RT Journal Article
SR Electronic
T1 N-hydroxymethyl metabolites of 450191-S, a 1H-1,2,4,-triazolyl benzophenone derivative, in dog plasma.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 426
OP 428
VO 15
IS 3
A1 M Koike
A1 R Norikura
A1 S Futaguchi
A1 T Yamaguchi
A1 K Sugeno
A1 K Iwatani
A1 Y Ikenishi
A1 Y Nakagawa
YR 1987
UL http://dmd.aspetjournals.org/content/15/3/426.abstract
AB In a metabolic experiment of 5-[(2-aminoacetamido)methyl]-1-[4-chloro-2-(o-chlorobenzoyl)phenyl ]-N, N-dimethyl-1H-1,2,4,-triazole-3-carboxamide hydrochloride dihydrate (450191-S) in dogs, two new metabolites 8-chloro-6-(o-chlorophenyl)-N-hydroxymethyl-4H-1,2,4-triazolo [1,5-a] [1,4]benzodiazepine-2-carboxamide (M-A) and 8-chloro-6-(o-chlorophenyl)-N-hydroxymethyl-N-methyl-4H-1,2,4-triazolo [1,5-a] [1,4]benzodiazepine-2-carboxamide (M-D) in plasma were found in addition to 8-chloro-6-(o-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo[1,5-a] [1,4] benzodiazepine-2-carboxamide (M-1), 8-chloro-6-(o-chlorophenyl)-N-methyl-4H-1,2,4-triazolo[1,5-a] [1,4] benzodiazepine-2-carboxamide (M-2), 8-chloro-6-(o-chlorophenyl)-4H-1,2,4-triazolo-[1,5-a] [1,4] benzodiazepine-2-carboxamide (M-3), and 8-chloro-6-(o-chlorophenyl)-4H-1,2,4-triazolo[1,5-a] [1,4] benzodiazepine-2-carboxylic acid (M-4). The structures of N-hydroxymethyl metabolites were elucidated mainly by mass spectrometry. The structures were confirmed by synthesizing the authentic compounds and comparing the mass spectra.