http://jcps.bjmu.edu.cn

• Full Papers • Previous Articles     Next Articles

Identification of the metabolite and cytochrome P450 isoforms involved in rat liver microsomal metabolism of TM208

De-Tao Kong, Xiao-Mei Ling*, Fang-Bin Han, Jing-Li Gong, Ze-Mei Ge, Run-Tao Li, Jing-Rong Cui**   

  1. 1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China;
    2. The State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China
  • Received:2007-11-09 Revised:2008-01-10 Online:2008-03-15 Published:2008-03-15
  • Contact: Xiao-Mei Ling*, Jing-Rong Cui**

Abstract:

To identify the metabolite and CYP450 isoforms involved in rat liver microsomal metabolism of TM208. 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 CYP1A 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.

Key words: TM208, TM208, Rat liver microsomes, Rat liver microsomes, Metabolism, Metabolism, Cytochrome P450 isoform, Cytochrome P450 isoform

CLC Number: 

Supporting: