货号 | 15429-250mg |
描述 | Metoprolol is a potent and selective β1-adrenergic receptor blocker (Ki = 47 nM for the β1 receptor, compared with 3.0 and 10 μM for the β2 and β3 receptors, respectively).1,2 This product is a racemic mixture of enantiomers that differ in their in vivo actions and metabolism.3 Metoprolol is predominantly metabolized by the cytochrome P450 (CYP) isoform CYP2D6, an enzyme with significant genetic heterogeneity in function.3,4 The succinate salt of metoprolol is used in formulations intended for extended release of the compound.5 Beta-blockers, including metoprolol, have diverse applications in cardiology and vascular disease.5 |
供应商 | Cayman |
应用文献 | |
1.Hoffmann, C.,Leitz, M.R.,Oberdorf-Maass, S., et al. Comparative pharmacology of human β-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn-Schmiedebergs Arch. Pharmacol. 369(2), 151-159 (2004). 2.Baker, J.G. The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors. Br. J. Pharmacol. 144(3), 317-322 (2005). 3.Mehvar, R. and Brocks, D.R. Stereospecific pharmacokinetics and pharmacodynamics of β-adrenergic blockers in humans. J. Pharm. Pharm. Sci. 4(2), 185-200 (2001). 4.Blake, C.M.,Kharasch, E.D.,Schwab, M., et al. A meta-analysis of CYP2D6 metabolizer phenotype and metoprolol pharmacokinetics. Clinical Pharmacology and Therapeutics 94(3), 394-399 (2013). 5.Tang, W.H.,Militello, M. and Francis, G.S. In heart failure, allβblockers are not necessarily equal. Cleveland Clinic Journal of Medicine 70(12), 1081-1087 (2003). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 385.5 |
分子式 | C15H25NO3 • C4H6O4 |
CAS号 | 207983-04-8 |
稳定性 | ≥ 2 years |
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