Metabolism of bambuterol in rat liver microsomes: identification of hydroxylated and demethylated products by liquid chromatography mass spectrometry.
Metabolism of bambuterol in rat liver microsomes: identification of hydroxylated and demethylated products by liquid chromatography mass spectrometry.
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发表时间：
1989-05
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通讯作者：
C. Lindberg;C. Roos;A. Tunek;L. Svensson
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作者：
C. Lindberg;C. Roos;A. Tunek;L. Svensson
本文研究了（R，S）-班布特罗在大鼠肝微粒体中的氧化代谢。代谢产物馏分进行了分析，热喷雾LC-MS。使用氘标记和未标记班布特罗的等摩尔混合物促进了代谢产物的质谱鉴定。通过羟基化、去甲基化和水解反应，鉴定出6种代谢产物。发现脱甲基代谢物在生理条件下化学不稳定。班布特罗向特布他林的复杂生物转化可能是导致班布特罗作用持续时间长的一个因素。
The oxidative metabolism of (R,S)-bambuterol in rat liver microsomes was studied. Metabolite fractions were analyzed by thermospray LC-MS. The use of an equimolar mixture of deuterium-labeled and unlabeled bambuterol facilitated the mass spectrometric identification of the metabolites. Six metabolites, formed via hydroxylation, demethylation, and hydrolytic reactions, were identified. The demethylated metabolites were found to be chemically unstable under physiological conditions. It is likely that the complex biotransformation of bambuterol into terbutaline is one factor contributing to the long duration of action of bambuterol.