Gardner C R, Webster R A
Eur J Pharmacol. 1977 Apr 7;42(3):247-56. doi: 10.1016/0014-2999(77)90291-6.
The effects of leptazol and bicuculline on the efflux of endogenous acetylcholine (ACh) from the surface of the cerebral cortex have been related to EEG activity in urethane-anaesthetised rats. During seizure activity there was a calcium dependent increase in ACh efflux which was related to increase EEG activity and clonic muscle movements. ACh release and EEG activity were reduced during convulsive activity by trimethadione but not phenytoin. Phenobarbitone reduced convulsive EEG activity but left ACh release relatively unaffected. Blood pressure changes induced by convulsant and anticonvulsant drugs were not consistently related to EEG activity or ACh release. It is suggested that ACh efflux from the cerebral cortex is closely related to the activity of neurones within the cortex where it is released from nerve endings. Comparison of EEG changes induced by anticonvulsants and urethane during control and convulsant activity showed that only trimethadione produces anticonvulsant activity unaccompanied by general CNS depression.
在氨基甲酸乙酯麻醉的大鼠中,已将戊四氮和荷包牡丹碱对大脑皮质表面内源性乙酰胆碱(ACh)外流的影响与脑电图活动联系起来。在癫痫发作活动期间,ACh外流出现钙依赖性增加,这与脑电图活动增加和阵挛性肌肉运动有关。在惊厥活动期间,三甲双酮可降低ACh释放和脑电图活动,但苯妥英钠则无此作用。苯巴比妥可降低惊厥性脑电图活动,但对ACh释放影响相对较小。惊厥药和抗惊厥药引起的血压变化与脑电图活动或ACh释放并无始终一致的关联。提示大脑皮质的ACh外流与皮质内从神经末梢释放ACh的神经元活动密切相关。对照期和惊厥活动期抗惊厥药和氨基甲酸乙酯引起的脑电图变化比较显示,只有三甲双酮产生的抗惊厥活性不伴有全身性中枢神经系统抑制。