An antagonist of β-adrenergic receptors
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Labeled Version(s)
29081Bufuralol-d9 (hydrochloride)
Metabolite(s)
221601'-hydroxy Bufuralol
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Bufuralol (hydrochloride)

Item No. 17794

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-[[(1,1-dimethylethyl)amino]methyl]-7-ethyl-2-benzofuranmethanol, monohydrochloride
CAS Number
60398-91-6
Synonyms
  • (±)-Bufuralol
  • DL-Bufuralol
  • Ro 3-4787
Molecular Formula
C16H23NO2 • HCl
Formula Weight
297.8
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 10 mg/mlEthanol: 15 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
209, 248 nm
SMILES
CCC1=C(OC(C(O)CNC(C)(C)C)=C2)C2=CC=C1.Cl
InChi Code
InChI=1S/C16H23NO2.ClH/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;1H
InChi Key
KJBONRGCLLBWCJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $90

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    5 mg

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    10 mg

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    Product Description

    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.

    References & Product Citations
    Product Description References

    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).

    Product Citations

    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).