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In vitro analysis on pharmacokinetics by microsomesfrom recombinant CYP3A46 cell lines |
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Abstract: |
The objective was to provide a scientific basis for the use of Bama miniature pig as a clinlical experimental
animal by comparatively analyzing pharmacokinetic parameters of microsomes from stably expressing recombinant cell lines
human CYP3A4 and Sus scrofa CYP3A46-Bama. The results demonstrated that the metabolic activities of microsomes from
recombiant cell lines CYP3A46 to nifedipine and testosterone were very close to that of CYP3A4 based on the analysis of
pharmacokinetic parameters Vmax, Km(S50) and Clint, so were the inhibitory activities of ketoconazole to CYP3A46 and
CYP3A46 based on IC50s. Further researches should do to determine whether human CYP3A4 and Sus scrofa CYP3A46
were homologous enzymes. |
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