Koster A S, Noordhoek J
J Pharmacol Exp Ther. 1983 Aug;226(2):533-8.
Glucuronidation of 1-naphthol in the rat intestinal wall was studied in isolated perfused intestinal segments. 1-Naphthol glucuronide appeared on the mucosal as well as on the serosal side of the intestinal segments irrespective of the side (mucosal and/or serosal) on which naphthol was administered. Appearance of naphthol glucuronide was linear with time. A lag phase of 3.9 +/- 0.9 and 4.3 +/- 1.0 min was observed for the appearance on the mucosal and serosal side, respectively. Total glucuronide appearance rate after serosal administration of 10 to 100 microM naphthol was 3- to 4-fold higher than after mucosal administration. It is concluded that glucuronidation after mucosal administration is limited by the entry of naphthol into the metabolizing compartment.
在离体灌注肠段中研究了大鼠肠壁中1-萘酚的葡糖醛酸化作用。无论萘酚是从肠段的哪一侧（黏膜侧和/或浆膜侧）给药，1-萘酚葡糖醛酸苷都会出现在肠段的黏膜侧和浆膜侧。萘酚葡糖醛酸苷的出现与时间呈线性关系。黏膜侧和浆膜侧出现萘酚葡糖醛酸苷的滞后时间分别为3.9±0.9分钟和4.3±1.0分钟。浆膜侧给予10至100微摩尔萘酚后葡糖醛酸苷的总出现率比黏膜侧给药后高3至4倍。结论是黏膜给药后的葡糖醛酸化作用受萘酚进入代谢区室的限制。
