Acebutolol is an antagonist of β1-adrenergic receptors (β1-ARs; Ki = 125 nM).1 It is selective for β1- over β2-ARs (Ki = 7,070 nM). In vivo, acebutolol decreases isoprenaline-induced tachycardia and diastolic hypotension in cats (ED50 = 0.09 mg/kg for both).2 Acebutolol (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).3 Formulations 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)