METABOLISM OF OXAMNIQUINE - NEW SCHISTOSOMICIDE

METABOLISM OF OXAMNIQUINE - NEW SCHISTOSOMICIDE
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DOI:
10.1080/00034983.1976.11687128
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发表时间:
1976-01-01
影响因子:
--
通讯作者:
WOOLHOUSE, NM
WOOLHOUSE, NM
中科院分区:
其他
文献类型:
--
作者:
KAYE, B;WOOLHOUSE, NM

文献摘要

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在小鼠、大鼠、仓鼠、兔、恒河猴、犬和人体中研究了奥曲喹(6-羟甲基-7-硝基-2-异丙基氨基甲基-1,2,3,4-四氢喹啉)的代谢。尿液排泄是人体的主要消除途径。该化合物转化为2种代谢产物,主要的一种由6-羟甲基氧化成羧基而产生,另一种由侧链氧化得到2-羧酸而产生。由于仅在小鼠、家兔、仓鼠和犬的尿液中发现了可感知量的两种酸性代谢产物,因此在所用剂量水平下存在种属差异。在恒河猴和大鼠尿液中未发现2-羧酸,在人尿液中仅存在痕量。
The metabolism of oxamniquine, 6-hydroxymethyl-7-nitro-2-isopropylaminomethyl-1,2,3,4-tetrahydroquinoline, was studied in the mouse, rat, hamster, rabbit, rhesus monkey, dog and man. Urinary excretion is a major route of elimination in man. The compound is converted to 2 metabolites, the major one arising from oxidation of the 6-hydroxymethyl group to a carboxyl group and the other by oxidation of the side chain to give the 2-carboxylic acid. There is a species difference at the dose levels used since both acidic metabolites were found in appreciable quantities only in the urine of mouse, rabbit, hamster and dog. The 2-carboxylic acid was not found in the urine of rhesus monkey and rat and occurred in only trace amounts in human urine.