vasopressin receptor

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2receptor (V2R) antagonist (Ki: 3.8 nM). dominant polycystic kidney disease (ADPKD).

Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist.

Fuscoside (OPC 21268) is a non-peptide Arginine vasopressin(AVP) Receptor V antagonist.

d[Cha4]-AVP acetate is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopr

d[Leu4,Lys8]-VP acetate is a selective vasopressin V1b receptor agonist. The Kis for rat, human and mouse V1b receptors are 0.16 nM, 0.52 nM and 0.1.38 nM, respectively. d[Leu4,Lys8]-VP acetate exhibits weak antidiuretic, vasopressor and oxytocic activiti

Conopressin S acetate(111317-90-9 free base) (Con-S acetate) is a natural product isolated from Conus striatus, shows high affinity with vasopressin V1b receptor (AVPR1B), with a Ki of 8.3 nM.

Vasopressin acetate is a peptide hormone with vasoconstrictive and antidiuretic activities that binds to the vascular arginine vasopressin receptor, V1, with Kd values of 1.31 and 1.44 nM in A7r5 rat aortic smooth muscle cells and neonatal rat cardiomyocy

Desmopressin acetate (16679-58-6 free base) (DDAVP) is the synthetic analog of the antidiuretic hormone arginine vasopressin. Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin acetate (16679-58-6 free base) works by limiting the amount of water that is eliminated in the urine. Desmopressin acetate (16679-58-6 free base) binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates the release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Selective vasopressin V1B receptor agonist (Ki values are 0.16, 64, 100 and 3800 nM for V1B, oxytocin, V2 and V1A receptors respectively). Displays weak antidiuretic, vasopressor and in vitro oxytocic activities.

Satavaptan fumarate is a selective antagonist of the non-peptide vasopressin V2 receptor.

Selepressin, an analog of vasopressin, is a potent, selective vasopressin V1a receptor agonist.

VA-111913, a vasopressin receptor antagonist, is used potentially for the treatment of dysmenorrhea.

Fedovapagon (VA106483) is a selective and potent agonist of the vasopressin V2 receptor (V2R) that inhibits the growth of intersegmental vessels in zebrafish. Fedovapagon can be used to study overactive bladder, nocturia, and painful bladder syndromes.

vasopressin V1A receptor antagonist

d[Cha4]-AVP TFA is a potent and selective agonist for the vasopressin (AVP) V1b receptor, displaying a high affinity with a K i of 1.2 nM. It exhibits greater selectivity for the V1b receptor over the V1a receptor, V2 receptor, and oxytocin receptors, demonstrating its specificity in targeting the human V1b receptor [1] [2].

Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin, a synthetic analog of vasopressin (AVP), acts as a weak agonist at the antidiuretic receptor but is a potent agonist at the pituitary corticotrope receptor [1].

SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V

Ribuvaptan is a antagonist of vasopressin receptor .

Potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.

(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin, a potent vasopressin V1 receptor (VP V1R) antagonist, significantly lowers mean arterial pressure (MAP) in rats [1].

D[LEU4,LYS8]-VP TFA is a selective agonist for the vasopressin V1b receptor, demonstrating Ki values of 0.16 nM, 0.52 nM, and 1.38 nM for rat, human, and mouse V1b receptors, respectively. This compound exhibits limited antidiuretic, vasopressor, and oxytocic activities in vitro [1] [2].

Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

Tolvaptan (OPC-41061) is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.

Val9-Oxytocin, an Oxytocin analog where Gly9 is substituted with Val9 [1], functions as a complete antagonist of the vasopressin (V1a) receptor.

Invopressin (Compound 42), a vasopressin V1A receptor partial agonist (EC50: 1.0 nM), is utilized in research related to cirrhosis conditions such as bacterial peritonitis, HRS2, and refractory ascites [1].

Conopressin S, isolated from Conus striatus, shows high affinity with vasopressin V1b receptor (AVPR1B), with a Ki of 8.3 nM.

YM-430 is a β1 adrenergic receptor antagonist and a calcium channel antagonist. YM430 could be both an antianginal and antihypertensive agent. YM430 (10(-8)-10(-6) M) inhibited 3,4-diaminopyridine-induced rhythmic contractions with an IC50 value of 59.2 n

L-368899 is a non-peptide and orally active antagonist of oxytocin receptor (IC50: 8.9 nM). It displays 40-fold selectivity over vasopressin V1a and V2 receptors (IC50: 370 and 570 nM respectively).

Satavaptan is a vasopressin V2 receptor antagonist. Satavaptan improves the control of ascites in cirrhosis.

YM 471 is a non-peptide arginine vasopressin (AVP) V1A and V2 receptor antagonist with oral activity.

Atosiban (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

VNA-932 is an agonist of the vasopressin V2-receptor (IC50: 80.3 nM and 778 nM in human-V2 binding and V1a binding assay).

Felypressin acetate (PLV-2) is an agonist of vasopressin 1 and acts on all arginine vasopressin receptors 1AS. Felypressin acetate can be used in dental procedures.

Terlipressin Acetate, a highly selective vasopressin V1 receptor agonist, on oxygen and glucose deprivation/re-oxygenation (OGD/R)-induced damage in intestinal epithelial cells (IEC-6).Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

PF-06478939 is a peptide that functions as an agonist at the oxytocin (OT) receptor and vasopressin receptor without crossing the blood-brain barrier. It exhibits EC50 values of 0.01 nM at the OT receptor and 0.078 nM at the vasopressin receptor [1].

(d(CH2)5[Tyr(Me)2, Dab5]AVP), a vasopressin V1a receptor-specific antagonist, demonstrates a pA2 value of 6.71 [1].

Dp[Tyr(Me)2,Arg8]-Vasopressin is a non-selective antagonist of the peptide arginine vasopressin V1b receptor [1].

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

Enuvaptan is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases.

YM 218 is a novel, potent, selective antagonist of nonpeptide vasopressin V1A receptor.

RWJ 676070 is an antagonist of vasopressin V1A/V2 receptor.

Pecavaptan is a vasopressin receptor antagonist.

Mozavaptan is a vasopressin receptor antagonist.

Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)

RG7713 (RO 5028442) has been used in trials studying Autistic Disorder.

'(D-Arg8)-Inotocin is a potent, selective, and competitive antagonist of the vasopressin receptor (V 1a R), exhibiting a binding affinity (K i) of 1.3 nM. It demonstrates over 3000-fold selectivity for the human V1aR compared to the OTR, V1bR, and V2R subtypes [1].'

Argipressin (Vasopressin) is a peptide hormone with vasoconstrictive and antidiuretic activities that binds to the vascular arginine vasopressin receptor, V1, with Kd values of 1.31 and 1.44 nM in A7r5 rat aortic smooth muscle cells and neonatal rat cardiomyocytes, respectively.

M-0002, a vasopressin V2 receptor antagonist, is used potentially for the treatment of ascites.