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目的研究罗丹宁衍生物Lj0104在大鼠体内的主要代谢产物。方法对雄性SD大鼠采用口服和静脉注射两种给药方式,给药剂量为5.0 mg/kg(口服)和1.0 mg/kg(静脉注射)。在24 h内眼眶取血,采用质谱方法对血浆中母体化合物及代谢产物进行分析。结果发现Lj0104有3种主要代谢产物。结论化合物Lj0104主要代谢为水解和羟基化产物。该研究为进一步对该化合物进行结构改造提供了实验及理论依据。
Objective To study the main metabolites of rhodanine derivative Lj0104 in rats. Methods Male Sprague-Dawley rats were administered orally and intravenously at doses of 5.0 mg / kg (oral) and 1.0 mg / kg (iv). The orbital blood was taken within 24 hours and the plasma samples of maternal compounds and metabolites were analyzed by mass spectrometry. The results showed that Lj0104 has three main metabolites. Conclusion Compound Lj0104 is mainly metabolized to the hydrolyzed and hydroxylated products. The research provided experimental and theoretical basis for further structural transformation of the compound.