Metabolism of diazepam in vitro by human liver. Independent variability of N-demethylation and C3-hydroxylation.
Metabolism of diazepam in vitro by human liver. Independent variability of N-demethylation and C3-hydroxylation.
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人肝脏对地西泮的体外代谢。
DOI：
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发表时间：
1988
期刊：
影响因子：
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通讯作者：
W. Kalow
中科院分区：
文献类型：
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作者：
T. Inaba;A. Tait;M. Nakano;W. Mahon;W. Kalow
使用人类肝脏研究了地西泮代谢的个体差异。通过气相色谱法监测N-去甲基地西泮（NDZ）和3-羟基地西泮（替马西泮，TMZ）的形成。在 10 个肝脏中，NDZ 和 TMZ 形成的 Km 值彼此独立变化，各变化 4 倍，从 100 到 400 microM。这种变异性与至少两种控制这些代谢物形成的不同细胞色素 P-450 物种的存在相一致。在相同的肝脏中，NDZ 和 TMZ 产生的 Vmax 分别变化 6 倍和 15 倍。
The interindividual variability of diazepam metabolism was studied using human livers. The formation of N-desmethyldiazepam (NDZ) and 3-hydroxydiazepam (temazepam, TMZ), was monitored by gas chromatography. In 10 livers, Km values for NDZ and TMZ formation varied independently from each other, each by a factor of 4, from 100 to 400 microM. This variability is consistent with the presence of at least two different cytochrome P-450 species controlling formation of these metabolites. In the same livers, Vmax for NDZ and TMZ production varied 6-fold and 15-fold, respectively.