Acebutolol is an antagonist of β₁-adrenergic receptors (β₁-ARs; K_i= 125 nM).¹It is selective for β₁- over β₂-ARs (K_i= 7,070 nM).In vivo, acebutolol decreases isoprenaline-induced tachycardia and diastolic hypotension in cats (ED₅₀= 0.09 mg/kg for both).²Acebutolol (12.5, 25, and 50 mg/kg) inhibits ouabain-induced arrhythmias in rabbits, as well as protects against chloroform-induced ventricular fibrillation in mice (ED₅₀= 0.067 mg/kg).³Formulations containing acebutolol have been used in the treatment of angina and irregular heartbeat.

1.Tsuchihashi, H., Nakashima, Y., Kinami, J., et al.Characteristics of 125I-iodocyanopindolol binding to β-adrenergic and serotonin-1B receptors of rat brain: Selectivity of β-adrenergic agentsJpn. J. Pharmacol.52(2)195-200(1990) 2.Basil, B., Jordan, R., Loveless, A.H., et al.β-Adrenoceptor blocking properties and cardioselectivity of M & B 17,803ABr. J. Pharmacol.48(2)198-211(1973) 3.Basil, B., Jordan, R., Loveless, A.H., et al.A comparison of the experimental anti-arrhythmic properties of acebutolol (M and B 17,803), propranolol and practololBr. J. Pharmacol.50(3)323-333(1974)