The disposition of N-(4,6-dimethyl-2-pyrimidinyl)benzene[U-14C]sulfonamide in the rat.
Rats given a single oral dose of N-(4,6-dimethyl-2-pyrimidinyl)benzene[U-14C]sulfonamide (14C-DAS) excreted 64.2% of the 14C in the urine and 22.4% in the feces within 96 hr. Compounds accounting for 86% of the 14C in the 0-24-hr urine were isolated by a variety of chromatographic techniques and identified by IR, NMR, and MS analysis. Approximately 4% of the 14C in the urine was the parent compound. The structures of 14C-metabolites in the urine indicated that 14C-DAS was metabolized by at least three pathways which included: 1) hydroxylation and glucuronic acid conjugation at the 4-position of the benzene ring; 2) hydroxylation, and sulfate ester and glucuronic acid conjugation at the 5-position on the heterocyclic ring; and 3) hydroxylation and glucuronic acid conjugation of one methyl group on the heterocyclic ring.
D000284:Administration, Oral; D000818:Animals; D002250:Carbon Radioisotopes; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains / Q000378:metabolism*; D012016:Reference Values; D013418:Sulfamethazine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D000096926:Benzenesulfonamides
D002250:Carbon Radioisotopes; D013418:Sulfamethazine; C028503:desaminosulfamethazine; D000096926:Benzenesulfonamides