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N-三苯甲基吗啉在犬和大鼠体内的代谢。

The metabolism of N-triphenylmethylmorpholine in the dog and rat.

作者信息

Griffiths M H

出版信息

Biochem J. 1968 Aug;108(5):731-40. doi: 10.1042/bj1080731.

Abstract
  1. Rats were given N-triphenyl[(14)C]methylmorpholine, triphenyl[(14)C]carbinol, N-triphenylmethyl[G-(3)H]morpholine or [G-(3)H]morpholine as single oral doses; the routes of excretion were examined. 2. Dogs were given single oral doses of N-triphenyl[(14)C]methylmorpholine. 3. (14)C-labelled metabolites were excreted mainly in the faeces in both rats and dogs; no (14)CO(2) was expired and less than 3% remained in the carcass and skin after 96hr. 4. (3)H-labelled metabolites were excreted rapidly in urine; part of the label was found in the expired gases and over 10% remained in the carcass and skin after 96hr. 5. Differences in excretion pattern between the sexes were noticed in rats but not in dogs. 6. N-Triphenylmethylmorpholine was rapidly hydrolysed to form triphenylcarbinol and morpholine in the stomach; morpholine was absorbed rapidly and excreted largely unchanged, though some was degraded, since some of the (3)H was found in water. 7. Triphenylcarbinol was absorbed only slowly and was oxidized to p-hydroxyphenyldiphenylcarbinol. 8. Both triphenylcarbinol and its p-hydroxy derivative were found in urine, bile and faeces in the free form and conjugated with glucuronic acid. The proportion of conjugates was higher in rat bile than in faeces. 9. Traces of o-hydroxyphenyldiphenylcarbinol and m-hydroxyphenyldiphenylcarbinol were detected as metabolites both free and conjugated.
摘要
  1. 给大鼠单次口服N-三苯基[(14)C]甲基吗啉、三苯基[(14)C]甲醇、N-三苯基甲基[G-(3)H]吗啉或[G-(3)H]吗啉;检查排泄途径。2. 给狗单次口服N-三苯基[(14)C]甲基吗啉。3. (14)C标记的代谢产物在大鼠和狗体内主要经粪便排泄;没有呼出(14)CO2,96小时后 carcass和皮肤中残留量不到3%。4. (3)H标记的代谢产物迅速经尿液排泄;部分标记物在呼出气体中被发现,96小时后 carcass和皮肤中残留量超过10%。5. 在大鼠中注意到两性排泄模式存在差异,但在狗中未发现。6. N-三苯基甲基吗啉在胃中迅速水解形成三苯基甲醇和吗啉;吗啉迅速吸收且大部分未发生变化地排泄,不过有一些被降解,因为在水中发现了一些(3)H。7. 三苯基甲醇吸收缓慢,被氧化为对羟基苯基二苯基甲醇。8. 三苯基甲醇及其对羟基衍生物以游离形式和与葡萄糖醛酸结合的形式存在于尿液、胆汁和粪便中。结合物在大鼠胆汁中的比例高于粪便。9. 检测到痕量的邻羟基苯基二苯基甲醇和间羟基苯基二苯基甲醇作为游离和结合的代谢产物。

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