Furafylline是一个强有力的和选择性抑制剂细胞色素P450IA2的男人。

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Sesardic D, Boobis AR,穆雷BP,穆雷年代,Segura J, de la Torre R,戴维斯DS

Furafylline是一个强有力的和选择性抑制剂细胞色素P450IA2的男人。

Br中国新药杂志。1990年6月29日(6):651 - 63。

PubMed ID

2378786 (在PubMed

]

文摘

1。Furafylline (8-dimethyl-3——“糠醇(2)methylxanthine) methylxanthine导数,介绍了作为一种长效替代茶碱治疗哮喘。管理furafylline血浆水平与海拔的咖啡因,咖啡因抑制氧化,反应催化了一个或多个hydrocarbon-inducible P450酶同功酶。我们现在研究的选择性抑制furafylline人类单氧酶的活动。2。Furafylline是强有力的,非竞争性抑制剂的高亲和力非那西汀O-deethylase活动的人类肝脏微粒体分数,P450IA2反应催化了,0.07 microM IC50值。3所示。Furafylline很少或没有影响人类活动单氧酶催化了其他同功酶P450,包括P450IID1 P450IIC P450IIA。特别感兴趣的,furafylline没有抑制P450IA1,评估从芳基碳氢化合物羟化酶活动的胎盘样本抽烟的女人。4所示。 It is concluded that furafylline is a highly selective inhibitor of P450IA2 in man. 5. Furafylline was a potent inhibitor of the N3-demethylation of caffeine and of a component of the N1- and N7-demethylation. This confirms earlier suggestions that caffeine is a selective substrate of a hydrocarbon-inducible isoenzyme of P450 in man, and identifies this as P450IA2. Thus, caffeine N3-demethylation should provide a good measure of the activity of P450IA in vivo in man. 6. Although furafylline selectively inhibited P450IA2, relative to P450IA1, in the rat, this was at 1000-times the concentration required to inhibit the human isoenzyme, suggesting a major difference in the active site geometry between the human and the rat orthologues of P50IA2.

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药物

Furafylline