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人、大鼠和豚鼠体内对羟基苯丙胺的尿液代谢产物。

Urinary metabolites of p-hydroxyamphetamine in man, rat and guinea-pig.

作者信息

Sever P S, Dring L G, Williams R T

出版信息

Xenobiotica. 1976 Jun;6(6):345-53. doi: 10.3109/00498257609151646.

DOI:10.3109/00498257609151646
PMID:969562
Abstract
  1. The metabolism of (+/-)-p-hydroxy[14C]amphetamine has been studied in the rat, guinea-pig and man. 2. Most of the administered 14C was excreted in the urine within the first 24 h (64-92%), and was present mainly as free and conjugated p-hydroxy[14C]-amphetamine. In the female rat and female guinea-pig the conjugate was a glucuronide, but in man, who received a much smaller dose, the conjugate was a sulphate ester. A sex difference in conjugation was found in the rat, the female partly conjugating the drug but not the male. 3. Small quantities (1-6% of dose) of p-hydroxynorephedrine, a putative false neurotransmitter, were found in the urine of the three species. 4. Some oxidative degradation of the side chain of p-hydroxyamphetamine occurred in rat and guinea-pig since small amounts of p-hydroxybenzoic acid (1-3%) were detected in the urine.
摘要
  1. 已在大鼠、豚鼠和人体中研究了(±)-对羟基[¹⁴C]苯丙胺的代谢情况。2. 大部分给予的¹⁴C在最初24小时内通过尿液排出(64 - 92%),并且主要以游离和结合的对羟基[¹⁴C]苯丙胺形式存在。在雌性大鼠和雌性豚鼠中,结合物是葡糖醛酸苷,但在接受剂量小得多的人体中,结合物是硫酸酯。在大鼠中发现了结合方面的性别差异,雌性部分地使药物结合而雄性则不然。3. 在这三个物种的尿液中发现了少量(剂量的1 - 6%)对羟基去甲麻黄碱,一种假定的假性神经递质。4. 在大鼠和豚鼠中,对羟基苯丙胺侧链发生了一些氧化降解,因为在尿液中检测到了少量的对羟基苯甲酸(1 - 3%)。

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