title: Metabolism of propyrisulfuron: 14C excretion, 14C concentration in plasma and tissues, and amount of metabolites in rats.
abstract: 1. Metabolism of a novel sulfonylurea herbicide, propyrisulfuron [1-(2-chloro-6-propylimidazo[1,2-b]pyridazin-3-ylsulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea] labeled at the C-1 position of the propyl group and C-5 position of the pyrimidine ring with (14)C was investigated after a single oral administration in male and female rats. 2. Administered (14)C was excreted into the urine (5.7-29.8%) and feces (64.6-97.4%), respectively. (14)C concentration in plasma reached a maximum level at 4 to 12 h post-administration and then decreased rapidly with a biological half-life of approximately 23 to 32 h. Total (14)C residues in the whole body were <0.1-1.4%, suggesting that the residues were not accumulated in the tissues. 3. The amount of metabolites in urine, feces, and bile were quantified using high-performance liquid chromatography (HPLC). There were no differences in metabolites found between male and female rats. 4. The absorption for the low dose (5 mg/kg) and the high dose (1000 mg/kg) was estimated to be approximately 90% and 20%, respectively, suggesting a saturable absorption. 5. The plasma protein binding in male and female rats was ≥ 98.8%, suggesting that propyrisulfuron had a strong affinity to plasma proteins.
authors.affiliation: Laboratory of Environmental Health Science, Sumitomo Chemical Co., Ltd. , Konohana-Ku, Osaka , Japan.
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Takaku
authors.forename: Kazuki
authors.initials: K
authors.lastname: Mikata
authors.forename: Hirohisa
authors.initials: H
authors.lastname: Nagahori
authors.forename: Yoshihisa
authors.initials: Y
authors.lastname: Sogame
mesh_terms: D000818:Animals; D001646:Bile / Q000737:chemistry; D001798:Blood Proteins / Q000378:metabolism; D001944:Breath Tests; D002250:Carbon Radioisotopes / Q000097:blood / Q000652:urine; D005243:Feces / Q000737:chemistry; D005260:Female; D006540:Herbicides / Q000378:metabolism*; D008297:Male; D051381:Rats; D014508:Urea / Q000031:analogs & derivatives* / Q000378:metabolism
chemical_list: D001798:Blood Proteins; D002250:Carbon Radioisotopes; D006540:Herbicides; D014508:Urea; C000598104:propyrisulfuron
keywords: Herbicide; metabolism; rat