川丁特罗对大鼠细胞色素P450酶的影响

J4 ›› 2010, Vol. 48 ›› Issue (06): 1061-1064.

川丁特罗对大鼠细胞色素P450酶的影响

孙严彤^1,2, 高峰¹, 张梦亮¹, 崔相勇¹, 王中华^1, 顾景凯¹

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

收稿日期:2010-03-15 出版日期:2010-11-26 发布日期:2010-11-26
通讯作者: 顾景凯 E-mail:gujk@mail.jlu.edu.cn

Effect of Trantinterol on Cytochrome P450 Enzymes

SUN Yantong^1,2, GAO Feng¹, ZHANG Mengliang¹, CUI Xiangyong¹,WANG Zhonghua¹, GU Jingkai¹

1. Research Center for Drug Metabolism, College of Life Science, Jilin University, Changchun 130012, China;
2. College of Pharmaceutical Sciences, Jilin University, Changchun 130021, China

Received:2010-03-15 Online:2010-11-26 Published:2010-11-26
Contact: GU Jingkai E-mail:gujk@mail.jlu.edu.cn

摘要/Abstract

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7 d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.

关键词: 川丁特罗；细胞色素P450；大鼠

Abstract:

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 (P>0.05). Chronic oral administration of trantinterol did not lead to the induction of the representative enzymes of the main drug metabolizing CYP450 subfamilies.

Key words: trantinterol, cytochrome P450, rat

中图分类号:

R969.1

孙严彤, 高峰, 张梦亮, 崔相勇, 王中华, 顾景凯. 川丁特罗对大鼠细胞色素P450酶的影响[J]. J4, 2010, 48(06): 1061-1064.

SUN Yan-Tong, GAO Feng, ZHANG Meng-Liang, CUI Xiang-Yong, WANG Zhong-Hua, GU Jing-Kai. Effect of Trantinterol on Cytochrome P450 Enzymes[J]. J4, 2010, 48(06): 1061-1064.