Identification of efonidipine hydrochloride metabolites in rats.
The metabolism of efonidipine hydrochloride (CAS 111011-76-8, NZ-105), a new dihydropyridine calcium antagonist, was studied after oral or intraperitoneal dosing in rats. Six metabolites were isolated from urine and bile and their structures were confirmed by spectral and chromatographic comparison with the authentic compounds. The main metabolic pathway of efonidipine hydrochloride involved N-debenzylation, N-dephenylation, oxidative deamination, ester hydrolysis and oxidation of the 1,4-dihydropyridine ring to the corresponding pyridine.
Nakabeppu
H
H
Shiraoka Research Station of Biological Science, Nissan Chemical Industries, Ltd., Saitama, Japan.
Nakajima
A
A
Kamikawaji
Y
Y
Shinozaki
Y
Y
D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism; D001711:Biotransformation; D002121:Calcium Channel Blockers / Q000737:chemistry / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004095:Dihydropyridines / Q000737:chemistry / Q000493:pharmacokinetics*; D007274:Injections, Intraperitoneal; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D009596:Nitrophenols; D009943:Organophosphorus Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D009596:Nitrophenols; D009943:Organophosphorus Compounds; C066425:efonidipine