フェンピロキシメートのラットにおける代謝

DOI NDLデジタルコレクション 日本農学文献記事索引 Web Site Web Site 被引用文献2件

書誌事項

タイトル別名
  • Metabolism of Fenpyroximate in Rats
  • フェンピロキシメートのラットにおける代謝〔英文〕
  • フェンピロキシメート ノ ラット ニ オケル タイシャ エイブン

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Metabolism of fenpyroximate, tert-butyl (E)-α-(1, 3-dimethyl-5-phenoxypyrazol-4-ylmethyleneaminooxy)-p-toluate in rats was studied. After a single oral administration of [pyrazole-3-14C], [phenyl-14C(U)] or [benzene ring-14C(U)]fenpyroximate, the radiocarbon level in the blood increased to reach the maximum level of 0.18, 0.16 or 0.18μg fenpyroximate eq./ml at 12, 12 or 9hr, respectively, and then decreased at a half-life of 11.3, 10.6 or 9hr, respectively. The radiocarbons in 14C-fenpyroximate were rapidly and almost completely excreted into the urine and feces within 72hr. The excretion rates of radiocarbon into the urine and feces were 26.2 and 65.5% for [pyrazole-3-14C], 26.1 and 63.9% for [phenyl-14C(U)] and 6.4 and 86.9% for [benzene ring-14C(U)]fenpyroximate, respectively. Urinary metabolites identified were 1, 3-dimethyl-5-phenoxypyrazole-4-carboxylic acid, 4-cyano-1-methyl-5-phenoxypyrazole-3-carboxylic acid and terephthalic acid. Major metabolites in the feces were (E)-4-[(1, 3-dimethyl-5-phenoxypyrazol-4-yl)methyleneaminooxymethyl]benzoic acid, (E)-2-[4-[(1, 3-dimethyl-5-phenoxypyrazol-4-yl)methyleneaminooxymethyl]benzoyloxy]-2-methylpropionic acid, (E)-2-[4-[[1, 3-dimethyl-5-(4-hydroxy)phenoxypyrazol-4-yl]methyleneaminooxymethyl]benzoyloxy]-2-methylpropionic acid, (E)-2-[4-[(1-hydroxymethyl-3-methyl-5-phenoxypyrazol-4-yl) methyleneaminooxymethyl] benzoyloxy]-2-methylpropionic acid and 4-hydroxymethylbenzoic acid. Fenpyroximate seemed to be metabolized via oxidation of the t-butyl group and methyl group at 3-position in the pyrazole ring, p-hydroxylation in the phenoxy moiety, N-demethylation, hydrolysis of the t-butyl ester, cleavage of the oxime ether bond and/or E/Z isomerization.

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