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赛坦贝在大鼠和犬体内的代谢情况。

Metabolic disposition of cytembena in rats and dogs.

作者信息

Mitoma C, Saito T, Howd R A

出版信息

Xenobiotica. 1977 Mar;7(3):165-79. doi: 10.3109/00498257709036248.

Abstract
  1. The metabolic disposition of cytembena (sodium cis-3-p-methoxybenzoyl-3-bromoacrylate)labelled at both carbonyl carbon atoms was studied in rats and dogs. 2. Rats excreted over 70% and dogs excreted over 50% of the radioactive dose in 24 h. Most of the radioactivity was found in urine. Kidney retained the highest level of radioactivity after 24 h. Renal cortex was responsible for the observed high retention. Both species exhibited similar tissue distribution and urinary metabolic patterns. 3. Cytembena was metabolized by demethylation catalysed by microsomes and by debromination and double bond saturation catalysed by the 100,000 g supernatant fraction in the presence of glutathione and NADPH. Tentative structures of the metabolites identified by mass spectrometry and the probable metabolic pathway of cytembena are presented,
摘要
  1. 在大鼠和狗体内研究了羰基碳原子均被标记的环丙苄星(顺式-3-对甲氧基苯甲酰基-3-溴丙烯酸酯钠)的代谢情况。2. 大鼠在24小时内排出超过70%的放射性剂量,狗在24小时内排出超过50%的放射性剂量。大部分放射性物质存在于尿液中。24小时后肾脏保留的放射性水平最高。肾皮质是观察到的高保留率的原因。两种动物均表现出相似的组织分布和尿液代谢模式。3. 环丙苄星在微粒体催化的去甲基化作用下以及在谷胱甘肽和NADPH存在时由100,000g上清液组分催化的脱溴和双键饱和作用下发生代谢。给出了通过质谱鉴定的代谢产物的暂定结构以及环丙苄星可能的代谢途径。

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