Croconazole metabolism in rats.
Croconazole metabolism in rats.
复制标题
克罗康唑在大鼠中的代谢。
DOI：
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发表时间：
1990
期刊：
影响因子：
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通讯作者：
K. Mizojiri
中科院分区：
文献类型：
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作者：
M. Nakano;M. Takeuchi;S. Kawahara;K. Mizojiri
1.大鼠皮下给予1-（2-（3-氯苄氧基）苯基）乙烯基）-1H-咪唑（克罗康唑）后，通过比较其质量和n.m.r.鉴别出4种代谢产物。光谱，g.l.c.，和T.L.C.与合成化合物和酶水解的那些相比。这些化合物为邻羟基苯乙酮硫酸盐（M1 S）、1-（1-（2-羟基苯甲酰甲基）乙烯基）-1H-咪唑硫酸盐（M12 S）、2-（3-氯苄氧基）苯甲酰甲基醇（M2）和2-（3-氯苄氧基）苯甲酸（M9-1）。2.在10 mg/kg剂量下，雄性大鼠血浆中原型药物的消除速率快于雌性大鼠。3. 24 h尿液中M12 S的排泄百分比为男性17%和女性7.5%，M1 S为男性6.6%和女性6.5%。24 h胆汁中M2的排泄百分比为14%（雄性）和22%（雌性），M9-1的排泄百分比为3.7%（雄性）和1.6%（雌性）。
1. Following subcutaneous administration of 1-(2-(3-chlorobenzyloxy)phenyl)vinyl)-1H-imidazole (croconazole) to rats, four metabolites were identified by comparison of their mass and n.m.r. spectra, g.l.c., and t.l.c. with those of synthetic compounds and enzyme hydrolysis. These compounds are o-hydroxyacetophenone sulphate (M1S), 1-(1-(2-hydroxyphenacyl)vinyl)-1H-imidazole sulphate (M12S), 2-(3-chlorobenzyloxy)phenacyl alcohol (M2), and 2-(3-chlorobenzyloxy)benzoic acid (M9-1). 2. At 10 mg/kg dosing of croconazole the elimination rate of the unchanged drug from plasma was faster in male than in female rats. 3. The percentage of excretion of M12S in 24 h urine was 17% for males and 7.5% for females, and that of M1S was 6.6% for males and 6.5% for females. The percentage of excretion of M2 in 24 h bile was 14% for males and 22% for females, and that of M9-1 was 3.7% for males and 1.6% for females.
影响因子：
21.1
作者：
C. Klaassen;J. Watkins
通讯作者：
C. Klaassen;J. Watkins