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二正丙基乙酸——小鼠抗惊厥活性概况

Di-n-propylacetic acid--profile of anticonvulsant activity in mice.

作者信息

Frey H H, Löscher W

出版信息

Arzneimittelforschung. 1976 Feb;26(2):299-301.

PMID:779804
Abstract

The anticonvulsant effect of di-n-propylacetic acid (n-DPA) was studied in mice and compared to those of phenobarbital, trimethadione and ethosuximide. n-DPA was only weakly active in the maximal electroshock test, but had an ED50 of 420 mg/kg orally in the pentetrazole seizure threshold test, which corresponds rather well to the activity of trimethadione and ethosuximide. The duration of action was only short, and the first signs of neurotoxicity--inability to perform in the chimney test--appeared well below the anticonvulsant ED50 against pentetrazole. n-DPA proved to be most active against convulsions induced by picrotoxin (ED50 200 mg/kg orally), which might indicate a role of the elevation of the central levels of gamma-aminobutyric acid in the anticonvulsant effect of the drug.

摘要

研究了二正丙基乙酸(n-DPA)对小鼠的抗惊厥作用,并与苯巴比妥、三甲双酮和乙琥胺的抗惊厥作用进行了比较。n-DPA在最大电休克试验中活性较弱,但在戊四氮惊厥阈值试验中口服的半数有效剂量(ED50)为420mg/kg,这与三甲双酮和乙琥胺的活性相当。其作用持续时间较短,在抗戊四氮惊厥的半数有效剂量以下就出现了神经毒性的最初迹象——无法在烟囱试验中完成动作。n-DPA对印防己毒素诱发的惊厥最为有效(口服半数有效剂量为200mg/kg),这可能表明该药抗惊厥作用中γ-氨基丁酸中枢水平升高所起的作用。

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