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大鼠、猴和人体内3,4,4'-三氯碳酰替苯胺的生物转化产物

Biotransformation products of 3,4,4'-trichlorocarbanilide in rat, monkey, and man.

作者信息

Birch C G, Hiles R A, Eichhold T H, Jeffcoat A R, Handy R W, Hill J M, Willis S L, Hess T R, Wall M E

出版信息

Drug Metab Dispos. 1978 Mar-Apr;6(2):169-76.

PMID:26533
Abstract

3,4,4'-Trichlorocarbanilide (TCC), uniformly labeled with 14C in the monochloro ring, was administered to rats, rhesus monkeys, and humans. Radioactive materials in the plasma and urine of all three species and in the bile of rats and monkeys were separated by high performance liquid chromatography. The chromatography showed great similarity between the monkey and the human. Principal metabolites common to all species were the sulfate and glucuronide conjugates of 2'-, 3'-, and 6-hydroxy-TCC. The rat also produced the glucuronide and sulfate conjugates of 2',6-dihydroxy-TCC. The major urinary excretion products found in humans and monkeys were the N- and N'-TCC glucuronides.

摘要

3,4,4'-三氯碳酰替苯胺(TCC),其单氯环用¹⁴C均匀标记,被给予大鼠、恒河猴和人类。通过高效液相色谱法分离了这三个物种的血浆、尿液以及大鼠和猴子胆汁中的放射性物质。色谱分析表明猴子和人类之间有很大的相似性。所有物种共有的主要代谢产物是2' -、3' -和6 -羟基-TCC的硫酸盐和葡糖醛酸苷缀合物。大鼠还产生了2',6 -二羟基-TCC的葡糖醛酸苷和硫酸盐缀合物。在人类和猴子中发现的主要尿排泄产物是N -和N'-TCC葡糖醛酸苷。

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