Bufuralol (hydrochloride)

Bufuralol is a non-selective antagonist of β-adrenergic receptors (β-ARs) that also has partial agonist activity.^1,2,3 It decreases mean arterial blood pressure and increases abdominal aortic blood flow in anesthetized cats when administered intravenously at doses of 0.3 and 1 mg/kg.³ Bufuralol is hydroxylated at the 1' position by the cytochrome P450 (CYP) isoform CYP2D6 and has been used as a substrate to measure CYP2D6 activity.^4,1,5,6

WARNING This product is not for human or veterinary use.

1. Narimatsu, S., Takemi, C., Kuramoto, S., et al. Stereoselectivity in the oxidation of bufuralol, a chiral substrate, by human cytochrome P450s. Chirality 15(4), 333-339 (2003).

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(5), 527-534 (1986).

3. Blaber, L.C., Burden, D.T., Eigenmann, R., et al. The effects of bufuralol, a β-adrenoceptor antagonist with predominant β₂-adrenoceptor agonistic activity, in the cat and the dog. J. Cardiovasc. Pharmacol. 6(1), 165-175 (1984).

4. Yamazaki, H., Guo, Z., Persmark, M., et al. Bufuralol hydroxylation by cytochrome P450 2D6 and 1A2 enzymes in human liver microsomes. Mol. Pharmacol. 46(3), 568-577 (1994).

5. Paine, M.J.I., Gilham, D., Roberts, G.C.K., et al. Functional high level expression of cytochrome P450 CYP2D6 using baculoviral expression systems. Arch. Biochem. Biophys. 328(1), 143-150 (1996).

6. Chen, N., Cui, D., Wang, Q., et al. In vitro drug-drug interactions of budesonide: Inhibition and induction of transporters and cytochrome P450 enzymes. Xenobiotica 48(6), 637-646 (2018).

Negoro, R., Tasaka, M., Deguchi, S., et al. Generation of HepG2 cells with high expression of multiple drug-metabolizing enzymes for drug discovery research using a PITCh system. Cells 11(10), 1677 (2022).