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[大鼠体内阿伏苯唑的代谢]

[Afobazole metabolism in rats].

作者信息

Seredenin S B, Viglinskaia A O, Mozhaeva T Ia, Kolyvanov G B, Litvin A A, Avdiunina N I, Savel'ev V L, Zgerdev V P

出版信息

Eksp Klin Farmakol. 2008 Mar-Apr;71(2):50-2.

Abstract

Metabolism of afobazole in rats has been studied using mass-spectrometry and HPLC, which revealed 17 products of afobazole biotransformation along with the parent compound. The structures of six afobazole metabolites were established and confirmed by comparison of HPLC retention times with the synthetic reference compounds and HPLC/mass spectrometry. Other metabolites were characterized by the masses of molecular ions. A significant fraction of the drug dose is biotransformed with the formation of hydroxylated benzimidazole moiety and oxidated morpholine.

摘要

已使用质谱法和高效液相色谱法研究了大鼠体内阿福唑的代谢情况,结果显示除母体化合物外,阿福唑还有17种生物转化产物。通过将高效液相色谱保留时间与合成参考化合物以及高效液相色谱/质谱法进行比较,确定并证实了六种阿福唑代谢物的结构。其他代谢物通过分子离子质量进行表征。相当一部分药物剂量会发生生物转化,形成羟基化苯并咪唑部分和氧化吗啉。

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