Characterization of urinary metabolites of a new benzofuroquinoline derivative, 3,9-bis(N,N-dimethylcarbamoyloxy)-5 H-benzofuro[3,2-c]-quinoline-6-one (KCA-098), in dogs.
The metabolism of 3,9-bis(N,N-dimethylcarbamoyloxy)-5 H-benzofuro[3,2-c]-quinoline-6-one (KCA-098), a new inhibitor of bone resorption and stimulator of bone formation, was examined after oral administration to dogs. Nine metabolites and the unchanged KCA-098 were isolated by extraction and HPLC from dog urine. The structures of these metabolites were characterized by LC/MS or LC/MS/MS, and/or were confirmed by comparison with corresponding authentic standards. The presumed main metabolic pathways were hydrolysis, hydroxylation, and N-demethylation of the N,N-dimethyl-carbamate ester group.
Yamada
T
T
Central Research Laboratories, Kissei Pharmaceutical Co. Ltd., Nagano-Prefecture, Japan.
Yamamoto
A
A
Fujioka
M
M
Miyagi
M
M
Saito
N
N
Imai
I
I
Otagiri
M
M
D000818:Animals; D001711:Biotransformation; D002851:Chromatography, High Pressure Liquid; D003375:Coumestrol / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000652:urine; D003640:Dealkylation; D004285:Dogs; D006868:Hydrolysis; D006900:Hydroxylation; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry
C088191:KCA 098; D003375:Coumestrol