| Identification | Back Directory | [Name]
Conivaptan impurity | [CAS]
1129433-63-1 | [Synonyms]
Conivaptan-d4
Conivaptan impurity
N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl-d4]-[1,1'-biphenyl]-2-carboxamide | [Molecular Formula]
C32H26N4O2 | [MOL File]
1129433-63-1.mol | [Molecular Weight]
498.59 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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)
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