C-Simeconazole was diluted as required by the addition of appropriate quantities of non-radiolabeled simeconazole. The solutions for dosing were prepared by dissolving or suspending 14 C-simeconazole in a 10% aqueous solution of Tween 80. Rats were orally administered 14 C-simeconazole at a dose of 5 mg/kg b.w. (low dose) and 70 mg/kg b.w. (high dose) using a gastric tube. The high-dose level was one-tenth the acute oral LD 50 for male and female rats. Rats were fasted overnight pre-dosing and fed approximately 2 hr post-dosing. 3. Excretion Five male and five female rats were orally administered 5 and 70 mg/kg b.w. of 14 C-simeconazole. The treated animals were
The metabolic fates of milbemycin A3 and A4 (M. A3 and M. A4) were examined by oral administration of M. A3 and M. A4 labeled with 3H at 5-position to male and female rats at 5 mg/kg. The administered 3H was almost completely excreted in the urine and feces within 7 days after administration of 3H-M. A3 or 3H-M. A4. 3H levels remained relatively high in the fat and liver, while 3H in the tissues rapidly decreased to a very low level 7 days after administration.Concentrations of 3H and the parent compound in the tissues were lower in rats treated with 3H-M. A3 than in those treated with 3H-M. A4, suggesting M. A3 was metabolized faster than M. A4. 13-Hydroxylated M. A3/A4 (13-OH-A3/A4) was a major metabolite in the tissues and dihydroxylated M. A3/A4 ((OH)2-A3/A4) in the urine. In the feces, M. A3/A4, 13-OH-A3/A4, (OH)2-A3/A4 and polar metabolites were found.M. A3/A4 were predominantly metabolized to 13-OH-A3/A4 and subsequently to (OH)2-A3/A4, which were supposed to be further metabolized to polar metabolites.No essential difference was observed in the metabolic fates between M. A3 and M. A4 in the rats. The in situ intestinal absorption of M. A3 was faster than that of M. A4.
Bioaccumulation potency and biodegradation of pyrazolate [4-(2, 4-dichlorobenzoyl and p-toluenesulfonic acid, were examined in guppies (Poecilia reticulata) and short-necked clams (Tapes philippinarum) using 14C-preparations. Uptake factors (UF: concentration of total 14C in aquatic organisms/concentration of a parent compound in test water) of pyrazolate in guppies at 0. 33 and 32. 3 ppb treatment levels were about 590 and 290, respectively, whereas those of DTP and p-toluenesulfonic acid were 15 at 0. 37 ppb and less than 1 at 2. 91 ppb, respectively. OF values in clams were 52 for pyrazolate at 2. 06 ppb and 6. 2 for DTP at 48. 4 ppb. On transference to clean water, 14C levels in the exposed aquatic organisms rapidly decreased, indicating that these chemicals and their metabolites did not bioaccumulate in the tested organisms. Pyrazolate was first metabolized through the hydrolysis of the ester linkage to give DTP and p-toluenesulfonic acid, followed by the oxidation at the 1-and 3-methyl groups of DTP and the cleavage of the benzoyl linkage into more polar compounds.
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