Laignelet L, Rivière J L, Lhuguenot J C
Ecole Nationale Supérieure de Biologie Appliquée à la Nutrition et à l'Alimentation, Campus Universitaire Montmuzard, Dijon, France.
Food Chem Toxicol. 1992 Jul;30(7):575-83. doi: 10.1016/0278-6915(92)90191-m.
The metabolic fate and pathway of the imidazole fungicide prochloraz (1-[N-propyl-N-2-(2,4,6-trichlorophenoxy) ethyl carbamoyl] imidazole) were investigated in the rat after administration of oral single doses with radiolabelled molecules. At both dose levels (50 and 250 mg/kg body weight), virtually all of the ingested [14C-phenyl]prochloraz was excreted in the urine or faeces within 96 hr, the bulk of excretion occurring between 24 and 48 hr after dosing. Urinary elimination accounted for 61 and 68% of the respective initial doses. Urinary metabolic products were isolated and identified by thin-layer chromatography, gas chromatography or gas chromatography coupled with mass spectrometry analysis. Prochloraz was completely metabolized with no unchanged compound being excreted in the urine. The main biotransformation products in rat urine were 2,4,6-trichlorophenoxyacetic acid and its corresponding alcohol, the latter as a glucuronic acid conjugate. Ring hydroxylation also occurred, with the hydroxy-2,4,6-trichlorophenoxyethanol and hydroxy-2,4,6-trichlorophenoxyacetic acid metabolites excreted in small amounts in the urine. 2,4,6-Trichlorophenol and unconjugated 2,4,6-trichlorophenoxyethanol were identified as minor urinary metabolites.
用放射性标记分子给大鼠口服单剂量后，研究了咪唑类杀菌剂咪鲜胺（1-[N-丙基-N-2-(2,4,6-三氯苯氧基)乙基氨基甲酰基]咪唑）的代谢归宿和途径。在两个剂量水平（50和250mg/kg体重）下，几乎所有摄入的[14C-苯基]咪鲜胺在96小时内通过尿液或粪便排出，大部分排泌发生在给药后24至48小时之间。尿液排泄分别占各自初始剂量的61%和68%。通过薄层色谱、气相色谱或气相色谱与质谱联用分析分离并鉴定尿液中的代谢产物。咪鲜胺完全代谢，尿液中无未变化的化合物排出。大鼠尿液中的主要生物转化产物是2,4,6-三氯苯氧基乙酸及其相应的醇，后者以葡萄糖醛酸共轭物形式存在。也发生了环羟基化，羟基-2,4,6-三氯苯氧基乙醇和羟基-2,4,6-三氯苯氧基乙酸代谢产物少量随尿液排出。2,4,6-三氯苯酚和未结合的2,4,6-三氯苯氧基乙醇被鉴定为次要尿液代谢产物。
