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2002•Zhongguo linchuang yaolixue yu zhiliaoxueRequires access

Studies on the metabolism and effect on the CYP450 of CH330331 in rat liver microsomes

Sun Hai-yan, Fan He, Huichang Bi, Huang Wen-lin, Min Huang

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Abstract

AIM:To study the metabolic kinetics of CH330331 in rat liver microsome,and its inhibition on CYP450 subtypes in the cocktail models.METHODS:The incubation parameters in rat liver microsome were optimized and were the Michaelis-Menten parameters Km and Vmax estimated the component of probe inhibitors in cocktail models were also confirmed and the effect of CH330331 on main subtypes of cytochrome P450 studied.RESULTS:The Km and Vmax of CH330331 were 18.96 μmol/L and 2.08 μmol/(min·mg protein),respectively.CH330331 had a weakly inhibition to the activity of CYP1A2,CYP2D6 and CYP2C9 but had no effect on CYP2C19,CYP2E1,and CYP3A4.CONCLUSION:CH330331 can increase the blood concentration of those drugs that are metabolized mainly by CYP1A2,CYP2D6 and CYP2C9.

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AIM:To study the metabolic kinetics of CH330331 in rat liver microsome,and its inhibition on CYP450 subtypes in the cocktail models.METHODS:The incubation parameters in rat liver microsome were optimized and were the Michaelis-Menten parameters Km and Vmax estimated the component of probe inhibitors in cocktail models were also confirmed and the effect of CH330331 on main subtypes of cytochrome P450 studied.RESULTS:The Km and Vmax of CH330331 were 18.96 μmol/L and 2.08 μmol/(min·mg protein),respectively.CH330331 had a weakly inhibition to the activity of CYP1A2,CYP2D6 and CYP2C9 but had no effect on CYP2C19,CYP2E1,and CYP3A4.CONCLUSION:CH330331 can increase the blood concentration of those drugs that are metabolized mainly by CYP1A2,CYP2D6 and CYP2C9.

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Available abstract

AIM:To study the metabolic kinetics of CH330331 in rat liver microsome,and its inhibition on CYP450 subtypes in the cocktail models.METHODS:The incubation parameters in rat liver microsome were optimized and were the Michaelis-Menten parameters Km and Vmax estimated the component of probe inhibitors in cocktail models were also confirmed and the effect of CH330331 on main subtypes of cytochrome P450 studied.RESULTS:The Km and Vmax of CH330331 were 18.96 μmol/L and 2.08 μmol/(min·mg protein),respectively.CH330331 had a weakly inhibition to the activity of CYP1A2,CYP2D6 and CYP2C9 but had no effect on CYP2C19,CYP2E1,and CYP3A4.CONCLUSION:CH330331 can increase the blood concentration of those drugs that are metabolized mainly by CYP1A2,CYP2D6 and CYP2C9.

Key concepts: CYP1A2, Microsome, CYP2C9, CYP3A4, CYP2E1, Cytochrome P450, CYP2C19, CYP2D6

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