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氯化镨对大鼠肝脏微粒体酶的影响。

Effect of praseodymium chloride on liver microsomal enzymes of rats.

作者信息

Oga S, Galvão J F, Yasaka W J, Araujo Filho A P

出版信息

Life Sci. 1986 Jun 2;38(22):2029-36. doi: 10.1016/0024-3205(86)90151-7.

Abstract

A single i.v. dose (5 mg/kg) of a light lanthanon, praseodymium, prolonged the duration of hexobarbital-induced sleep and zoxazolamine-induced paralysis, as well as it modified pharmacokinetic parameters of hexobarbital and zoxazolamine, in rats. Half-lives (t1/2) and area under the curve (AUC) were increased, while elimination coefficient (beta) and clearance (Cl) were decreased. However, in daily doses of 1 mg/kg i.p. for 15 days, praseodymium did not alter pharmacological effects and pharmacokinetic parameters. The in vitro hydroxylation of hexobarbital and zoxazolamine by liver microsomes was inhibited when the animals were treated previously with a single i.v. dose (5 mg/kg) of praseodymium chloride. In these animals, the amount of cytochromes P-450 and b5 were reduced significantly, whereas that of NADPH-cytochrome c reductase remained unchanged. The pretreatment of animals with phenobarbital normalized the microsomal enzyme impairment caused by praseodymium.

摘要

给大鼠静脉注射单剂量(5毫克/千克)的轻镧系元素镨,可延长己巴比妥诱导的睡眠时间和唑沙宗诱导的麻痹时间,同时改变己巴比妥和唑沙宗的药代动力学参数。半衰期(t1/2)和曲线下面积(AUC)增加,而消除系数(β)和清除率(Cl)降低。然而,以每日1毫克/千克的腹腔注射剂量连续给药15天,镨并未改变其药理作用和药代动力学参数。当动物预先静脉注射单剂量(5毫克/千克)的氯化镨时,肝脏微粒体对己巴比妥和唑沙宗的体外羟化作用受到抑制。在这些动物中,细胞色素P-450和b5的含量显著降低,而NADPH-细胞色素c还原酶的含量保持不变。用苯巴比妥对动物进行预处理可使由镨引起的微粒体酶损伤恢复正常。

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