Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity, which is also a CYP2D6 probe substrate [1] [2].

Bufuralol is widely used in the characterization of CYP2D6 activity. Bufuralol possesses aromatic rings and a basic nitrogen that are characteristic of CYP2D6 substrates [3].

NADPH-mediated metabolism of Bufuralol exhibits biphasic kinetics and is less efficient than that observed in the presence of cumene hydroperoxide (CuOOH) in and monkey intestines, in agreement with the observations in the livers [4].