Studies of the arylhydroxylation of monochlorophenylureas in the isolated perfused rat liver

D. Westphal, K. Lucas, V. Hilbig
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引用次数: 3

Abstract

Biotransformation studies with phenylurea and the three isomers of monochlorophenylurea were performed using an isolated perfused rat-liver preparation. In the perfusate and the bile, ring-hydroxylation was detected only with phenylurea and with o- and m-chlorophenylurea, and yielded the corresponding p-hydroxylated compounds in each case, while with p-chlorophenylurea no ring hydroxylation was observed at the ortho or meta position. Similar results were obtained with the arylhydroxylation of the herbicide monolinuron (3-(4-chlorophenyl)-1-methoxy-1-methylurea) in the perfused rat liver. In contrast, studies of monolinuron biotransformation in vivo in rats, pigs and hens showed that ring hydroxylation at the ortho or meta position was the main degradation step. The possible reasons for the difference in biotransformation in vivo and in vitro are discussed.

单氯苯脲在离体灌注大鼠肝脏中芳基羟基化的研究
用离体大鼠肝灌注制剂对苯脲和三种单氯苯脲异构体进行了生物转化研究。在灌注液和胆汁中,仅与苯脲、邻氯苯脲和间氯苯脲发生环羟基化反应,并产生相应的对羟基化化合物,而与对氯苯脲在邻位和间位均未发生环羟基化反应。除草剂monolinuron的芳基羟基化(3-(4-氯苯基)-1-甲氧基-1-甲基脲)在灌注的大鼠肝脏中也得到了类似的结果。相比之下,在大鼠、猪和母鸡的体内生物转化研究表明,在正位或中间位的环羟基化是主要的降解步骤。讨论了体内和体外生物转化差异的可能原因。
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