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

Melting point:

143-146 °C

storage temp. 

2-8°C

solubility 

H2O: soluble

form 

solid

color 

white to off-white

Safety

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

(±)-alpha-[[(tert-butyl)amino]methyl]-7-ethyl-2-benzofuranmethanol hydrochloride Chemical Properties,Usage,Production

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).