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[吲哚啉衍生物的抗惊厥作用]

[Anticonvulsant effects of indoline derivatives].

作者信息

Fischer W, Schilling E, Schmiedel R, Müller M

出版信息

Pharmazie. 1982 Dec;37(12):858-61.

PMID:7163375
Abstract

The anticonvulsant activities of several indoline derivatives were tested in mice using the pentetrazole (PTZ) and electroshock seizure model. Furthermore, the toxicity and the influence on hexobarbitone anaesthesia were determined. 2-oxoindoline--the most potent anticonvulsant compound--shows a characteristic modification of PTZ-induced seizures, especially a suppression of the tonic phase and a marked prolongation of survival time at lethal PTZ-doses as well as in doses of 100 mg/kg a complete protection effect to maximum electroshock. The majority of indolines possess also a marked sedative effect. The LD50 values of the derivatives under investigation are differing considerably, however, majority of compounds being within the range of 300 to 800 mg/kg (i.p.).

摘要

使用戊四氮(PTZ)和电休克惊厥模型在小鼠中测试了几种吲哚啉衍生物的抗惊厥活性。此外,还测定了其毒性以及对戊巴比妥麻醉的影响。2-氧代吲哚啉——最有效的抗惊厥化合物——显示出PTZ诱导惊厥的特征性改变,特别是抑制强直相,在致死剂量的PTZ以及100 mg/kg剂量下显著延长存活时间,并对最大电休克有完全的保护作用。大多数吲哚啉也具有显著的镇静作用。所研究衍生物的半数致死量(LD50)值差异很大,然而,大多数化合物的LD50值在300至800 mg/kg(腹腔注射)范围内。

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