(±)-alpha-[[(tert-butyl)amino]methyl]-7-ethyl-2-benzofuranmethanol hydrochloride

Description

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

Uses

A β-Adrenergic blocker with peripheral vasodilating activity. Antianginal; antihypertensive.

Uses

CYP2D6 substrate

Biochem/physiol Actions

Bufuralol hydrochloride is known to be a non-specific β-receptor inhibitor that has an affinity for β 1 and β 2 receptors. Furthermore, studies have reported that bufuralol hydrochloride can decrease isoproterenol peripheral resistance.

in vitro

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

in vivo

Bufuralol metabolism mediated by NADPH 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.

References

[1] fothergill ga, francis rj, hamilton tc, osbond jm, parkes mw. bufuralol, a new beta-adrenoceptor blocking agent. experientia. 1975 nov 15;31(11):1322-3.
[2] pringle, t. h.,francis, r.j.,east, p.b., et al. pharmacodynamic and pharmacokinetic studies on bufuralol in man. br.j.clin.pharmac. 22, 527-534 (1986).