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-107037
    Tolmesoxide
    		Antagonist
    Tolmesoxide (RX71107) is a peripheral vascular dilator with blood pressure lowering activity. Tolmesoxide has shown direct vasodilation in the human forearm arterial bed and dorsal hand vein. Tolmesoxide can dose-dependently increase blood flow in the forearm and produce dilation during contraction of the dorsal hand veins. Tolmesoxide can be used to study high blood pressure and angina.
    Tolmesoxide
  • HY-N12638
    Endolide F
    		Antagonist
    Endolide F (Compound 2) is a proline-containing lactone. Endolide F is a moderate antagonist of the arginine antidiuretic hormone V1A receptor.
    Endolide F
  • HY-16783
    Ribuvaptan
    		Antagonist
    Ribuvaptan is a vasopressin receptor antagonist. Ribuvaptan can be used for the study of Heart failure.
    Ribuvaptan
  • HY-P4009
    [Lys8] Vasopressin Desglycinamide
    [Lys8] Vasopressin Desglycinamide is a vasopressin analog, used for the maintenance of active and passive avoidance behavior. [Lys8] Vasopressin Desglycinamide facilitates memory consolidation processes.
    [Lys8] Vasopressin Desglycinamide
  • HY-178573
    V1b Receptor antagonist-1
    		Antagonist
    V1b receptor antagonist-1 is a potent, selective and brain-penetrant vasopressin 1b (V1b) receptor antagonist. V1b receptor antagonist-1 exhibits anti-depressant activity. V1b receptor antagonist-1 can be used for the research of neurological disease, such as depression.
    V1b Receptor antagonist-1
  • HY-172427
    Elsovaptan
    		Antagonist
    Elsovaptan is the antagonist for vasopressin receptor that can be used in researchs of Alzheimer disease.
    Elsovaptan
  • 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-124275
    ML389
    		Antagonist
    ML389 is a highly selective vasopressin 1a (V1a) receptor antagonist (IC50=40 nM). ML389 is promising for research of central nervous system disorders such as anxiety, depression, and post-traumatic stress disorder (PTSD).
    ML389
  • HY-109133
    Pecavaptan
    		Inhibitor
    Pecavaptan, a chemical probe, 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-B0662A
    Imidafenacin hydrochloride
    		Inhibitor
    Imidafenacin (KRP-197; ONO-8025) hydrochloride is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin hydrochloride potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin hydrochloride can be used in research related to overactive bladder.
    Imidafenacin hydrochloride
  • 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-P1747
    Pneumadin, rat
    Pneumadin, rat (PNM) is a decapeptide, which possess a potent stimulating effect on arginine-vasopressin (AVP) release. Pneumadin, rat (PNM) exerts a marked antidiuretic effect in animals with functional AVP system.
    Pneumadin, rat
  • 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-18347
    Conivaptan
    		Antagonist
    Conivaptan (YM 087 free base) is antagonist for vasopressin V1A receptor and vasopressin V2 receptor. Conivaptan ameliorates congestive heart failure, improves cardiac systolic function.
    Conivaptan
  • HY-105685R
    SRX246 (Standard)
    		Antagonist
    SRX246 (Standard) is the analytical standard of SRX246 (HY-105685). This product is intended for research and analytical applications. 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 (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
Vasopressin Receptor Isoform Comparison

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