ピレスロイド系殺虫剤S-4068SFのラットにおける代謝

  • 斯波 久二雄
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 角田 紀子
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 金子 秀雄
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 中塚 巌
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 吉武 彬
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • 山田 宏彦
    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 the Pyrethroid Insecticide S-4068SF in Rats
  • ピレスロイド系殺虫剤S-4068 SFのラットにおける代謝〔英文〕
  • ピレスロイドケイ サッチュウザイ S-4068 SF ノ ラット ニ オケル

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抄録

The metabolic fate of 5-4068SF [Etoc®, (S)-2-methyl-4-oxo-3-(2-propynyl)cyclopent-2-enyl (1R)-trans, cis-chrysanthemate], a novel pyrethroid, was examined by administering [alcohol-14C](4S, 1R)-trans- and [alcohol-14C] (4S, 1R)-cis-S-4068 orally or subcutaneously to male and female rats at 2mg/kg. The administered radiocarbon was almost completely eliminated in urine and feces within 7 days after treatment. 14C levels in blood and other tissues reached maxima within 3hr after oral administration and thereafter decreased rapidly. Biological half-lives of 14C tissue levels for 3-12 and 12-48hr after oral administration were 3-5hr and 7-35hr, respectively. 14C tissue residues were generally very low on the 7th day after administration. Twenty metabolites found in excreta were identified. Proposed metabolic pathways of S-4068SF involved, 1) oxidation at methyl of the isobutenyl group in the acid moiety and at the C-1 or the C-2 position of the propynyl group in the alcohol moiety, 2) cleavage of ester linkage, and 3) conjugation of resultant hydroxy derivatives with glucuronic acid and sulfuric acid. There was no marked difference in the metabolic fate of (4S, 1R)-trans- or (4S, 1R)-cis-S-4068 between sexes and administration routes.

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