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  • Title: Metabolism of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate in rats, guinea pigs, dogs and monkeys.
    Author: Sugiyama M, Ando T, Okuyama Y, Sugimoto T, Choukai S.
    Journal: Arzneimittelforschung; 1986 Aug; 36(8):1229-36. PubMed ID: 3778560.
    Abstract:
    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.
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