Liu J F, Pei Y Q, Wang Z D, Xu J G, Lei X P, Ling Y Z
Department of Pharmacology, Beijing Medical University.
Yao Xue Xue Bao. 1994;29(3):166-70.
The anticonvulsive activity of three kinds of pyrazolidinones: 5-benzyl-substituted-3-pyrazolidinones; 5-benzyl-1-alkyl substituted and 1-alkyl substituted-3-pyrazolidinones were studied. Fourteen substitutes of these three kinds of pyrazolidinones were found to be potent anticonvulsants. In doses less than TD50, they were found to be able to protect mice and rats from seizures produced by maximal electroshock seizure (MES), such action appeared rapidly and lasted for a short period. II-f was shown to be the most potent anti-MES agent among these three kinds of pyrazolidinones. It also showed therapeutic effect in treating experimental epilepsy produced by intrahippocampal injection of zinc sulfate in rabbits and audiogenic seizures in rats. The third kind of pyrazolidinones also showed anti-metrazol induced seizures in mice.
5-苄基取代的-3-吡唑啉酮;5-苄基-1-烷基取代的和1-烷基取代的-3-吡唑啉酮。发现这三种吡唑啉酮的14种取代物是有效的抗惊厥药。在小于半数中毒剂量(TD50)的剂量下,发现它们能够保护小鼠和大鼠免受最大电休克惊厥(MES)引起的癫痫发作,这种作用出现迅速且持续时间短。II-f被证明是这三种吡唑啉酮中最有效的抗MES药物。它在治疗兔海马内注射硫酸锌引起的实验性癫痫和大鼠听源性癫痫发作方面也显示出治疗效果。第三种吡唑啉酮在小鼠中也显示出对抗戊四氮诱发的癫痫发作的作用。