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大鼠体内α-氨基苯并[b]噻吩-3-丙酸(色氨酸的硫类似物)的代谢

The metabolism of alpha-aminobenzo(b)thiophene-3-propionic acid (the sulfur analog of tryptophan) in the rat.

作者信息

Bosin T R, Bickers R G, Dinner A

出版信息

Drug Metab Dispos. 1978 Jan-Feb;6(1):31-7.

PMID:23271
Abstract

The biotransformation of 3H-labeled alpha-aminobenzo[b]thiophene-3-propionic acid (the sulfur analog of tryptophan) was investigated in rats. Forty-eight hours after ip administration, 80% of the radioactive dose was recovered in the urine and 5% in the feces; tissue levels of radioactivity accounted for the remainder of the administered dose. The urinary metabolites were identified by a combination of thin-layer chromatography, gas chromatography, and gas chromatography-mass spectrometry, and were quantitated by thin-layer chromatography and liquid-scintillation counting to give, as percentages of the administered dose, unchanged alpha-aminobenzo[b]thiophene-3-propionic acid (20.6%), benzo[b]thiophene-3-acetic acid (1.3%), benzo[b]thiophene-3-pyruvic acid (14.2%), benzo[b]thiophene-3-lactic acid (4.9%), and N-(benzo[b]thiophene-3-acetyl)glycine (46.2%).

摘要

在大鼠体内研究了3H标记的α-氨基苯并[b]噻吩-3-丙酸(色氨酸的硫类似物)的生物转化。腹腔注射48小时后,80%的放射性剂量在尿液中回收,5%在粪便中回收;放射性组织水平占给药剂量的其余部分。通过薄层色谱、气相色谱和气相色谱-质谱联用鉴定尿液代谢物,并通过薄层色谱和液体闪烁计数进行定量,以给药剂量的百分比表示,未变化的α-氨基苯并[b]噻吩-3-丙酸(20.6%)、苯并[b]噻吩-3-乙酸(1.3%)、苯并[b]噻吩-3-丙酮酸(14.2%)、苯并[b]噻吩-3-乳酸(4.9%)和N-(苯并[b]噻吩-3-乙酰基)甘氨酸(46.2%)。

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