Westphal D, Lucas K, Hilbig V, Mechler U, Piasecki A
Food Chem Toxicol. 1984 Jul;22(7):521-8. doi: 10.1016/0278-6915(84)90221-7.
The biotransformation of radioactively labelled monolinuron (N-(4-chloro[U-14C]phenyl)-N'-methyl-N'-methoxyurea) was studied in the isolated perfused liver of the chicken. After a 4-hr perfusion, 83.1% of the added radioactivity was recovered, 56.6% in the perfusion medium and 26.5% in the liver and bile. The fraction of radioactivity extractable from the perfusion medium into ethyl acetate amounted to 47.8% of the added dose. In addition to monolinuron, five breakdown products were identified in this extract, namely N-(4-chlorophenyl)-N'-hydroxymethyl-N'-methoxyurea, N-(4-chlorophenyl)-N'-methoxyurea, N-(4-chlorophenyl)-N'-methylurea, 4-chlorophenylurea and 4-chloroacetanilide. Of particular interest was the absence of arylhydroxylated monolinuron derivatives, since in monolinuron-metabolism studies in the laying hen 2-hydroxy-4-chlorophenylurea and 3-hydroxy-4-chlorophenylurea were both detected. This differing metabolism corresponds to earlier findings in the rat, in which arylhydroxylated breakdown products were detected only in in vivo studies and not in rat-liver perfusion. Possible reasons for the differing metabolism of monolinuron in vivo and in vitro are discussed.
在鸡的离体灌注肝脏中研究了放射性标记的绿麦隆（N-(4-氯[U-14C]苯基)-N'-甲基-N'-甲氧基脲）的生物转化。灌注4小时后，回收了添加放射性的83.1%，其中56.6%在灌注介质中，26.5%在肝脏和胆汁中。可从灌注介质中萃取到乙酸乙酯中的放射性部分占添加剂量的47.8%。除绿麦隆外，在该萃取物中还鉴定出5种分解产物，即N-(4-氯苯基)-N'-羟甲基-N'-甲氧基脲、N-(4-氯苯基)-N'-甲氧基脲、N-(4-氯苯基)-N'-甲基脲、4-氯苯基脲和4-氯乙酰苯胺。特别令人感兴趣的是不存在芳基羟基化的绿麦隆衍生物，因为在蛋鸡的绿麦隆代谢研究中检测到了2-羟基-4-氯苯基脲和3-羟基-4-氯苯基脲。这种不同的代谢情况与在大鼠中更早的发现一致，在大鼠中，芳基羟基化分解产物仅在体内研究中检测到，而在大鼠肝脏灌注研究中未检测到。讨论了绿麦隆在体内和体外代谢不同的可能原因。
