Bufuralol hydrochloride  (Synonyms: Ro 3-4787 hydrochloride)

Bufuralol (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^[1][2].

Bufuralol (Ro 3-4787) hydrochloride is widely used in the characterization of CYP2D6 activity, and possesses aromatic rings and a basic nitrogen that are characteristic of CYP2D6 substrates^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Bufuralol (Ro 3-4787) hydrochloride 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^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

297.82

Solid

C₁₆H₂₄ClNO₂

60398-91-6

OC(CNC(C)(C)C)C1=CC2=CC=CC(CC)=C2O1.[H]Cl

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. T H Pringle, et al. Pharmacodynamic and pharmacokinetic studies on bufuralol in man. Br J Clin Pharmacol. 1986 Nov;22(5):527-34.  [Content Brief]

  [2]. Jie Cai, et al. Effects of 22 Novel CYP2D6 Variants Found in the Chinese Population on the Bufuralol and Dextromethorphan Metabolisms In Vitro. Basic Clin Pharmacol Toxicol. 2016 Mar;118(3):190-9.  [Content Brief]

  [3]. Sarah M Glass, et al. CYP2D6 Allelic Variants *34, *17-2, *17-3, and *53 and a Thr309Ala Mutant Display Altered Kinetics and NADPH Coupling in Metabolism of Bufuralol and Dextromethorphan and Altered Susceptibility to Inactivation by SCH 66712. Drug Metab Dispos. 2018 Aug;46(8):1106-1117.  [Content Brief]

  [4]. T Prueksaritanont, et al. (+)-bufuralol 1'-hydroxylation activity in human and rhesus monkey intestine and liver. Biochem Pharmacol. 1995 Oct 26;50(9):1521-5.  [Content Brief]