Sugiyama M, Ando T, Okuyama Y, Sugimoto T, Choukai S
Arzneimittelforschung. 1986 Aug;36(8):1229-36.
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.
对马来酸2,4-二氨基-6-(2,5-二氯苯基)-s-三嗪（MN-1695）在大鼠、豚鼠、狗和猴子体内的代谢情况进行了研究。在大鼠中，以3.1mg/kg的剂量口服给药后，MN-1695被代谢为8种以上的代谢产物。这些代谢产物从尿液中分离出来，并通过与参考化合物共色谱、质谱分析及其他仪器分析进行表征。在大鼠和豚鼠尿液中的主要代谢产物是MN-1695 X m-OH，它以结合物的形式排泄；在狗尿液中的主要代谢产物是MN-1695 X N-氧化物。在猴子中，尽管MN-1695没有广泛代谢，但尿液中MN-1695 X m-OH（游离和结合形式）和MN-1695 X N-氧化物占主导。在大鼠中，排泄到胆汁中的放射性物质超过90%由极性代谢产物组成。在各种动物物种中发现的MN-1695的主要代谢途径包括芳香环3位和4位的羟基化以及s-三嗪环3位的N-氧化。此外，在所有检测的物种中均检测到含硫代谢产物。
