| Bioactivity | Bufuralol (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[1][2]. |
| Invitro | Bufuralol (Ro 3-4787) hydrochloride 广泛用于表征 CYP2D6 活性，并具有 CYP2D6 底物特有的芳香环和碱性氮[3]。 |
| In Vivo | Bufuralol (Ro 3-4787) hydrochloride 代谢由 NADPH 介导表现出双相动力学，其效率低于在和猴子肠道中观察到的氢过氧化异丙苯 (CuOOH) 存在的情况，这与在肝脏中的观察结果一致[4]。 |
| Name | Bufuralol hydrochloride |
| CAS | 60398-91-6 |
| Formula | C16H24ClNO2 |
| Molar Mass | 297.82 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. 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. [2]. 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. [3]. 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. |
Bufuralol hydrochloride
CAS: 60398-91-6 F: C16H24ClNO2 W: 297.82
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial a
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