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-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-157220
    Tolvaptan phosphate ester sodium
    		Antagonist 99.85%
    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-P5213
    Vasopressin Dimer (parallel) (TFA)
    		Activator 99.55%
    Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR.
    Vasopressin Dimer (parallel) (TFA)
  • HY-P4683A
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate
    		Antagonist 99.81%
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats.
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate
  • 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-P4683
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
    		Antagonist
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats.
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
  • 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
  • HY-P1810
    c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm
    		Agonist
    c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.25 and 0.05 nM for hV2R and rV2R, respectively.
    c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm
  • HY-P1809
    Velmupressin
    		Agonist
    Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) 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
  • HY-159507
    Brezivaptan
    		Antagonist
    Brezivaptan (Brezivaptanum; TH1773; TS-121) is a vasopressin receptor antagonist.
    Brezivaptan
  • HY-P0049A
    Argipressin diacetate
    		Agonist
    Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)) is a 9 amino acid neuropeptide secreted by the posterior pituitary. Argipressin (diacetate) (AVP (diacetate)) can regulate the biological effects of fluid balance, osmolality and cardiovascular through three separate G-protein coupled receptors (GPCRs), namely Avpr1a (V1a), Avpr1b (V1b) and Avpr2 (V2). Argipressin (diacetate) (AVP (diacetate)) also have potentially important effects on centrally regulated metabolic processes.
    Argipressin diacetate
  • HY-P1390A
    d[Cha4]-AVP TFA
    		Agonist
    d[Cha4]-AVP TFA is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. d[Cha4]-AVP TFA shows more selective for V1b receptor than human V1a receptor, V2 receptor, and oxytocin receptors.
    d[Cha4]-AVP TFA
  • HY-146272
    Vasopressin V2 receptor antagonist 1
    		Antagonist
    Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM. Vasopressin V2 receptor antagonist 1 can be used for autosomal dominant polycystic kidney disease (ADPKD) research.
    Vasopressin V2 receptor antagonist 1
  • HY-168742
    V1a/V2 antagonist 1
    		Antagonist
    V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice.
    V1a/V2 antagonist 1
  • HY-P4201
    JKC 301
    		Antagonist
    JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking.
    JKC 301
  • HY-114594
    Khusimol
    		Ligand
    Khusimol is a compound used in chemotherapy for oral squamous cell carcinoma.
    Khusimol
  • HY-139572
    Enuvaptan
    		Antagonist
    Enuvaptan (BAY-2327949) is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases.
    Enuvaptan
  • HY-P2539
    Big Endothelin-1 (1-39), porcine
    		Agonist
    Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide. Big Endothelin-1 (1-39), porcine has similar pressor effects in vivo.
    Big Endothelin-1 (1-39), porcine
  • 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-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
Vasopressin Receptor Isoform Comparison

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