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用于通过液相色谱-质谱联用快速评估药物代谢和抑制作用的微粒体生物胶体

Microsome biocolloids for rapid drug metabolism and inhibition assessment by LC-MS.

作者信息

Bajrami Besnik, Krishnan Sadagopan, Rusling James F

机构信息

Department of Chemistry, University of Connecticut, Storrs, Connecticut 06269-3060. USA.

出版信息

Drug Metab Lett. 2008 Aug;2(3):158-62. doi: 10.2174/187231208785425854.

Abstract

Rat liver microsomes attached to nanoparticles were used for LC-MS studies of CYP3A and 2E1 enzymes in metabolism of N-nitroso compounds. Using these biocolloids, turnover rates were measured within 2 min. Inhibitor IC(50) values for ketoconazole (KET) and 4-methylpyrazole (4-MEP) were estimated.

摘要

附着于纳米颗粒的大鼠肝微粒体用于N-亚硝基化合物代谢中CYP3A和2E1酶的液相色谱-质谱联用(LC-MS)研究。使用这些生物胶体,在2分钟内测量了周转率。估算了酮康唑(KET)和4-甲基吡唑(4-MEP)的抑制剂半数抑制浓度(IC50)值。

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