Metabolism of Diethofencarb in Rats

SHIBA Kunio, KANEKO Hideo, KAKUTA Noriko, YOSHINO Hiromi, IBA Kazuhiko, NAKATSUKA Iwao, YOSHITAKE Akira, YAMADA Hirohiko

doi:10.1584/jpestics.15.395

Metabolic fates of diethofencarb (isopropyl 3, 4-diethoxycarbanilate) were examined in male and female rats. After single oral doses of [phenyl-¹⁴C]diethofencarb at 10mg/kg or 300mg/kg, most of the dosed ¹⁴C was recovered in the urine and feces within 48hr after dosing. The total ¹⁴C-recovery ranged from 99 to 100% of the dose during 7 days after administration with the ¹⁴C urinary excretion being 80 to 88% of the dose. ¹⁴C-Levels in the blood and various tissues reached maxima within 0.5hr after administration and decreased rapidly thereafter with biological half-lives of 12 to 35hr. ¹⁴C-Tissue residues were substantially low. The residue levels were the highest in the liver (0.05-0.07 and 1.70-2.22ppm for the low and high doses, respectively). Total tissue residues of ¹⁴C on the 7th day after dosing were less than 0.2% of the dose. Major metabolic reactions of diethofencarb were (1) de-ethylation of the 4-ethoxy group, (2) cleavage of the carbamate linkage, (3) acetylation of the amino group and (4) conjugation of the resultant phenols with sulfuric acid or glucuronic acid. A major metabolite in the urine was the sulfate of isopropyl 3-ethoxy-4-hydroxycarbanilate (30.0-48.7% of the dose). No marked sex-related difference was observed in the metabolism of diethofencarb.

Metabolism of Diethofencarb in Rats

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