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| | Conivaptan impurity Basic information |
| Product Name: | Conivaptan impurity | | Synonyms: | Conivaptan impurity;Conivaptan-d4;N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl-d4]-[1,1'-biphenyl]-2-carboxamide | | CAS: | 1129433-63-1 | | MF: | C32H26N4O2 | | MW: | 498.59 | | EINECS: | | | Product Categories: | | | Mol File: | 1129433-63-1.mol |  |
| | 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)
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| | Conivaptan impurity Preparation Products And Raw materials |
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