(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

磯部 直彦, 井藤 重美, 吉武 彬, 松尾 昌年, 宮本 純之

doi:10.1584/jpestics.12.421

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.

(<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

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