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在DBA/lac小鼠中经肠胃外给予14C标记化合物后,香豆素、7-羟基香豆素及其7-羟基代谢物的组织分布情况。

Tissue distribution of coumarin, 7-hydroxycoumarin and their 7-hydroxy metabolites following parenteral administration of 14C-labeled compound in the DBA/lac mouse.

作者信息

Ritschel W A, Hardt T

出版信息

Arzneimittelforschung. 1983;33(6):836-40.

PMID:6684437
Abstract

The time related tissue distributions of coumarin (C), 7-hydroxycoumarin (7HC) and their metabolites were studied in DBA/lac mice following retro-orbital injection of 14C-labeled compound. The activity was determined as dpm/ml or g wet weight over a period of 120 min. C was found in blood, kidney, liver, muscle, brain, heart, lung and fat but not in the testes. Upon C dosing, 7HC was found in kidney, liver and lung; 7-hydroxycoumarin glucuronide (7HCG) was found in blood, kidney and liver; 7-hydroxycoumarin sulfate (7HCS) was found in the blood, kidney and lung. Unidentified glucuronide and sulfate metabolites were detected in blood, kidney, liver and lung. Two unidentified unconjugated metabolites were detected in the kidney and liver. Unidentified water soluble metabolites were detected in kidney, liver, muscle, heart and testes. Upon 7HC dosing only 7HC, 7HCG and 7HCS were detected in any organ. 7HC and 7HCG were found in blood, kidney, liver, muscle and lung. 7HCS was detected in blood, kidney, liver and lung. Upon both C and 7HC dosing the kidney and liver contained the highest levels of radioactivity.

摘要

在向DBA/lac小鼠眶后注射14C标记的香豆素(C)、7-羟基香豆素(7HC)及其代谢产物后,研究了它们随时间的组织分布情况。在120分钟的时间段内,活性以每分钟衰变数/毫升或克湿重表示。在血液、肾脏、肝脏、肌肉、大脑、心脏、肺和脂肪中发现了C,但在睾丸中未发现。给予C后,在肾脏、肝脏和肺中发现了7HC;在血液、肾脏和肝脏中发现了7-羟基香豆素葡萄糖醛酸苷(7HCG);在血液、肾脏和肺中发现了7-羟基香豆素硫酸盐(7HCS)。在血液、肾脏、肝脏和肺中检测到了未鉴定的葡萄糖醛酸苷和硫酸盐代谢产物。在肾脏和肝脏中检测到了两种未鉴定的未结合代谢产物。在肾脏、肝脏肌肉、心脏和睾丸中检测到了未鉴定的水溶性代谢产物。给予7HC后,在任何器官中仅检测到7HC、7HCG和7HCS。在血液、肾脏、肝脏、肌肉和肺中发现了7HC和7HCG。在血液、肾脏、肝脏和肺中检测到了7HCS。给予C和7HC后,肾脏和肝脏中的放射性水平最高。

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