Identification of benidipine hydrochloride metabolites in rats and dogs.
A study of the metabolism of [14C]-(+/-)-(R*)-2,6-dimethyl-4-(m-nitrophenyl)- 1,4-dihydropyridine-3, 5- dicarboxylic acid (R*)-1-benzyl-3-piperdidinyl ester, methyl ester hydrochloride (14C-benidipine hydrochloride, 14C-KW-3049) revealed as major metabolic pathways oxidative N-dealkylation, hydrolysis of the ester moiety, dehydrogenation of the 1,4-dihydropyridine ring, hydroxylation of the methyl group and decarboxylation in rat and dog. Rat and dog showed similar metabolic pathways, but some quantitative differences were found between rat and dog.
Kobayashi
H
H
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Okumura
S
S
Kosaka
Y
Y
Kobayashi
S
S
Inoue
A
A
Oka
T
T
Nakamizo
N
N
D000818:Animals; D002121:Calcium Channel Blockers / Q000493:pharmacokinetics*; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004285:Dogs; D006868:Hydrolysis; D008297:Male; D015394:Molecular Structure; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D010084:Oxidation-Reduction; D051381:Rats; D011919:Rats, Inbred Strains; D012588:Scintillation Counting
D002121:Calcium Channel Blockers; C050883:benidipine hydrochloride; D009543:Nifedipine