vasopressin-v2

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 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).

Vasopressin V2 receptor antagonist 2 (Compound 33) is an arginine vasopressin V2 receptor (V2R) antagonist with a Ki of 6.2 nM. It effectively reduces cAMP levels, thereby inhibiting the growth of renal cysts.

Tolvaptan (OPC-41061) is an orally active, selective, competitive vasopressin receptor 2 (V2R) antagonist (IC50 = 1.28 μM) that inhibits AVP-induced platelet aggregation. Tolvaptan is used in studies of hyponatremia.

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.

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

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

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).

DM-4111, one of the primary monohydroxy metabolites of Tolvaptan, is an effective vasopressin V2 receptor (vasopressin V2 receptor) inhibitor. By inhibiting water reabsorption in renal tubules, it facilitates the excretion of electrolyte-free water. DM-4111 holds potential for research in cardiovascular diseases.

Conivaptan, a non-peptide inhibitor of antidiuretic hormone, was approved for hyponatremia caused by the syndrome of inappropriate antidiuretic hormone (SIADH), there is also some evidence that it may be effective in heart failure. Conivaptan inhibits sub

XYDC2050 (Compound 29) is a selective vasopressin V2 receptor (V2R) antagonist, with an IC50 of 27 nM and a Ki of 2.8 nM. It exhibits a Ki of 420.7 nM for V1R with a selectivity index of 162. XYDC2050 inhibits vasopressin-induced intracellular cyclic adenosine monophosphate (cAMP) accumulation with an IC50 of 12 nM. This compound can suppress kidney cyst growth, reduce kidney-to-body weight ratio, and decrease cyst area and cystic index, making it a candidate for autosomal dominant polycystic kidney disease (ADPKD) research.

ASP-7035 (compound 55) is an arginine vasopressin V2 receptor agonist potentially useful for research on nocturia.

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

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

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

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.

Desmopressin acetate (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.

Lazuvapagon is a vasopressin V2 receptor agonist that can be used to study enuresis.

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

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

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].

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.