• 金子 秀雄
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 泉 敏彦
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 松尾 昌年
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 宮本 純之
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.

書誌事項

タイトル別名
  • Metabolism of Fenvalerate in Dogs
  • Fenvalerateのイヌにおける代謝〔英文〕
  • Fenvalerate ノ イヌ ニ オケル タイシャ エイブン

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抄録

On single oral administration of 14C-chlorophenyl-ring- and 14C-phenyl-ring-fenvalerate [(RS)-α-cyano-3-phenoxybenzyl-(RS)-2-(4-chlorophenyl)-3-methylbutylate] preparations to male dogs at 1.7mg/kg, the radiocarbon from the acid and alcohol moieties was eliminated from the animal bodies within 3 days to the extent of 87.1 and 79.1%, respectively. The biological half-life (T1/2) for fenvalerate in the blood was about 2.0hr, and the level of fenvalerate decreased below the detection limit (0.01ppm) in 48hr after dose. Fenvalerate was metabolized mainly by oxidation at the 4′-phenoxy position of the alcohol moiety and at the C-2 and C-3 positions of the acid moiety, cleavage of the ester linkage and conjugation of the resultant carboxylic acids, phenols and alcohols with glucuronic acid, sulfate and/or amino acid. The following remarkable species differences were found between dogs and rodents such as rats and mice: 1) hydroxylation at the 2′-position of the alcohol moiety occurred in rats and mice, but not in dogs. 2) 3-phenoxybenzyl alcohol and 3-(4′-hydroxyphenoxy) benzyl alcohol were obtained from dogs to a considerable extent, but not detected in rats and mice. 3) 3-phenoxybenzoylglycine was the predominant conjugate of the alcohol moiety in dogs, but a minor one in rats and mice. 4) glucuronides of acid moiety and its hydroxy derivatives were obtained from dogs to a larger extent than rats and mice.

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