大鼠和犬体内盐酸贝尼地平代谢物的鉴定。
Identification of benidipine hydrochloride metabolites in rats and dogs.
作者信息
Kobayashi H, Okumura S, Kosaka Y, Kobayashi S, Inoue A, Oka T, Nakamizo N
机构信息
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
出版信息
Arzneimittelforschung. 1988 Nov;38(11A):1753-6.
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.
对[14C]-(±)-(R*)-2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-3,5-二羧酸(R*)-1-苄基-3-哌啶酯甲酯盐酸盐（14C-贝尼地平盐酸盐，14C-KW-3049）的代谢研究表明，在大鼠和犬体内，主要代谢途径包括氧化N-脱烷基化、酯部分的水解、1,4-二氢吡啶环的脱氢、甲基的羟基化和脱羧。大鼠和犬表现出相似的代谢途径，但在大鼠和犬之间发现了一些定量差异。
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