Bufuralol

• CAT Number: I023794
• CAS Number: 54340-62-4
• Molecular Formula: C16H23NO2
• Molecular Weight: 261.36
• Purity: ≥95%
• Synonyms: 2-(tert-butylamino)-1-(7-ethyl-1-benzofuran-2-yl)ethanol
• InChI: InChI=1S/C16H23NO2/c1-5-11-7-6-8-12-9-14(19-15(11)12)13(18)10-17-16(2,3)4/h6-9,13,17-18H,5,10H2,1-4H3
• InChIKey: SSEBTPPFLLCUMN-UHFFFAOYSA-N
• SMILES: CCC1=CC=CC2=C1OC(=C2)C(CNC(C)(C)C)O

Bufuralol (Cat No.: I023794) is a β-adrenergic receptor antagonist (beta-blocker) with intrinsic sympathomimetic activity, used primarily in pharmacological research. It is a well-known substrate of cytochrome P450 2D6 (CYP2D6), making it a standard probe in drug metabolism and pharmacokinetics studies. Bufuralol’s dual activity allows modulation of heart rate and contractility without causing excessive bradycardia. It is valuable for investigating CYP2D6 polymorphisms, drug-drug interactions, and β-receptor signaling pathways, particularly in the context of cardiovascular function and precision medicine applications.

Reference

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