含有3,4-亚甲基二氧苯基的几种羧酸衍生物的大鼠代谢。

J Klungsøyr, R R Scheline
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引用次数: 12

摘要

研究了扁桃酸(1)、苯乙酸(2)、苯甲酸(3)、3-苯丙酸(4)和肉桂酸(5)的3,4-亚甲二氧基衍生物在大鼠体内的代谢。灌胃剂量(1 mmol/kg)后,化合物及其代谢物在24小时内随尿液排出。回收率约为85%。除化合物(1)在排泄时基本保持不变外,甘氨酸偶联物是主要的尿代谢产物。化合物(2)生成3,4-亚甲二氧苯乙酰甘氨酸,而化合物(3)、(4)和(5)转化为3,4-亚甲二氧苯甲酰甘氨酸。没有证据表明任何化合物与去甲基化和随后的儿茶酚代谢物排泄有关。
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Metabolism in rats of several carboxylic acid derivatives containing the 3,4-methylenedioxyphenyl group.

The metabolism of the 3,4-methylenedioxy derivatives of mandelic acid (1), phenylacetic acid (2), benzoic acid (3), 3-phenylpropionic acid (4) and cinnamic acid (5) was studied in rats. Following intragastric dosage (1 mmol/kg) the compounds and their metabolites were excreted in the urine within 24 hrs. Recoveries of roughly 85% were obtained. Except for compound (1) which was excreted to a large extent unchanged, glycine conjugates were the major urinary metabolites. Compound (2) formed 3,4-methylenedioxyphenylacetylglycine whereas compounds (3), (4) and (5) were converted to 3,4-methylenedioxybenzoylglycine. No evidence was found with any of the compounds for demethylenation and subsequent excretion of catecholic metabolites.

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