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-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-18347A
    Conivaptan hydrochloride
    		Antagonist 99.95%
    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 98.71%
    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-17572
    Atosiban
    		Antagonist 99.44%
    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-18345
    SR 49059
    		Antagonist 99.33%
    SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM.
    SR 49059
  • HY-165456
    AGN-190851
    		Inhibitor
    AGN-190851 is a potent and selective agonist of α2-adrenergic receptor (α2 adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α2-adrenergic receptor subtypes, and parturition.
    AGN-190851
  • HY-W752502
    Docarpamine
    		Activator
    Docarpamine is an orally active dopamine prodrug that can be hydroxylated in the small intestine and liver to form active dopamine. Docarpamine mainly activates D1-like receptors in peripheral blood vessels to lower blood pressure and heart rate in a state of spontaneous hypertension. Docarpamine exerts a pressor and tachycardic effect by activating D1-like receptors, vasopressin V1 receptors, and α-adrenergic receptors in normal blood pressure conditions. Docarpamine can be used for research on renal vascular dilation and diuresis.
    Docarpamine
  • HY-133173
    Niravoline
    Niravoline (RU51599) is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. Niravoline has a pure water diuresis effect without associated electrolyte excretion. Niravoline can reduce brain oedema following transient forebrain ischaemia in rats.
    Niravoline
  • HY-12554A
    Terlipressin diacetate
    		Agonist 98.86%
    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-17572A
    Atosiban acetate
    		Antagonist 98.87%
    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-10066
    Nelivaptan
    		Antagonist 99.89%
    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, anxiety and depression.
    Nelivaptan
  • HY-18346
    Mozavaptan
    		Antagonist 99.71%
    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 99.34%
    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-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-105239
    Selepressin
    		Agonist 98.17%
    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
  • HY-14185
    Lixivaptan
    		Antagonist 99.67%
    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-B0662
    Imidafenacin
    		Inhibitor 99.26%
    Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder.
    Imidafenacin
  • HY-P1163A
    D[LEU4,LYS8]-VP TFA
    		Agonist 98.97%
    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.
    D[LEU4,LYS8]-VP TFA
  • HY-123593
    Mozavaptan hydrochloride
    		Antagonist 99.80%
    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-W158030
    2-Guanidinobezimidazole
    		Inhibitor
    2-Guanidinobezimidazole (2GBI) is a NLRP3 agonist with a KD of 1.29 μM and a selective state-dependent HVCN1 blocker. 2-Guanidinobezimidazole directly binds NLRP3’s LRR domain, enhances NLRP3-ASC and NLRP3-NEK7 interactions, and drives NLRP3 inflammasome activation. 2-Guanidinobezimidazole can be used for the research of LLC lung carcinoma, B16F10 melanoma and ischemic stroke.
    2-Guanidinobezimidazole
Vasopressin Receptor Isoform Comparison

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