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首页> 外文会议>ASMS Conference on Mass Spectrometry and Allied Topics >A study on the main biotransformation pathways of vaptansby liquid chromatography-mass spectrometry-based techniques following in vitrometabolism assays
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A study on the main biotransformation pathways of vaptansby liquid chromatography-mass spectrometry-based techniques following in vitrometabolism assays

机译：vaptansby液相色谱 - 质谱 - 质谱型技术在葡萄干蛋白神经分析中的主要生物转化途径研究

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The analytical strategy and the in vitro protocols proposed and already successfully applied in similar, previous studies [5-6] allowed to identify 15 metabolites for lixivaptan (Fig. 2), 6 for mozavaptan (Fig. 3) and 17 for tolvaptan (Fig. 4), several of which, to the best of our knowledge, not yet reported in the scientific literature. The phase I metabolic reactions include hydroxylation in different positions, de-hydrogenation, hydrogenation, N-dealkylation, carboxylation, isomerization and combination of them. No significant differences in the phase I metabolic profile were registered after incubation of the drugs under investigation in the presence of either pooled female or male HLM. The enzymatic isoforms mainly involved in the vaptans phase I biotransformation pathways identified are the CYP3A4 and the CYP3A5. Once formed, most of the phase I metabolites were subjected to phase II reactions (glucuronidation).
机译：提出的分析策略和已经成功地应用于类似的研究[5-6]，允许鉴定15个代谢物，用于LIXIVAPTAN（图2），6用于Mozavaptan（图3）和17用于Tolvaptan（图。4），其中一些是我们所知，尚未在科学文学中报道。 I相的代谢反应包括不同位置的羟基化，脱氢，氢化，正催化剂，羧化，异构化和它们的组合。在汇集的女性或雄性HLM的存在下，在调查中孵育药物后，在孵育的药物孵育后没有显着差异。鉴定的酶IOFORM主要涉及vaptans期I生物转化途径是CYP3A4和CYP3A5。一旦形成，大多数I相代谢物受到II代反应（葡糖醛）。

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