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- W2362604100 abstract "OBJECTIVE To investigate the metabolic activated metabolites and the kinetic characteristics of isocarbophos in rat microsomes in vitro.METHOD Metabolites of isocarbophos were screened and identified by liquid chromatography-quadrupole-time of flight mass spectrometry(LC/Q TOF MS) in rat liver microsomes.The toxicity of isocarbophos and its metabolite was assessed by the acetylcholinesterase inhibition assay.The quantification analysis of isocarbophos and its metabolite was made using a liquid chromatography-triple quadrupole tandem mass spectrometry(LC/Triple-Q MS/MS) method to investigate the metabolic kinetics of the isocarbophos and its oxidative metabolite.RESULTS Isocarbophos was rapidly eliminated in rat liver microsomes,and its t1/2 was14.6 min and the extrapolated ClH was 43.8 ml·min-1·kg-1.The major oxidative metabolite identified in incubates was its desulfuration metabolite isocarbophos oxon.The enzyme inhibition activity of the metabolite was much higher than that of isocarbophos and its IC50 was found to be four orders of magnitude lower than the parent,which indicated that the biotransformation of isocarbophos to isocarbophos oxon was a metabolic activation process.The kinetic curve of desulfuration to form isocarbophos oxon was biphasic,and the parameters obtained were Km,app1 1.12 μmol·L-1,Vmax1 0.43 μmol·min-1·g-1 protein,Km,app2 67.92 μmol·L-1 and Vmax2 1.28 μmol·min-1·g-1 protein.CONCLUSION Isocarbophos can be metabolically activated by rat hepatic microsomes to form isocarbophos oxon.Like other phosphorothioates,the metabolic activation of isocarbophos may contribute significantly to its toxicity in bodies." @default.
- W2362604100 created "2016-06-24" @default.
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- W2362604100 date "2012-01-01" @default.
- W2362604100 modified "2023-09-28" @default.
- W2362604100 title "Biotransformation and kinetics of isocarbophos in liver microsomes of rats in vitro" @default.
- W2362604100 hasPublicationYear "2012" @default.
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