Metabolism of 1,3-di-(4-[N-(4,6-dimethyl-2-pyrimidinyl)sulphamoyl] phenyl)triazene (DDPSPT) in the rat.
1. Six hours after rats were orally dosed with 1,3-di-(4-[N-(4,6-dimethyl-2-pyrimidinyl)sulphamoyl][U-14C]phenyl) triazene (14C-DDPSPT), approx. 81% of the 14C remained in the gastrointestinal tract (gut) and less than 3% was excreted in the urine. 2. Six hours after dosing, more than half of the 14C in the gut was present as DDPSPT. 14C-Labelled metabolites in the gut included 4-amino-N-(4,6-dimethyl-2-pyrimidinyl)-benzenesulphonamide (Sulmet), N4-glucosyl-N-(4,6-dimethyl-2-pyrimidinyl)benzenesulphonamide (N4-gluc-Sulmet), 4-acetamido-N-(4,6-dimethyl-2-pyrimidinyl)benzenesulphonamide (N4-acetyl-Sulmet), and [N-4,6-dimethyl-2-pyrimidinyl) benzenesulphonamide] (desamino-Sulmet). 3. 14C-Labelled compounds in the blood, liver and skeletal muscle included DDPSPT, Sulmet, N4-gluc-Sulmet, N4-acetyl-Sulmet and desamino-Sulmet. 4. There was little or no reaction of DDPSPT with cysteine, bovine serum albumin, AMP, GMP, or calf thymus deoxyribonucleic acid in vitro (pH 3, 5, 7 or 8).
Paulson
G D
GD
Biosciences Research Laboratory, US Department of Agriculture, Fargo, ND 58105.
Feil
V J
VJ
McDonald
J J
JJ
D000284:Administration, Oral; D000818:Animals; D004064:Digestive System / Q000378:metabolism; D066298:In Vitro Techniques; D008099:Liver / Q000378:metabolism; D015394:Molecular Structure; D009132:Muscles / Q000378:metabolism; D051381:Rats; D014018:Tissue Distribution; D014226:Triazenes / Q000097:blood / Q000378:metabolism* / Q000652:urine; D015262:Xenobiotics / Q000378:metabolism
D014226:Triazenes; D015262:Xenobiotics; C053071:1,3-di-(4(N-(4,6-dimethyl-2-pyrimidinyl))sulfamoylphenyl)triazene