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奥卡西平、10,11-二氢-10-羟基卡马西平和卡马西平对大鼠肝脏微粒体酶的诱导作用。

Induction of microsomal enzymes in rat liver by oxcarbazepine, 10,11-dihydro-10-hydroxy-carbamazepine and carbamazepine.

作者信息

Wagner J, Schmid K

机构信息

Research and Development Department, CIBA-GEIGY Limited, Basle, Switzerland.

出版信息

Xenobiotica. 1987 Aug;17(8):951-6. doi: 10.3109/00498258709044193.

Abstract
  1. The effects of the new anti-epileptic drug, oxcarbazepine, its major metabolite in man, 10,11-dihydro-10-hydroxy-carbamazepine, and carbamazepine, on hepatic microsomal enzyme activities have been studied in rats after repeated administration of equimolar doses. 2. All three compounds caused a qualitatively similar induction of the mono-oxygenase system, the greatest increase being observed in the activity of 4-nitroanisole O-demethylase. Oxcarbazepine is as potent as carbamazepine, while 10,11-dihydro-10-hydroxy-carbamazepine is a weak inducer. 3. The observation that oxcarbazepine is a potent inducer in rats but not in man is explained by the species differences in its metabolism.
摘要
  1. 在大鼠中重复给予等摩尔剂量后,研究了新型抗癫痫药物奥卡西平、其在人体内的主要代谢产物10,11 - 二氢 - 10 - 羟基卡马西平和卡马西平对肝微粒体酶活性的影响。2. 所有这三种化合物在质量上对单加氧酶系统有相似的诱导作用,其中4 - 硝基苯甲醚O - 脱甲基酶的活性增加最为显著。奥卡西平与卡马西平的诱导作用相当,而10,11 - 二氢 - 10 - 羟基卡马西平是一种弱诱导剂。3. 奥卡西平在大鼠中是一种强效诱导剂而在人体中不是,这一观察结果可通过其代谢的种属差异来解释。

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