Metoprolol-d6 (tartrate)

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 (K_i = 47 nM).¹ It is selective for β₁- over β₂- and β₃-ARs (K_is = 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)