Metabolism of14C-leptophos in the rat
Metabolism of14C-leptophos in the rat
复制标题
14C-细磷在大鼠体内的代谢
DOI：
10.1007/bf02097784
复制
发表时间：
1977
影响因子：
4
通讯作者：
S. I. Mohammed
中科院分区：
文献类型：
--
作者：
A. Hassan;F. Abdel;S. I. Mohammed
用~(14)C-苯基和~(14)C-甲基标记杀虫剂研究了[O-(4-溴-2，5-二氯苯基)O-甲基苯基硫代膦]在大鼠体内的代谢去向。口服单剂量14C-苯基列磷(15 mg/kg)后，尿液中14C活性的46%至75%在9天后恢复。尿液代谢物中含有O-甲基苯基膦酸、O-甲基苯基硫代膦酸和苯基膦酸，以及两种性质不明的代谢物。体内瘦磷和/或其氧类似物的脱甲基化程度很小，从14C-甲基瘦肉精呼出的空气中排出的14CO2证实了这一点。杀虫剂似乎积聚在大网膜和皮下脂肪中，因为在给药12周后，脂肪中仍然存在微量的杀虫剂。对乙酰胆碱酯酶抑制动力学的研究表明，氧合酶是最有效的抑制剂。降解产物一般为弱抑制剂。
The metabolic fate of leptophos [O-(4-Bromo-2,5-dichlorophenyl)O-methyl phenyl phosphonothioate] in the rat was investigatedin vivo, using14C-phenyl and14C-methyl-labeled insecticide. Following the administration of a single oral dose of14C-phenyl leptophos (15 mg/kg) 46 to 75% of the14C-activity was recovered after nine days, in the urine. No radioactivity was eliminated in the expired air.O-methyl phenylphosphonic,O-methyl phenylphosphonothioic and phenylphosphonic acids were identified among the urinary metabolites, together with two metabolites of unknown nature. Demethylation of leptophos and/or its oxygen analog occurredin vivo to a small extent, as confirmed by the elimination of14CO2 in the expired air, from14C-methyl leptophos.The insecticide seemed to accumulate in omental and subcutaneous fat since traces were still found in fat 12 weeks after administration of the chemical. A study of the kinetics of acetylcholinesterase inhibition revealed that the oxon was the most potent inhibitor. The degradation products were generally weak inhibitors.