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一种利用司巴丁作为细胞色素P450 2D6探针和三联吡啶钌(II)-电化学发光检测来研究药物代谢酶抑制剂的方法的开发与应用。

Development and application of a method to investigate drug-metabolizing enzyme inhibitors using sparteine for probe of cytochrome P450 2D6 and tris(2,2'-bipyridine)ruthenium(II)-electrogenerated chemiluminescence detection.

作者信息

Shibano Yuu, Taki Shiwori, Miyamoto Aoi, Uchikura Kazuo

机构信息

College of Pharmacy, Nihon University, Funabashi, Chiba, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2011;59(2):249-53. doi: 10.1248/cpb.59.249.

DOI:10.1248/cpb.59.249
PMID:21297307
Abstract

We studied the detection of drug-metabolizing enzyme inhibitiors using column-switching high performance liquid chromatography with tris(2,2'-bipyridine)ruthenium(II) (Ru(bpy)(3)(2+))-electrogenerated chemiluminescence detection. This can be applied to evaluate the genetic diversity concerning the ability of cytochrome P450 (CYP) 2D6 to metabolize drug in vitro. We demonstrated the ability of CYP2D6 to enable us to examine drugs metabolizing enzyme inhibition with high performance and sensitivity. This method can be applied to investigate metabolite inhibitors of CYP2D6 in vitro and in vivo. Thus, Metixene was found to be a potential CYP2D6 inhibitor.

摘要

我们使用柱切换高效液相色谱结合三(2,2'-联吡啶)钌(II)(Ru(bpy)(3)(2+))-电化学发光检测法研究了药物代谢酶抑制剂的检测。这可用于评估细胞色素P450(CYP)2D6体外代谢药物能力的遗传多样性。我们证明了CYP2D6能够使我们以高性能和高灵敏度检测药物代谢酶抑制作用。该方法可用于体外和体内研究CYP2D6的代谢物抑制剂。因此,发现美噻吨是一种潜在的CYP2D6抑制剂。

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