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具有利胆活性的新型胆道平滑肌松弛剂3-(2',4',5'-三乙氧基苯甲酰基)丙酸的代谢。II. 大鼠重复给药后的代谢及其与利胆活性的关系。

Metabolism of 3-(2', 4', 5'-triethoxybenzoyl) propionic acid, a new biliary smooth muscle relaxant with choleretic activity. II. Metabolism after repeated dosing in rats, in relation to choleretic activity.

作者信息

Tanayama S, Kobayashi T, Kanai Y

出版信息

Xenobiotica. 1978 Jun;8(6):377-82. doi: 10.3109/00498257809070021.

Abstract
  1. Accumulation and possible induction in the metabolism of triethoxybenzoylpropionate were studied in rats in relation to the choleretic effect of the drug. Daily oral administration of [14 C] triethoxybenzoylpropionate showed no accumulation of drug or metabolites. Pre-treatment of rats with the drug did not induce its own metabolism or the metabolism of aminopyrine, p-nitroanisole, hexobarbital or zoxazolamine. 2. Choleresis in rats induced by triethoxybenzoylpropionate resulted from enhanced formation of the bile acid-independent fraction of canalicular origin, presumably mediated by the increased transfer of sodium into the canaliculi. This was not altered by repeated pre-treatment with the drug, in accordance with the metabolic findings.
摘要
  1. 研究了大鼠体内三乙氧基苯甲酰丙酸酯在代谢过程中的蓄积情况以及可能的诱导作用,及其与该药物利胆作用的关系。每日口服[¹⁴C]三乙氧基苯甲酰丙酸酯未显示药物或代谢物的蓄积。用该药物对大鼠进行预处理并未诱导其自身代谢或氨基比林、对硝基苯甲醚、己巴比妥或唑沙胺的代谢。2. 三乙氧基苯甲酰丙酸酯诱导大鼠利胆是由于肝小管起源的不依赖胆汁酸部分的形成增强,推测是由钠向肝小管转运增加介导的。与代谢研究结果一致,该药物的重复预处理并未改变这一情况。

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