Bisoprolol (hemifumarate)

Bisoprolol is an antagonist of the β₁-adrenergic receptor (β₁-AR; K_i = 25 nM for the human receptor).¹ It is selective for β₁- over β₂-ARs (K_i = 480 nM for the human receptor in a radioligand binding assay).¹ Bisoprolol binds to rat ventricular myocytes and heart membranes that endogenously express β₁-ARs and β₁- and β₂-ARs, respectively (K_is = 20 and 38.1 nM, respectively).² In vivo, bisoprolol (0.3 mg/kg) inhibits increases in heart rate and myocardial contractility induced by isoproterenol (Item No. 15592) in conscious dogs.³ It 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. Bisoprolol also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M^pro), also known as 3C-like protease (3CL^pro; IC₅₀ = 118.5 µg/ml) and reduces viral infectivity in SARS-CoV-2 infected Vero E6 cells (IC₅₀ = 15.917 µg/ml).⁴ 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.

WARNING This product is not for human or veterinary use.

1. Smith, C., and Teitler, M. β-blocker selectivity at cloned human β1- and β₂-adrenergic receptors. Cardiovasc. Drugs Ther. 13(2), 123-126 (1999).

2. 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 bisoprolol. J. Cardiovasc. Pharmacol. 15(3), 421-427 (1990).

3. Haeusler, G., Schliep, H.-J., Schelling, P., et al. High β1-selectivity and favourable pharmacokinetics as the outstanding properties of bisoprolol. J. Cardiovasc. Pharmacol. 8(Suppl. 11), S2-S15 (1986).

4. Hamed, M.I.A., Darwish, K.M., Soltane, R., et al. β-Blockers bearing hydroxyethylamine and hydroxyethylene as potential SARS-CoV-2 Mpro inhibitors: Rational based design, in silico, in vitro, and SAR studies for lead optimization. RSC Adv. 11(56), 35536-35558 (2021).