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1,2,4-三甲基苯(假枯烯)在大鼠体内的分布与代谢

Distribution and metabolism of 1,2,4-trimethylbenzene (pseudocumene) in the rat.

作者信息

Huo J Z, Aldous S, Campbell K, Davies N

机构信息

School of Pharmacy, University of Tasmania, Australia.

出版信息

Xenobiotica. 1989 Feb;19(2):161-70. doi: 10.3109/00498258909034688.

Abstract
  1. Single doses of 1,2,4-trimethylbenzene (124TMB) or 14C-124TMB were administered orally to rats for metabolism and distribution studies. 2. 14C-124TMB was rapidly and widely distributed throughout the body with the highest levels in adipose tissue. No other preferential uptake of 14C-124TMB by any of the organs or tissues examined was evident. 3. Tissue levels declined rapidly within 24 h after dosage, with more than 99% of the administered radioactivity recovered in the urine during this period. 4. A complex mixture of isomeric trimethylphenols, dimethylbenzyl alcohols, dimethylbenzoic acids and dimethylhippuric acids excreted in the urine accounted for more than 81% of the administered dose. The major metabolites were 3,4-dimethylhippuric acid (30.2% dose), 2,4-dimethylbenzyl alcohol (12.7% dose, primarily as sulphate and glucuronide conjugates) and 2,5-dimethylbenzyl alcohol (11.7% dose, primarily as sulphate and glucuronide conjugates).
摘要
  1. 给大鼠口服单剂量的1,2,4-三甲基苯(124TMB)或14C-124TMB,用于代谢和分布研究。2. 14C-124TMB在体内迅速且广泛分布,脂肪组织中的含量最高。在所检查的任何器官或组织中,均未发现14C-124TMB有其他优先摄取现象。3. 给药后24小时内,组织水平迅速下降,在此期间,超过99%的给药放射性在尿液中回收。4. 尿液中排出的异构三甲基苯酚、二甲基苄醇、二甲基苯甲酸和二甲基马尿酸的复杂混合物占给药剂量的81%以上。主要代谢产物为3,4-二甲基马尿酸(占剂量的30.2%)、2,4-二甲基苄醇(占剂量的12.7%,主要为硫酸盐和葡糖醛酸共轭物)和2,5-二甲基苄醇(占剂量的11.7%,主要为硫酸盐和葡糖醛酸共轭物)。

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