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体外镉对不同年龄大鼠中苄非他明 -N-去甲基化和乙氧试卤灵 -O-去乙基化的影响。

Effect of cadmium in vitro on benzphetamine-N-demethylation and ethoxyresorufin-O-deethylation in rats of different age.

作者信息

Kadiiska M, Stoytchev T, Jahn F, Klinger W

出版信息

Acta Physiol Pharmacol Bulg. 1983;9(4):21-30.

PMID:6677060
Abstract

The in vitro influence of CdSO4 on the liver microsomal benzphetamine-N-demethylation and ethoxyresorufin-O-deethylation activities in male Wistar rats/age 10, 30, 60 and 240 days/as well as the type of inhibition were studied after phenobarbital or beta-naphthoflavone pretreatment. Both reactions were inhibited by CdSO4 in dependence on concentration in all age groups. After phenobarbital pretreatment the inhibition of N-demethylation was slightly pronounced in 10-day old rats. In 10 and 30-days old rats the type of inhibition was competitive while in 60 and 240-days old rats a non-competitive type of inhibition was observed. O-deethylation of ethoxyresorufin was inhibited also in 10-day old rats, the inhibition type was non-competitive in all age groups. After beta-naphthoflavone pretreatment N-demethylation was inhibited competitively in all age groups. The inhibition of O-deethylation was more pronounced in 30-day old rats, in other age groups the inhibition was weak but concentration dependent. The type of inhibition was noncompetitive for all age groups studied.

摘要

研究了硫酸镉(CdSO4)对10日龄、30日龄、60日龄和240日龄雄性Wistar大鼠肝脏微粒体中苄非他明-N-脱甲基酶和乙氧试卤灵-O-脱乙基酶活性的体外影响,以及在苯巴比妥或β-萘黄酮预处理后抑制的类型。在所有年龄组中,硫酸镉均以浓度依赖的方式抑制这两种反应。苯巴比妥预处理后,10日龄大鼠中N-脱甲基酶的抑制作用略有增强。在10日龄和30日龄大鼠中,抑制类型为竞争性,而在60日龄和240日龄大鼠中观察到非竞争性抑制类型。10日龄大鼠中乙氧试卤灵的O-脱乙基作用也受到抑制,所有年龄组的抑制类型均为非竞争性。β-萘黄酮预处理后,所有年龄组中N-脱甲基酶均受到竞争性抑制。O-脱乙基作用的抑制在30日龄大鼠中更为明显,在其他年龄组中抑制作用较弱但呈浓度依赖性。在所研究的所有年龄组中,抑制类型均为非竞争性。

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