Sapota Andrzej, Czerski Bogdan, Jedrzejczak Marian
Department of Toxicology, Medical University, Lódź, Poland.
Int J Occup Med Environ Health. 2003;16(4):351-7.
The principal commercial use of o-anisidine is believed to be as an intermediate in the manufacture of dyes. It has also been reported to be an intermediate in the manufacture of synthetic guaiacol and its derivatives. o-Anisidine is an urinary bladder carcinogen in mice and rats. The aim of the study was to investigate the kinetics of body distribution, excretion and biotransformation of o-anisidine in rats following a single, intraperitoneal administration.
The tissue distribution and excretion of o-anisidine following i.p. administration of a single dose of 10 mg/kg was investigated using radiotracer [3H]. Metabolism of o-anisidine was investigated in the rats following i.p. administration of a single dose of 50 mg/kg using GC/MS technique.
After 72 h, about 72% of the given dose was excreted in urine. As indicated, urine proved to be the main route of tritium excretion. In all examined tissues, the highest concentrations of tritium were found 12 h after injection and the highest accumulation was detected in the liver, kidneys and in the muscle tissue. In urine, the following substances were identified and quantified by GC peak areas: N-acetyl-2-methoxyaniline and N-acetyl-4-hydroxy-2-methoxyaniline.
Prolonged tritium retention observed in the majority of tissues indicated that o-anisidine, especially in the case of repeated exposure, might accumulate in the body. The metabolism encompasses amine group acetylation and ring oxidation.
邻氨基苯甲醚的主要商业用途据信是作为染料制造中的中间体。也有报道称它是合成愈创木酚及其衍生物制造中的中间体。邻氨基苯甲醚在小鼠和大鼠中是膀胱致癌物。本研究的目的是调查大鼠单次腹腔注射后邻氨基苯甲醚在体内的分布、排泄和生物转化动力学。
使用放射性示踪剂[³H]研究了腹腔注射单剂量10mg/kg后邻氨基苯甲醚的组织分布和排泄情况。使用气相色谱/质谱技术研究了腹腔注射单剂量50mg/kg后大鼠体内邻氨基苯甲醚的代谢情况。
72小时后，约72%的给药剂量经尿液排出。如所示，尿液被证明是氚排泄的主要途径。在所有检测的组织中，注射后12小时氚的浓度最高，且在肝脏、肾脏和肌肉组织中检测到最高蓄积量。在尿液中，通过气相色谱峰面积鉴定并定量了以下物质：N-乙酰基-2-甲氧基苯胺和N-乙酰基-4-羟基-2-甲氧基苯胺。
在大多数组织中观察到的氚长时间滞留表明，邻氨基苯甲醚，尤其是在重复暴露的情况下，可能会在体内蓄积。其代谢包括胺基乙酰化和环氧化。
