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-157220
    Tolvaptan phosphate ester sodium
    		Antagonist
    Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. 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 phosphate ester sodium
  • HY-18346S
    Mozavaptan-d6
    		Antagonist
    Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. 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-d<sub>6</sub>
  • HY-P1185A
    Antagonist G TFA
    		Antagonist
    Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
    Antagonist G TFA
  • 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-109133
    Pecavaptan
    		Inhibitor
    Pecavaptan is an orally active and dual antagonist of V1a/V2 receptor (Ki=0.5 nM and 0.6 nM for human, respectively). Pecavaptan promotes an increase in urine production, which reduces the associated symptoms of water retention and edema.
    Pecavaptan
  • HY-P10046
    [Deamino-Pen1,Val4,D-Arg8]-vasopressin
    		Inhibitor
    [Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an arginine-vasopressin (AVP) antagonist. AVP-A can significantly lower plasma aldosterone concentration in rats. AVP-A can be used for the research of the growth and steroidogenic capacity of rat adrenal zona glomerulosa.
    [Deamino-Pen1,Val4,D-Arg8]-vasopressin
  • HY-P4994
    Val9-Oxytocin
    		Antagonist
    Val9-Oxytocin is a full antagonist of vasopressin (V1a) receptor. Val9-Oxytocin is an analog of Oxytocin (HY-17571A) in which changing Gly9 to Val9.
    Val9-Oxytocin
  • HY-P4010
    Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin
    		Agonist
    Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin, a synthetic analog of vasopressin (AVP), is a weak agonist at antidiuretic receptor. However, Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin is a potent agonist at pituitary corticotrope receptor.
    Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin
  • HY-P10325
    Kalata B7
    		Agonist
    Kalata B7 is a cyclotide that can be isolated from Oldenlandia affinis DC (Rubiaceae) and possesses membrane-permeating capabilities. Kalata B7 is also a partial agonist of oxytocin and vasopressin V1a receptors.
    Kalata B7
  • HY-P4237
    [8-L-arginine] deaminovasopressin
    		Modulator
    [8-L-arginine] deaminovasopressin (dAVP) is a vasopressin analog.
    [8-L-arginine] deaminovasopressin
  • HY-17572R
    Atosiban (Standard)
    		Antagonist
    Atosiban (Standard) is the analytical standard of Atosiban. This product is intended for research and analytical applications. 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 (Standard)
  • HY-129333
    L-364918
    		Antagonist
    L-364918 is a potent and selective oxytocin and arginine vasopressin antagonist with Ki values of 30, 1300, 2400 nM for OT, AVP-V1, AVP-V2, respectively. L-364918 has the potential for the research of preterm labor and disturbances in water balance.
    L-364918
  • 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-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-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-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-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[1][2].
    Tolvaptan-d<sub>7</sub>
Vasopressin Receptor Isoform Comparison

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