Bufuralol hydrochloride

Bufuralol hydrochloride用途

Bufuralol hydrochloride (Ro 3-4787 hydrochloride) 是一种有效的非选择性,具有口服活性的 β-肾上腺素受体 (β-adrenoreceptor) 拮抗剂,具有部分激动剂活性。Bufuralol hydrochloride 是一种 CYP2D6 探针的底物。

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Bufuralol hydrochloride名称

[ CAS 号 ]:
60398-91-6

[ 中文名 ]:
Bufuralol hydrochloride

[ 英文名 ]:
Bufuralol hydrochloride

[英文别名 ]:

Bufuralol hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

研究领域 >> 内分泌

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[体外研究]

呋喃洛尔广泛用于CYP2D6活性的表征,并具有CYP2D6底物所特有的芳香环和碱性氮[3]。

[体内研究]

由NADPH介导的Bufuralol代谢表现出双相动力学,其效率低于在存在过氧化氢异丙苯(CuOOH)时观察到的效率,这与在肝脏中的观察结果一致[4]。

[参考文献]

[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.

Bufuralol hydrochloride物理化学性质

[ 沸点 ]:
393.2ºC at 760 mmHg

[ 熔点 ]:
143-146ºC

[ 分子式 ]:
C₁₆H₂₄ClNO₂

[ 分子量 ]:
297.82000

[ 闪点 ]:
191.6ºC

[ 精确质量 ]:
297.15000

[ PSA ]:
45.40000

[ LogP ]:
4.60960

[ 储存条件 ]:
-20°C，密闭，干燥

Bufuralol hydrochloride安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 危险品运输编码 ]:
NONH for all modes of transport

Bufuralol hydrochloride合成路线

详细合成路线

Bufuralol hydrochloride上下游产品

Bufuralol hydrochloride上游产品

Bufuralol hydrochloride下游产品

Bufuralol hydrochloride文献

Binding of bufuralol, dextromethorphan, and 3,4-methylenedioxymethylamphetamine to wild-type and F120A mutant cytochrome P450 2D6 studied by resonance Raman spectroscopy.

Biochem. Biophys. Res. Commun. 343(3) , 772-9, (2006)

Cytochrome P450 2D6 (CYP2D6) is one of the most important drug-metabolizing enzymes in humans. Resonance Raman data, reported for the first time for CYP2D6, show that the CYP2D6 heme is found to be in...

The ability of cytochrome P450 2D isoforms to synthesize dopamine in the brain: An in vitro study.

Eur. J. Pharmacol. 626(2-3) , 171-8, (2010)

The present study was aimed at determining which rat cytochrome P450 (CYP) isoforms are involved in the hydroxylation of tyramine to dopamine and at determining whether the reaction can take place in ...

Predictions of cytochrome P450-mediated drug-drug interactions using cryopreserved human hepatocytes: comparison of plasma and protein-free media incubation conditions.

Drug Metab. Dispos. 40(4) , 706-16, (2012)

Cryopreserved human hepatocytes suspended in human plasma (HHSHP) have previously provided accurate CYP3A drug-drug interaction (DDI) predictions from a single IC(50) that captures both reversible and...

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