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Gender-related differences in metabolism of the enantiomers of trans tramadol and trans O-demethyltramadol in rat liver microsomes

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Author:
No author available
Journal Title:
ACTA PHARMACEUTICA SINICA
Issue:
8
DOI:
10.3321/j.issn:0513-4870.2004.08.002
Key Word:
反式曲马朵;反式氧去甲基曲马朵;立体选择性代谢;肝微粒体

Abstract: 目的研究反式曲马朵(trans T)对映体代谢,反式氧去甲基曲马朵(M1)对映体生成及其与葡糖醛酸结合的性别差异.方法以trans T或M1为底物分别与大鼠肝微粒体孵育,高效毛细管电泳法测定孵育液中trans T和M1对映体.结果与(+)-对映体相比,(-)-trans T优先代谢,(-)-M1优先生成.在雌性大鼠肝微粒体中(-)-M1优先与葡糖醛酸结合;M1两对映体生成及其与葡糖醛酸结合的CLint比值偏离1的程度较大.在雄性大鼠肝微粒体中(+)-M1优先与葡糖醛酸结合.结论Trans T代谢,M1生成及其与葡糖醛酸结合均具立体选择性和性别差异;M1生成及其与葡糖醛酸结合立体选择性的程度以雌性大鼠的较高.

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