Metabolism of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate in rats, guinea pigs, dogs and monkeys.
The metabolism of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) was studied in rats, guinea pigs, dogs and monkeys. MN-1695 was metabolized to more than 8 metabolites after oral administration in a dose of 3.1 mg/kg in rats. These metabolites were isolated from the urine and characterized by cochromatography with reference compounds, mass spectrometry and other instrumental analysis. The main metabolite in the urine was MN-1695 X m-OH, which was excreted as a conjugate, in rats and guinea pigs, and MN-1695 X N-oxide in dogs. In monkeys, MN-1695 X m-OH (free and conjugate) and MN-1695 X N-oxide predominated in the urine, although MN-1695 was not extensively metabolized. In rats, over 90% of the radioactivity excreted into the bile consisted of the polar metabolites. The major metabolic pathways of MN-1695 found in various animal species involved the hydroxylation at the positions of 3 and 4 of the aromatic ring and the N-oxidation at the position of 3 of the s-triazine ring. In addition, the sulfur-containing metabolites were detected in all species examined.
D000818:Animals; D000897:Anti-Ulcer Agents / Q000378:metabolism*; D001646:Bile / Q000032:analysis; D001711:Biotransformation; D002855:Chromatography, Thin Layer; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D006868:Hydrolysis; D008253:Macaca mulatta; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D014227:Triazines / Q000378:metabolism*
D000897:Anti-Ulcer Agents; D014227:Triazines; C041836:irsogladine