Conivaptan impurity Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO: soluble

form 

A solid

Conivaptan impurity Usage And Synthesis

Biological Activity

Conivaptan-d4 is intended for use as an internal standard for the quantification of conivaptan by GC- or LC-MS. Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V1A and V2 (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2, respectively).1 It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (Ki = 44 nM) but has no effect on AVP binding to anterior pituitary V1B receptors at concentrations up to 100 μM in a radioligand binding assay. Conivaptan suppresses AVP-induced increases in intracellular calcium in vascular smooth muscle cells (VSMCs) in vitro and the pressor response in pithed rats. Conivaptan (0.01-0.3 mg/kg, i.v.) increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner. It also reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model.2

References

1.Tahara, A., Tomura, Y., Wada, K.-I., et al.Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivoJ. Pharmacol. Exp. Ther.282(1)301-308(1997) 2.Zeynalov, E., Jones, S.M., Seo, J.W., et al.Arginine-vasopressin receptor blocker conivaptan reduces brain edema and blood-brain barrier disruption after experimental stroke in micePLoS One10(8)e0136121(2015)

Conivaptan impurity(1129433-63-1)Related Product Information

• 2-Methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine
• 2-Methyl-5,6-dihydro-4H-benzo[b]oxazolo[5,4-d]azepine
• 2-Methyl-6-[(4-methylphenyl)sulfonyl]-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine
• Conivaptan hydrochloride
• 4-[(Biphenyl-2-ylcarbonyl)amino]benzoic acid
• N-(4-(2-Methyl-5,6-dihydro-4H-benzo[b]oxazolo[5,4-d]azepine-6-carbonyl)phenyl)-[1,1'-biphenyl]-2-carboxaMide