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HomeProduct name listConivaptan impurity

Conivaptan impurity

  • CAS NO.:1129433-63-1
  • Empirical Formula: C32H26N4O2
  • Molecular Weight: 498.59
  • Update Date: 2023-05-21 10:59:17
Conivaptan impurity Structural

What is Conivaptan impurity?

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)

Properties of Conivaptan impurity

storage temp.  Store at -20°C
solubility  DMSO: soluble
form  A solid

Safety information for Conivaptan impurity

Computed Descriptors for Conivaptan impurity

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