生物活性 | |||
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描述 | Cytochrome P450 comprises a superfamily of structurally and functionally related isoenzymes which are involved in the metabolism of a diverse range of both exogenous and endogenous compounds. Furafylline is a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC50 value of 0.07 µM. Furafylline is a highly selective inhibitor of P450IA2 in man. Furafylline is also a potent inhibitor of the N3-demethylation of caffeine and of a component of the N1- and N7-demethylation suggesting that caffeine is a selective substrate of a hydrocarbon-inducible isoenzyme of P450 in man. Furafylline is a methylxanthine derivative that is introduced as a long-acting replacement for theophylline in the treatment of asthma. Administration of furafylline was associated with an elevation in plasma levels of caffeine, due to inhibition of caffeine oxidation, a reaction catalysed by one or more hydrocarbon-inducible isoenzymes of P450[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.84mL 0.77mL 0.38mL |
19.21mL 3.84mL 1.92mL |
38.42mL 7.68mL 3.84mL |
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