The metabolism of flufenpyr-ethyl [ethyl 2-chloro-5-[1,6-dihydro-5-methyl-6-oxo-4-(trifluoromethyl)pyridazin-1-yl]-4-fluorophenoxyacetate] was examined in rats and mice. [Phenyl-¹⁴C]flufenpyr-ethyl was administered to rats and mice as a single oral dose at a level of 500 mg/kg, and ¹⁴C-excretion was examined. Total ¹⁴C-recoveries within 7 days after administration were 93.2 to 97.5% (feces, 42.0 to 46.0%; and urine, 47.2 to 55.5%) in rats and 92.6 to 96.4% (feces, 26.7 to 32.7%; and urine, 59.9 to 69.7%) in mice. ¹⁴C-Excretion into expired air was not detected in rats (expired air of mice was not analyzed). No marked species- or sex-related differences were observed in the rate of ¹⁴C-elimination, but a relatively higher excretion into the urine of mice was observed compared to that in rats. ¹⁴C-residues in tissue 7 days after administration were relatively high for liver, hair, skin, and kidney, but total ¹⁴C-residues were low, below 0.2% of the dose. An ester cleaved metabolite (S-3153acid) was the major metabolite in feces and urine. Hydroxylation of the methyl group on the C5 of the pyridazine ring and ether cleavage were also observed. No sex-related differences were observed in ¹⁴C-elimination, ¹⁴C-distribution, and metabolite profiles, and metabolism of flufenpyr-ethyl in rats and mice was similar. In vitro metabolism of flufenpyr-ethyl was examined using stomach and intestinal contents and blood and liver S9 fractions (postmitochondrial supernatant fractions) in rats. S-3153acid was detected as a major metabolite in the presence of intestinal contents and blood and liver S9 fractions, and a small amount was also formed in the presence of stomach contents, indicating that the parent compound is rapidly metabolized by intestinal contents and blood and liver S9 fractions through ester cleavage.

中文翻译：

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氟苯吡啶在大鼠和小鼠中的代谢

在大鼠和大鼠中检查氟苯并乙基[2-氯-5- [1,6-二氢-5-甲基-6-氧代-4-（三氟甲基）哒嗪-1-基] -4-氟苯氧乙酸乙酯]的代谢。老鼠。以500 mg / kg的单次口服剂量向大鼠和小鼠服用[苯基¹⁴ C]氟苯并乙基，并检查了¹⁴ C的排泄。总¹⁴后7天施用内C-回收率为93.2至97.5％（粪便，42.0至46.0％;以及尿，47.2至55.5％）在大鼠和92.6至96.4％（粪便，26.7至32.7％;以及尿，59.9 （至69.7％）。在大鼠中未检测到¹⁴ C-排泄到呼出空气中（未分析小鼠的呼出空气）。在¹⁴的比率中未观察到明显的与物种或性别相关的差异C-消除，但观察到与大鼠相比排泄到小鼠尿中的量相对较高。¹⁴在给药后7天组织C-残基相对较高肝，毛发，皮肤，肾和，但总¹⁴ C-残基为低，低于剂量的0.2％。酯裂解的代谢产物（S-3153酸）是粪便和尿液中的主要代谢产物。还观察到哒嗪环的C 5上的甲基的羟基化和醚裂解。在¹⁴ C消除，¹⁴中未观察到性别相关的差异大鼠和小鼠中氟苯吡咯乙酯的C分布和代谢物谱以及新陈代谢相似。使用大鼠的胃和肠内容物以及血液和肝脏S9馏分（线粒体后上清液馏分）检查了氟苯丙胺的体外代谢。在肠内容物，血液和肝脏S9组分的存在下，S-3153酸被检测为主要代谢产物，在胃内容物的存在下也形成少量，表明母体化合物通过肠内容物和血液快速代谢。肝S9馏分通过酯裂解。