1. Signaling Pathways
  2. GPCR/G Protein
  3. Vasopressin Receptor

Vasopressin Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-105239A
    Selepressin acetate
    Agonist 98.04%
    Selepressin (FE 202158) acetate is a selective vasopressin V1A receptor agonist. Selepressin acetate is a potent vasopressin. Selepressin acetate can be used in the study of septic shock.
    Selepressin acetate
  • HY-19381
    WAY-151932
    Agonist 99.87%
    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-105685
    SRX246
    Antagonist 99.76%
    SRX246 is a potent, BBB-penetrant, highly selective 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-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-A0182
    Felypressin
    Agonist 99.74%
    Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.
    Felypressin
  • HY-P0083
    Ornipressin
    Agonist 99.87%
    Ornipressin (POR-8) is a vasopressin agonist specific for the V1 receptor. Ornipressin can be used as a local vasoconstrictor. Ornipressin can reverse the hypotension associated with combine general/epidural anesthesia. Ornipressin has antidiuretic activity. Ornipressin decreases renal vascular resistance and increases renal blood flow in renal failure model.
    Ornipressin
  • HY-W539944
    Argipressin acetate
    Agonist 99.16%
    Argipressin (Arg8-vasopressin) (acetate) 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 acetate
  • 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-A0182A
    Felypressin acetate
    Agonist 98.90%
    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-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-P4678
    (Phe2,Orn8)-Oxytocin
    Agonist 99.55%
    (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-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-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-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-P5535
    Invopressin
    99.40%
    Invopressin (Compound 42) is a vasopressin V1A receptor partial agonist (EC50: 1.0 nM). Invopressin can be used for research of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.
    Invopressin
  • 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-P2538
    Big Endothelin-1 (1-38), human
    Agonist 99.23%
    Big Endothelin-1 (1-38), human is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide.
    Big Endothelin-1 (1-38), human
  • 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-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
  • HY-P0083A
    Ornipressin acetate
    Agonist 99.63%
    Ornipressin (POR-8) acetate is a potent vasoconstrictor, hemostatic and renal agent. Ornipressin acetate is a vasopressin agonist specific for the V1 receptor. Ornipressin acetate can be used as a local vasoconstrictor. Ornipressin acetate can reverse the hypotension associated with combine general/epidural anesthesia. Ornipressin acetate has antidiuretic activity. Ornipressin acetate decreases renal vascular resistance and increases renal blood flow in renal failure model.
    Ornipressin acetate

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