川丁特罗对大鼠细胞色素P450酶的影响  

Effect of Trantinterol on Cytochrome P450 Enzymes

作　　者：孙严彤[1,2] 高峰[1] 张梦亮[1] 崔相勇[1] 王中华[1] 顾景凯[1] 

机构地区：[1]吉林大学生命科学学院药物代谢研究中心,长春130012 [2]吉林大学药学院,长春130021

出　　处：《吉林大学学报（理学版）》2010年第6期1061-1064,共4页Journal of Jilin University:Science Edition

基　　金：国家自然科学基金(批准号:30973587);科技部"十一五"重大科技项目基金(批准号:2009ZX09304-003)

摘　　要：研究新型抗哮喘药川丁特罗(trantinterol)对大鼠细胞色素P450酶的影响.大鼠连续7d灌胃给予川丁特罗后,测定肝微粒体中CYP450的质量摩尔浓度和主要3种亚型CYP1A2,CYP2D6和CYP3A4活性的变化.实验结果表明,与对照组相比,川丁特罗给药组的大鼠肝微粒体中CYP450的总质量摩尔浓度未受影响(P>0.05),对主要亚型CYP1A2,CYP2D6和CYP3A4的活性也无影响(P>0.05),表明该药物对肝微粒体中的主要代谢酶无抑制或诱导作用.To study the effect of trantinterol on cytochrome P450 （CYP450） in rat liver microsomes,rats were given single daily oral doses of trantinterol or saline for one week. Liver microsomes were prepared and the effects of treatment on the total CYP450 content and the activities of CYP1A2,CYP2D6,and CYP3A4 were determined. The latter employed phenacetin,debrisoquine and midazolam respectively as probe substrates. The results indicate that the level of total CYP450 and the activities of CYP1A2,CYP2D6,and CYP3A4 in rat liver microsomes were unchanged after treatment by trantinterol （P0.05）. Chronic oral administration of trantinterol did not lead to the induction of the representative enzymes of the main drug metabolizing CYP450 subfamilies.

关 键 词：川丁特罗 细胞色素P450 大鼠 

分 类 号：R969.1[医药卫生—药理学]