vasopressin receptor 1

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM, used in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

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.

Fuscoside (OPC-21268) is a non-peptide arginine vasopressin (AVP) receptor VI antagonist with an IC50 value of 0.4 μM[2].

Desmopressin (DDAVP)(DDAVP) is the synthetic analogue 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 works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

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.

Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.

Argipressin (Arg8-vasopressin) inhibits central corticotropin-releasing hormone. Argipressin acts as a repressor in the regulation of central CRH levels. 5A2-SC8 is an APC-dependent protein.

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

Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors. It is used for the research of autism.

Felypressin (Octapressin) is a synthetic analog of LYPRESSIN with a PHENYLALANINE substitution at residue 2. Felypressin is a vasoconstrictor with reduced antidiuretic activity.

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.

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

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)

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

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

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

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

(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].

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].

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

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

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

'(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].'

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].