Boobis A R, Powis G
Drug Metab Dispos. 1975 Mar-Apr;3(2):63-8.
In the isolated, blood-perfused liver of the rat, aniline is removed from the perfusion medium rapidly over the first 60 min, but more slowly over the following 120 min. The main metabolite found in the perfusion medium is an acid-labile conjugate of aniline which after 3 hr accounts for 33% of the aniline added, whereas p-aminophenol conjugates account for a further 13%. No free p-aminophenol could be detected in the perfusion medium and only a small amount in the bile. Aniline conjugates form the major metabolites found in the bile. A kinetic analysis of the data is presented and a two-compartment model is postulated in which aniline is removed for excretion in the bile or for metabolism from the first compartment. SKF 525-A, 0.2 mM, completely blocks the formation of p-aminophenol and inhibits the formation of the acid-labile aniline conjugate by 62%. There is also an increase in the size of the second compartment.
在大鼠离体、血液灌注的肝脏中，苯胺在最初60分钟内从灌注介质中快速清除，但在随后的120分钟内清除速度较慢。灌注介质中发现的主要代谢产物是苯胺的酸不稳定共轭物，3小时后占添加苯胺的33%，而对氨基苯酚共轭物再占13%。在灌注介质中未检测到游离的对氨基苯酚，在胆汁中也只有少量。苯胺共轭物是胆汁中发现的主要代谢产物。本文对数据进行了动力学分析，并提出了一个双室模型，其中苯胺从第一个室中被清除以排泄到胆汁中或进行代谢。0.2 mM的SKF 525 - A完全阻断了对氨基苯酚的形成，并将酸不稳定苯胺共轭物的形成抑制了62%。第二个室的大小也有所增加。
