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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。
Cytochrome P450 subtype metabolic enzymes acting on TM208 were studied in in vitro metabolism of rat liver microsomes. The samples without cytochrome P450 chemical inhibitors were used as control to study the effect of different cytochrome P450 selective chemical inhibitors on the metabolic rate of TM208. Selective inhibitors of CYP2D and CYP2B showed a concentration-dependent inhibition of TM208 metabolism, and selective inhibitors of CYP1A inhibited the metabolism of TM208 to a certain extent. Selective inhibitors of CYP3A did not show significant inhibitory effects on the metabolism of TM208. TM208 metabolizes in vitro metabolism of rat liver microsomes mainly through CYP2D and CYP2B cytochrome P450 isoforms.