Fischer W, Schilling E, Schmiedel R, Müller M
Pharmazie. 1982 Dec;37(12):858-61.
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.).
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。