Metabolism of (<i>R</i>)- and (<i>S</i>)-Isomers of (<i>E</i>)-1-(2, 4-Dichlorophenyl)-4, 4-dimethyl-2-(1, 2, 4-triazol-1-yl)-1-penten-3-ol (S-3308L) in Rats

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  • ISOBE Naohiko
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • ITO Shigemi
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • YOSHITAKE Akira
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • MATSUO Masatoshi
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.
  • MIYAMOTO Junshi
    Laboratory of Biochemistry and Toxicology, Takarazuka Research Center, Sumitomo Chemical Co., Ltd.

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Other Title
  • (<i>E</i>)-1-(2,4-Dichlorophenyl)-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-1-penten-3-ol (S-3308L) の (<i>R</i>) および (<i>S</i>) 異性体のラットにおける代謝
  • (E)-1-(2,4-Dichlorophenyl)-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-1-penten-3-ol(S-3308L)の(R)および(S)異性体のラットにおける代謝〔英文〕
  • E 1 2 4 Dichlorophenyl 4 4 dimethyl 2 1

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Abstract

Metabolic fates of (R)- and (S)-(E)-1-(2, 4-dichlorophenyl)-4, 4-dimethyl-2-(1, 2, 4-triazol-1-yl)-1-penten-3-ols, designated as (R)-E and (S)-E, labeled with 14C at the benzene or triazole ring were examined after oral administration to male and female rats at dose levels of 5 and 125mg/kg. There was no remarkable difference between enantiomers in the 14C-excretion into the feces and urine, 14C tissue residues on the 7th day after administration, and amounts of metabolites in the feces and urine. However, biotransformation and excretion rates were faster with (S)-E in vivo than with (R)-E, and also biotransforming rates by the hepatic microsomal fraction of rats were faster with (S)-E than with (R)-E. Males excreted more 14C into the feces than females. A major metabolite, a carboxylic acid derivative of the 4-methyl group of (R)-E or (S)-E, was mainly excreted into feces in both sexes, but its excretion into the urine was in larger amounts in females than in males. 1-(2, 4-Dichlorophenyl)-2-(1, 2, 4-triazol-1-yl)propan-1, 3-diols were found in small amounts in the feces, and 1, 2, 4-triazole in the feces, urine and skin with hair. A successive 14-day pretreatment with unlabeled S-3308L, a mixture of (R)-E and (S)-E (ca. 8/2), did not affect the metabolism of (R)-E and (S)-E in rats.

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