Turnbull L B, Teng L, Newman J, Bruce R B, Maynard W R
Drug Metab Dispos. 1976 Jul-Aug;4(4):379-86.
Studies with a 14C-labeled sample have shown that the title compound A is readily absorbed and very rapidly excreted by the rat, dog, and man. The metabolites result from aromatic ring hydroxylation, oxidation, and dealkylation of the urea methyl group, and oxidative ring opening of the pyrrolidine ring. Rat metabolites were 3-(3-chloro-4-hydroxyphenoxy)-N-methyl-l-pyrrolidinecarboxamide (C) 3-(3-chloro-4-hydroxyphenoxy)-1-pyrrolidinecarboxamide (D), 3-(3-chlorohydroxyphenoxy)-1-pyrrolidinecarboxamide (E), 3-(3-chlorophenoxy)-4([(methylamino)-carbonyl]amino)butanoic acid (G), 3-(3-chlorophenoxy)-4[(aminocarbonyl)amino]butanoic acid (H). Dog metabolites were C, D, G, and H. Human metabolites were 3-(3-chloro-4-hydroxyphenoxy)-N-formyl-l-pyrrolidinecarboxamide (F), C, D, G, and H. An electron-capture gas chromatographic assay for the parent compound is described. Whole-body autoradiograms of rat slices and the tissue residue data from these slices are reported and indicate rapid tissue depletion of radioactivity.
对一个用¹⁴C标记的样品进行的研究表明，标题化合物A能被大鼠、狗和人迅速吸收并极快地排泄。代谢产物源于芳环羟基化、氧化、脲甲基脱烷基化以及吡咯烷环的氧化开环。大鼠的代谢产物有3-(3-氯-4-羟基苯氧基)-N-甲基-1-吡咯烷甲酰胺（C）、3-(3-氯-4-羟基苯氧基)-1-吡咯烷甲酰胺（D）、3-(3-氯羟基苯氧基)-1-吡咯烷甲酰胺（E）、3-(3-氯苯氧基)-4([(甲氨基)-羰基]氨基)丁酸（G）、3-(3-氯苯氧基)-4[(氨基羰基)氨基]丁酸（H）。狗的代谢产物有C、D、G和H。人的代谢产物有3-(3-氯-4-羟基苯氧基)-N-甲酰基-1-吡咯烷甲酰胺（F）、C、D、G和H。描述了一种用于母体化合物的电子捕获气相色谱分析法。报告了大鼠切片的全身放射自显影片以及这些切片的组织残留数据，这些数据表明放射性在组织中迅速消耗。
