vasopressin 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).

Barbadin is a novel and specific inhibitor of β-arrestin β2-adaptin interaction with an IC50 value of 19.1 μM for β-arestin1 and 15.6 μM for β-arestin2. Barbadin potentiates the long term effects of lorcaserin on POMC neurons and weight loss. Barbadin potentiates the long-term effects of lorcaserin on POMC neurons and weight loss, blocks agonist-promoted endocytosis of prototypic β2-adrenergic, V2-vasopressin, and angiotensin-II-1 receptors, and may be useful in the study of obesity.

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.

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

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.

Desmopressin acetate is a synthetic replacement for vasopressin, which reduces urine production. Medical use of Desmopressin acetate includes: (a) bed wetting; (b) diabetes insipidus; (c) nighttime urination; (d) clotting disorders.

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

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.

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)

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.

(S)-Bromoenol lactone ((S)-BEL) inhibits the arachidonate release induced by vasopressin from cultured rat aortic smooth muscle (A10) cells with an IC50 of 2 μM. (S)-BEL is an irreversible, chiral, mechanism-based calcium-independent phospholipase A2β (iPLA2β) inhibitor [1].

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.

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

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.

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].

Antagonist G TFA is a potent antagonist of vasopressin and exhibits weaker antagonistic effects on GRP and Bradykinin. Additionally, this compound promotes AP-1 transcription and enhances cellular sensitivity to chemotherapy [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].

[Asu1,6-Arg8]Vasopressin is a vasopressin agonist that enhances cyclic AMP accumulation and adrenocorticotropic hormone (ACTH) release triggered by corticotropin-releasing factor (CRF) in cultured rat anterior pituitary cells [1] [2].

[8-L-arginine] deaminovasopressin (dAVP) is a vasopressin analog [1].

(Phe2,Orn8)-Oxytocin, a selective V1 vasopressin agonist, exhibits sustained contractility in rabbit epididymis, achieving an EC50 value of 280 nM [1].

(Phe2,Orn8)-Oxytocin acetate, a selective V1 vasopressin agonist, demonstrates pronounced contractility induction in rabbit epididymis, characterized by a sustained response with an EC50 value of 280 nM [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].

Oxytocin Parallel Dimer TFA, a disulfide-bridged homopeptide dimer, exhibits both oxytocin and vasopressin-like activity while being less toxic than oxytocin [1] [2].