Abstract
The metabolism of 14C-labeled methazole, 2-(3,4-dichlorophenyl)-4-methyl-1,2,4-oxidiazolidine-3,5-dione, in rats was investigated, and the nature and levels or residues in the urine, feces, and tissues were determined. Elimination in the urine and feces was 58% of an administered single oral dose by 48 hr after treatment. The major metabolite in the urine was N-(2-hydroxy-4,5-dichlorophenyl)urea, accounting for 46% of the total radiocarbon in the urine. Another ring-hydroxylated material, N-(2-hydroxy-3,4-dichlorophenyl)urea, was 14% of the total, and both compounds were present almost entirely as glucuronides. 3,4-Dichlorophenylurea was the major metabolite in the feces and existed almost completely in the free form. In tissues sampled 96 hr after treatment, the highest methazole-14C equivalents were in the kidney, liver, and fat, with concentrations of 0.8, 0.1, and 0.07% of the dose per g, respectively. Rats dosed orally with methazole, 100 mg/kg/day for 17 days, or given a single oral dose of 3-(3,4-dichlorophenyl)-1-methylurea gave the same series of metabolites in the urine as rats treated with a single oral dose of methazole.
Footnotes
- Received October 26, 1973.
- Copyright © 1974 by The American Society for Pharmacology and Experimental Therapeutics
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