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Wistar大鼠和Gunn大鼠中三[14C]甲基 -(3 - 羟基苯基)碘化铵的胆汁排泄差异。

Differences between the biliary excretion of tri [14C] methyl-(3-hydroxy-phenyl) ammonium iodide in Wistar and Gunn rats.

作者信息

Calvey T N, Somani S M, Wright A

出版信息

Biochem J. 1970 Oct;119(4):659-63. doi: 10.1042/bj1190659.

Abstract
  1. The biliary excretion of [(14)C]trimophonium iodide [tri[(14)C]methyl(3-hydroxyphenyl)ammonium iodide] was studied in normal Wistar animals and in jaundiced homozygous Gunn rats. 2. In normal Wistar rats small amounts of radioactivity (approx. 3% of the dose in 4h) were excreted in bile as two glucuronide conjugates, i.e. [(14)C]trimophonium glucuronide [tri[(14)C]methyl-(3-oxyphenyl)ammonium glucuronide] (85%) and 3-di[(14)C]methylaminophenyl glucuronide (10-15%). Only minor amounts of the unchanged drug were detected in bile. 3. In the homozygous jaundiced Gunn rat large amounts of radioactivity (26% of the dose in 4h) were eliminated in bile as [(14)C]trimophonium glucuronide alone. The quantitative excretion of this metabolite in Gunn rat bile was about ten times that in normal animals. 4. It is proposed that the biochemical lesion in the homozygous Gunn rat may indirectly affect the biliary transport of exogenous glucuronides across the canalicular membrane.
摘要
  1. 在正常Wistar动物和黄疸纯合子Gunn大鼠中研究了碘化[(14)C]曲莫铵[三[(14)C]甲基(3-羟基苯基)氯化铵]的胆汁排泄情况。2. 在正常Wistar大鼠中,少量放射性物质(4小时内约占剂量的3%)以两种葡萄糖醛酸结合物的形式经胆汁排泄,即[(14)C]曲莫铵葡萄糖醛酸苷[三[(14)C]甲基-(3-氧代苯基)氯化铵葡萄糖醛酸苷](85%)和3-二[(14)C]甲基氨基苯基葡萄糖醛酸苷(10 - 15%)。在胆汁中仅检测到少量未变化的药物。3. 在纯合子黄疸Gunn大鼠中,大量放射性物质(4小时内占剂量的26%)仅以[(14)C]曲莫铵葡萄糖醛酸苷的形式经胆汁消除。这种代谢物在Gunn大鼠胆汁中的定量排泄约为正常动物的10倍。4. 有人提出,纯合子Gunn大鼠的生化损伤可能间接影响外源性葡萄糖醛酸结合物跨胆小管膜的胆汁转运。

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