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-P1163A
    D[LEU4,LYS8]-VP TFA
    		Agonist 99.29%
    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-117820
    TASP0390325
    		Antagonist 99.67%
    TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.
    TASP0390325
  • HY-105239
    Selepressin
    		Agonist 99.34%
    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-15009
    Fuscoside
    		Antagonist ≥98.0%
    Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
    Fuscoside
  • HY-14887
    Fedovapagon
    		Agonist 99.43%
    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-19381
    WAY-151932
    		Agonist 99.44%
    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.
    WAY-151932
  • HY-P1390
    d[Cha4]-AVP
    		Agonist 98.81%
    d[Cha4]-AVP is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors.
    d[Cha4]-AVP
  • HY-P1185
    Antagonist G
    		Antagonist 99.05%
    Antagonist G 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
  • HY-P3066
    SKF 100398
    		99.48%
    SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
    SKF 100398
  • HY-P4678
    (Phe2,Orn8)-Oxytocin
    		Agonist 98.22%
    (Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM.
    (Phe2,Orn8)-Oxytocin
  • HY-P0041A
    F992 TFA
    		Inhibitor 98.19%
    F992 TFA is an antidiuretic peptide and vasopressin (antidiuretic hormone) analogue.
    F992 TFA
  • HY-116567
    OPC-51803
    		Agonist 99.77%
    OPC-51803 is an orally active nonpeptide vasopressin V2 receptor agonist. OPC-51803 can be used for the research of micturition disorders that result in frequent micturition, such as that from polyuria, nocturnal polyuria, and some kinds of urinary incontinence.
    OPC-51803
  • HY-P1809A
    Velmupressin acetate
    		Agonist 99.47%
    Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) acetate is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively.
    Velmupressin acetate
  • HY-108678
    TC OT 39
    		Antagonist
    TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models.
    TC OT 39
  • HY-12981
    RG7713
    		Antagonist 99.92%
    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).
    RG7713
  • HY-A0182
    Felypressin
    		Agonist 99.62%
    Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.
    Felypressin
  • HY-109181
    Lazuvapagon
    		Agonist
    Lazuvapagon (SK-1404) is a vasopressin V2 receptor agonist for the research of nocturia.
    Lazuvapagon
  • HY-159507
    Brezivaptan
    		Antagonist
    Brezivaptan (Brezivaptanum; TH1773; TS-121) is a vasopressin receptor antagonist.
    Brezivaptan
  • HY-12554B
    Terlipressin acetate
    		Agonist 98.46%
    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.
    Terlipressin acetate
  • HY-162394
    Vasopressin V2 receptor antagonist 2
    		Antagonist 99.81%
    Vasopressin V2 receptor antagonist 2 (Compound 33) is an antagonist of the arginine vasopressin V2 receptor (V2R) with a Ki value of 6.2 nM. Vasopressin V2 receptor antagonist 2 can effectively reduce cAMP levels, thereby inhibiting the growth of renal cysts[1].
    Vasopressin V2 receptor antagonist 2
Vasopressin Receptor Isoform Comparison

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