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Displacement of [3H]dihydroalprenolol binding from rat heart and lung by acebutolol, diacetolol and D‐diacetolol

Acebutolol is a cardioselective @-adrenoceptor antagonist with membrane-stabilizing and partial agonist activity (Basil & Jordan 1980). It is effective in the treatment of hypertension, angina pectoris and certain cardiac arrhythmias (Cowling & Leary 1981; DiBianco et al 1982; Mitenko et al 1982; Shapiro et al 1982). Acebutolol is almost exclusively metabolized to diacetolol and the plasma concentration of diacetolol rapidly exceeds that of unchanged acebutolol following oral administration of Sectral (acebutolol HCI, May & Baker) to man (Meffin et al 1978).