加锡果宁的中枢抑制作用与神经递质受体的关系

Relevance of central depression by edulinine(ed) and neurotransmittens and receptors in brain

加锡果宁ip或ig后能诱发小鼠入睡,明显延长戊巴比妥钠小鼠的睡眠时间和入睡鼠数,对抗小鼠、大鼠MES,提高小鼠脑内DA、DOFAC、5-HT、HVA含量,并能从受体上置换出~3H-绳蕈醇,~3H-安定,其IC_(50)分别为5×10^(-4)M及4.4×10^(-5)M,提示加锡果宁的抗惊厥作用可能与其学兴奋DA、5-HT能神经元,提高DA、5-HT递质含量、激活苯二氮唑受体有关。

Edulinine (ed), an alkaloid isolated from Zanihoxyjum Simians Hance, was found to have sedative-hypnotic and anticonvulsive action in mice and rats. Simultaneous determination of concents of monoamines and their main metabolites in rats brain using HPLC with electrochemiccal detectiion indicated that DA, DOPAC, HVA and 5-HT increased significantly. Using radioligand binding assay method, the ICscs of ed for replacement of H-muscimol and 3H-diazepam were 5 Xl54 M and 4.4X10M, respectively. It is suggested that the anticonvulsive action of ed may be related to the stimulation of dopaminergic and serotoninnergic systems and elevation of DA, 5-HT levels and the activation of benzodiazepine receptors in brain.