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大鼠体内1-(邻氯苯基)-1-(对氯苯基)-2,2-二氯乙烷(邻,对'-滴滴滴)的代谢

Metabolism of 1-(0-chlorophenyl)-1-(p-chlorophenyl)-2,2-dichloroethane (o,p'-DDD) in rats.

作者信息

Reif V D, Sinsheimer J E

出版信息

Drug Metab Dispos. 1975 Jan-Feb;3(1):15-25.

PMID:234830
Abstract

The metabolism of 14C-labeled 1-(p-chlorophenyl)-2,2-dichloroethane (o,p'-DDD) in rats was investigated. Metabolites were identified in feces and urine extracts by thin-layter chromatography (TLC), gas-liquid chromatography, and mass spectropmetry. Extracts of acidic metabolites were methylated with diazomethane for identification. Metabolites were quantitated by TLC and liquid scintillation counting. After a 100-mg oral dose to each of three rats, an average of 7.1% of the radioactivity was excreted in the urine and 87.8% in the feces within 8 days. The urine was found to contain o,p'-dichlorodiphenylacetic acid (o,p'-DDA) as well as 4-hydroxy-, 3-hydroxy-, and 3,4-dihydroxy-substituted o,p'-DDA. The serine and glycine conjugates of o,p'-DDA were also identified. In addition to the above metabolites the feces contained o,p'-DDD. 1-(o-chlorophenyl)-1-(P-chlorophenyl)-2-chloroethylene, and the aspartic acid conjugate of o,p'-DDA. The presence of aromatic mono- and dihydroxylated o,p'-DDD was also detected in feces.

摘要

研究了大鼠体内14C标记的1-(对氯苯基)-2,2-二氯乙烷(邻,对'-滴滴滴)的代谢情况。通过薄层色谱法(TLC)、气液色谱法和质谱法在粪便和尿液提取物中鉴定代谢产物。酸性代谢产物提取物用重氮甲烷甲基化以进行鉴定。代谢产物通过TLC和液体闪烁计数进行定量。给三只大鼠每只口服100毫克剂量后,在8天内平均有7.1%的放射性从尿液中排出,87.8%从粪便中排出。发现尿液中含有邻,对'-二氯二苯乙酸(邻,对'-DDA)以及4-羟基-、3-羟基-和3,4-二羟基取代的邻,对'-DDA。还鉴定出了邻,对'-DDA的丝氨酸和甘氨酸共轭物。除上述代谢产物外,粪便中还含有邻,对'-滴滴滴、1-(邻氯苯基)-1-(对氯苯基)-2-氯乙烯以及邻,对'-DDA的天冬氨酸共轭物。在粪便中还检测到了芳香族单羟基化和二羟基化的邻,对'-滴滴滴。

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