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呋拉茶碱

呋拉茶碱用途

Furafylline 是一种有效且有选择性的人细胞色素 P450IA2 抑制剂，其 IC₅₀ 值为 0.07 μM。

呋拉茶碱名称

[ CAS 号 ]:
80288-49-9

[ 中文名 ]:
呋喃茶碱

[ 英文名 ]:
Furafylline

[中文别名 ]:

[英文别名 ]:

furafylline
3-Furfuryl-1,8-dimethylxanthine

呋拉茶碱生物活性

[ 描述 ]:

Furafylline 是一种有效且有选择性的人细胞色素 P450IA2 抑制剂,其 IC50 值为 0.07 μM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

研究领域 >> 癌症

[ 靶点 ]

IC50: 0.07 μM (human cytochrome P450IA2)[1]

[体内研究]

Furafylline是一种有效的选择性人细胞色素P450IA2抑制剂,在激酶实验中IC50为0.07μM。呋喃茶碱是甲基黄嘌呤衍生物,作为茶碱的长效替代物用于治疗哮喘。由于抑制咖啡因氧化,由一种或多种P450的烃诱导型同工酶催化的反应,呋喃茶碱的施用与咖啡因的血浆水平升高有关。呋喃茶碱对P450的其他同工酶催化的人体单加氧酶活性影响很小或没有影响,包括P4501ID1,P4501IC,P450IIIA [1]。

[参考文献]

[1]. Sesardic D, et al. Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man. Br J Clin Pharmacol. 1990 Jun;29(6):651-63.

[相关活性小分子]

呋拉茶碱物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
543.6±60.0 °C at 760 mmHg

[ 分子式 ]:
C₁₂H₁₂N₄O₃

[ 分子量 ]:
260.249

[ 闪点 ]:
282.6±32.9 °C

[ 精确质量 ]:
260.090942

[ PSA ]:
85.82000

[ LogP ]:
-0.24

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.637

[ 储存条件 ]:
2-8℃

呋拉茶碱安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
3

[ 海关编码 ]:
2939590000

呋拉茶碱海关

[ 海关编码 ]: 2939590000

呋拉茶碱文献

Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity.

Expert Opin. Drug Metab. Toxicol. 10(10) , 1313-24, (2014)

Drug resistance by Plasmodium falciparum remains a challenge in malaria chemotherapy. This paper will focus on physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hy...

The cytochrome P450-catalyzed metabolism of levomepromazine: a phenothiazine neuroleptic with a wide spectrum of clinical application.

Biochem. Pharmacol. 90(2) , 188-95, (2014)

The aim of the present study was to identify cytochrome P450 isoenzymes (CYPs) involved in the 5-sulfoxidation and N-demethylation of the aliphatic-type phenothiazine neuroleptic levomepromazine in hu...

Identification of the human cytochrome P450 enzymes involved in the two oxidative steps in the bioactivation of clopidogrel to its pharmacologically active metabolite.

Drug Metab. Dispos. 38(1) , 92-9, (2010)

The aim of the current study is to identify the human cytochrome P450 (P450) isoforms involved in the two oxidative steps in the bioactivation of clopidogrel to its pharmacologically active metabolite...

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