摘要
观察了三个三甲氧桂皮酰胺类化合物:3,4,5-三甲氧桂皮酰异丙胺(8701)、3,4,5-三甲氧桂皮酰环戊胺(8702)和3,4,5-三甲氧桂皮酰另丁胺(8703)的抗惊和镇静作用,发现8701具有明显的影响。它能有效的对抗最大电休克发作、戊四唑和印防己毒素所引起的惊厥,但对士的宁惊厥无效。8702和8703对上述实验性癫痫均无明显影响。8701抗戊四唑惊厥作用的机制可能与其对中枢神经递质NE和5-HT的影啊有关。
Anticonvulsant and sedative effects of some 3,4,5 -trimethoxycinnam-amides, 3 , 4 , 5-trimethoxycinnamoylisopropylamine (8701) , 3 , 4 , 5-trim-ethoxycinnamoylcyclopentylamine (8702) , and 3 , 4, 5 -trimethoxycinnamoyl-sec.-butylamine (8703),were studies in mice.The results of experiment showed that 8701 was found to be able to protect mice from seizures produced by maximal electroshock, metrazol and picrotoxin, but not from seizures produced by strychnine.8702 and 8703 have not marked anticonvulsant activity.The mechanisms of anti-MST of 8701 are mainly related to content of NE and 5-HT in the whole brain of mice: ( 1 )The pretreatment with reserpine , a depletion of monoamines in the brain, markedly antagonized the effect of anti-MST of 8701, (2) An intracerebroventricular injection of NE to mice, increased the brain NE content, enhanced the effect of anti-MST of 8701,(3) The pretreatment with disulfiram,a DA-β- hydroxylase inhibitor.reduced the brain NE content and antagonized the effect of anti-MST of 8701,(4) The pretreatment with L-tryptophane, a precursor of 5-HT, increased the brain 5-HT content and enhanced the effect of anti-MST of 8701, (5) The pretreatment with p-CPA, a tryptophane hydroxylase inhibitor, reduced the brain 5-HT content and antagonized the effect of anti-MST of 8701.8701 also exhibits sedative activity in mice.
出处
《生理科学》
CSCD
1989年第3期168-173,共6页
基金
国家自然科学基金
关键词
桂皮酰胺类
抗惊
镇静
trimethoxycinnammamides 3 , 4 , 5-trimethoxycinnamoylisopropylamine (8701) 3,4,5-trimethoxycinnamoylcyclopcntylamine (8702) 3 , 4 , 5 -trimethoxyeinnamoyl-sec, -butylamine (8703) nticonvulsant activity sedative activity NE 5-HT
