A neuropeptide with diverse biological activities
Metoprolol-d6 is intended for use as an internal standard for the quantification of metoprolol by GC- or LC-MS. Metoprolol is a potent and selective β1-adrenergic receptor (β1-AR) antagonist (Ki = 47 nM).1 It is selective for β1- over β2- and β3-ARs (Kis = 2.96 and 10.1 μM, respectively). In vivo, metoprolol (2.5 mg/kg per hour) reduces aortic atherosclerotic plaque area, serum levels of TNF-α and CXCL1, and plaque macrophage content in an ApoE-/- mouse model of atherosclerosis.2 Metoprolol (1 mg/kg per day) reduces biventricular cavity expansion and myocardial necrosis in a mouse model of encephalomyocarditis-induced congestive heart failure when administered in combination with captopril .3 Formulations containing metoprolol have been used in the treatment of high blood pressure and heart failure.
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 cellsNaunyn Schmiedebergs Arch. Pharmacol.369(2)151-159(2004) 2.Ulleryd, M.A., Bernberg, E., Yang, L.J., et al.Metoprolol reduces proinflammatory cytokines and atherosclerosis in ApoE-/- mice.Biomed. Res. Int.548783(2014) 3.Kanda, T., Inoue, M., Suzuki, T., et al.Low-dose combination therapy with metoprolol and captopril for congestive heart failure in mice.Cardiovasc. Drugs Ther.7(5)795-800(1993)
动态评分
0.0