Bisoprolol-d7 (hemifumarate) is intended for use as an internal standard for the quantification of bisoprolol by GC- or LC-MS. Bisoprolol is a potent β-adrenergic receptor (β-AR) antagonist that is selective for β1-ARs over β2-ARs (Kis = 25 and 480 nM, respectively in S49 cells overexpressing the human receptors).1 It also selectively binds to β1-ARs over β2-ARs in human myocardium (Kis = 75.8 and 991 nM, respectively).2 Bisoprolol binds to rat ventricular myocytes and heart membrane (Kis = 20 and 38.1 nM, respectively) and to rat β1-AR in salivary glands and β2-AR in reticulocytes (Kis = 24 and 1,945 nM, respectively).3,4 In vivo, it inhibits increases in heart rate induced by isoproterenol in guinea pigs.5 Bisoprolol (0.3 mg/kg) inhibits isoproterenol-induced increases in heart rate and myocardial contractility in conscious dogs. It also decreases blood pressure and heart rate in spontaneously hypertensive rats (SHRs) when chronically administered at a dose of 7.5 mg/kg twice per day over 19 weeks. Formulations containing bisoprolol have been used in the treatment of heart failure, angina pectoris, mild to moderate hypertension, and for secondary prevention of myocardial infarction.
1.Smith, C., and Teitler, M.β-blocker selectivity at cloned human β1- and β2-adrenergic receptorsCardiovasc. Drugs Ther.13(2)123-126(1999) 2.Bundkirchen, A., Brixius, K., BÖlck, B., et al.β1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studiesEur. J. Pharmacol.460(1)19-26(2003) 3.Mauz, A.B., and Pelzer, H.β-adrenoceptor-binding studies of the cardioselective β blockers bisoprolol, H-I 42 BS, and HX-CH 44 BS to heart membranes and intact ventricular myocytes of adult rats: two β1-binding sites for bisoprololJ. Cardiovasc. Pharmacol.15(3)421-427(1990) 4.Wellstein, A., Palm, D., and Belz, G.G.Affinity and selectivity of β-adrenoceptor antagonists in vitroJ. Cardiovasc. Pharmacol.8(Suppl. 11)S36-S40(1986) 5.Haeusler, G., Schliep, H.-J., Schelling, P., et al.High β1-selectivity and favourable pharmacokinetics as the outstanding properties of bisoprololJ. Cardiovasc. Pharmacol.8(Suppl. 11)S2-S15(1986)