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(±)-甲基麻黄碱在大鼠和人体中的代谢

The metabolism of (+-)-methylephedrine in rat and man.

作者信息

Inoue T, Suzuki S

机构信息

National Research Institute of Police Science, Tokyo, Japan.

出版信息

Xenobiotica. 1990 Jan;20(1):99-106. doi: 10.3109/00498259009046816.

Abstract
  1. Urinary metabolites of methylephedrine and their excretion after oral administration to rat and human volunteers have been studied. 2. The unchanged drug, ephedrine, norephedrine, their aromatic hydroxylated compounds and methylephedrine N-oxide were found in rat urine. The same metabolites, except the p-hydroxylated metabolites, were detected in human urine. The most abundant metabolite in rat urine was methylephedrine N-oxide, and in human urine was the unchanged drug. 3. Metabolites excreted in three days after administration of the drug to rat amounted to about 54% of the dose and those after administration to man, 70-72%.
摘要
  1. 已对甲基麻黄碱的尿液代谢产物及其在大鼠和人类志愿者口服给药后的排泄情况进行了研究。2. 在大鼠尿液中发现了未变化的药物、麻黄碱、去甲麻黄碱、它们的芳香族羟基化化合物以及甲基麻黄碱N - 氧化物。在人类尿液中检测到了相同的代谢产物,但对羟基化代谢产物除外。大鼠尿液中最丰富的代谢产物是甲基麻黄碱N - 氧化物,而人类尿液中是未变化的药物。3. 给大鼠给药后三天内排泄的代谢产物约占剂量的54%,给人类给药后则为70 - 72%。

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