Bufuralol

Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate[1][2][3][4].

Product Specifications

CAS Number

[54340-62-4]

Product Name Alternative

Ro 3-4787

UNSPSC

12352005

Target

Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/bufuralol.html

Purity

99.25

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CCC1=CC=CC2=C1OC(C(O)CNC(C)(C)C)=C2

Molecular Formula

C16H23NO2

Molecular Weight

261.36

References & Citations

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