3,4-二氯苯丙烯酰异丁胺对中枢神经系统的药理作用

7903是一种新的胡椒碱衍化物,口服给药易从胃肠道吸收,作用出现快。大鼠口服后2小时已有较强的抗MES作用,4小时作用达高峰。有效时间持续较长,48小时作用才消失。7903的抗惊厥作用较强;对多种急性和慢性实验性癫痫模型有不同程度的对抗作用,其中以对抗硫酸锌惊厥、MES和AS的作用最强;对抗戊四唑惊厥和谷氨酸钠惊厥次之。这些作用比其它胡椒碱衍化物强。此外,7903还具有镇静作用和加强其它中枢抑制药的中枢抑制作用。

THE PHARMACOLOGICAL ACTIONS OF 3,4-DICHLOROPHENYL PROPENOYL ISOBUTYLAMIDE ON THE CENTRAL NERVOUS SYSTEM

7903, an analogue of piperine, was shown to be a potent broad spectrum anticonvulsant. In doses less than TD_(50), it was found to be able to protect rats and mice from seizures produced by maximum electroshock (MES), metrazol, sound of electric bell (audiogenic), soclium glutamate andzinc sulfate. It also showed therapeutic effect in treating experimental epilepsy produced by intracerebral injection of ferrous sulfate in rabbits and normalized the ECOG. No protection in mice from seizures produced by picrotoxin and strychnine was found. However, the mortality of animals was reduced to various extent by pretreatment with 7903. Its action resembled diphenylhydantoin in protecting rats arid mice from MES. However, it was shown to antagonize metrazol seizure without producing convulsions when used in large doses. It also resembled phenobarbital in anticonvulsive spectrum, although it does not produce anesthesia in large doses. In addition, it was found to have sedative-hypnotic and weak tranquillizing actions, and intensify the central depressive actions of other depressants when used in combination.