CAJ | 학술논문

在大鼠肝微粒体的体外代谢中研究作用于TM208的细胞色素P450亚型代谢酶.以不含细胞色素P450化学抑制剂的样品为对照,研究不同细胞色素P450亚型选择性化学抑制剂对TM208代谢转化率的影响.CYP2D和CYP2B的选择性抑制剂对TM208的代谢表现出浓度依赖性较强抑制作用,CYP1A的选择性抑制剂对TM208的代谢表现出一定抑制作用.CYP3A的选择性抑制剂对TM208的代谢没有表现出明显的抑制作用.TM208在大鼠肝微粒体体外代谢中主要通过CYP2D和CYP2B两种细胞色素P450亚型代谢酶参与代谢.
재대서간미립체적체외대사중연구작용우TM208적세포색소P450아형대사매.이불함세포색소P450화학억제제적양품위대조,연구불동세포색소P450아형선택성화학억제제대TM208대사전화솔적영향.CYP2D화CYP2B적선택성억제제대TM208적대사표현출농도의뢰성교강억제작용,CYP1A적선택성억제제대TM208적대사표현출일정억제작용.CYP3A적선택성억제제대TM208적대사몰유표현출명현적억제작용.TM208재대서간미립체체외대사중주요통과CYP2D화CYP2B량충세포색소P450아형대사매삼여대사.
To identify the metabolite and CYP450 isoforms involved in rat liver microsomal metabolism of TM2O8.The present study investigated the metabolism of TM208 and the effects of selective CYP450 inhibitors on the metabolism of TM208 in rat liver microsomes.Various specific inhibitors of CYP were used to identify the isoforms of CYP involved in the metabolism of TM208.The inhibitor of CYP2D and that of CYP2B had strong inhibitory effects on TM208 metabolism in a concentration-dependant manner,the inhibitor of CYPIA had a modest inhibitory effect,and the inhibitor of CYP3A seemed not to have an obvious inhibitory effect on TM208 metabolism.TM208 might mainly be metabolized by CYP2D and CYP2B in rat liver microsomes.