). This product is intended for research and analytical applications. 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 (Standard)
  • HY-17000A
    (R)-(+)-Tolvaptan
    		Control
    (R)-(+)-Tolvaptan ((R)-(+)-OPC-41061) is the (R)-(+) enantiomer of Tolvaptan (HY-17000). Tolvaptan (OPC-41061) is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist.
    (R)-(+)-Tolvaptan
  • HY-17572AR
    Atosiban acetate (Standard)
    		Antagonist
    Atosiban (acetate) (Standard) is the analytical standard of Atosiban (acetate). This product is intended for research and analytical applications. 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 (Standard)
  • 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-105239R
    Selepressin (Standard)
    		Agonist
    Selepressin (Standard) is the analytical standard of Selepressin (HY-105239). This product is intended for research and analytical applications. 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.
    Selepressin (Standard)
  • HY-18347AR
    Conivaptan hydrochloride (Standard)
    		Antagonist
    Conivaptan (hydrochloride) (Standard) is the analytical standard of Conivaptan (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-165423
    DM-4111
    		Inhibitor
    DM-4111, one of the major monohydroxyl metabolites of Tolvaptan (HY-17000), is a potent vasopressin V2 receptor inhibitor. DM-4111 inhibits water reabsorption in the renal tubules, thereby promoting the excretion of electrolyte-free water. DM-4111 is promising for research of cardiovascular diseases.
    DM-4111
  • HY-17000R
    Tolvaptan (Standard)
    		Antagonist
    Tolvaptan (Standard) is the analytical standard of Tolvaptan. This product is intended for research and analytical applications. 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 (Standard)
  • HY-17000S
    Tolvaptan-d7
    		Antagonist
    Tolvaptan-d7 is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.
    Tolvaptan-d<sub>7</sub>
  • HY-12554AR
    Terlipressin diacetate (Standard)
    		Agonist
    Terlipressin (diacetate) (Standard) is the analytical standard of Terlipressin (diacetate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-129557
    A-49816
    A-49816 is an orally active diuretic that increases urine volume and sodium and chloride excretion. A-49816 at high doses (12.5, 15, and 20 mg) caused significant salt and chloride excretion and diuresis in experimental animals.
    A-49816
  • HY-120247
    TASP0434299
    		Ligand
    TASP0434299 (Compound 10) is a labeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography.
    TASP0434299
Vasopressin Receptor Isoform Comparison

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