N-acetyl derivative as the major active metabolite of 2-amino-6-methyldipyrido[1,2-a:3',2'-d]imidazole in rat bile.
2-Amino-6-methyldipyrido[1,2-a:3',2'-d]imidazole (Glu-P-1) is a mutagen and carcinogen isolated from a glutamic acid pyrolysate. When this 14C-labeled compound was administered to male F344 rats at a dose of 0.3 mCi (20.8 mg)/kg b.w., 70% of the radioactivity was excreted into the bile in 24 h. On HPLC analysis of this bile, several metabolites of Glu-P-1 were found with unmetabolized Glu-P-1. One of the mutagenic metabolites was identified as N-acetyl-Glu-P-1. This metabolite had a specific mutagenic activity of about one quarter of that of Glu-P-1 and its amount in the bile corresponded to a few percent of the dose of Glu-P-1 administered.
D000818:Animals; D001646:Bile / Q000032:analysis / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D007093:Imidazoles / Q000032:analysis / Q000302:isolation & purification / Q000378:metabolism* / Q000494:pharmacology*; D008297:Male; D013058:Mass Spectrometry; D009152:Mutagenicity Tests; D009153:Mutagens / Q000494:pharmacology*; D051381:Rats; D011916:Rats, Inbred F344; D012486:Salmonella typhimurium / Q000187:drug effects
D007093:Imidazoles; D009153:Mutagens; C049870:N-acetyl-2-amino-6-methyldipyrido(1,2-a-3',2'-d)imidazole; C023785:2-amino-6-methyldipyrido(1,2-a-3',2'-d)imidazole