The protective effect and mechanism of diazepam on ischemia neurons during cerebral ischemia and reperfusion were studied. Sixty three Wistar rats were divided randomly into nine groups: control group , ischemia groups including subgroups of is3h, is3 h/rep1 h, is3 h/rep2 h, is3 h/rep3 h, diazepam treated groups , including subgroups of is3 h, is3 h/rep1 h, is3 h/rep2 h, is3 h/rep3 h with Zea longa’s animal model of middle cerebral artery occlusion. The comparison between the ischemia group and diazepam treated group showed that diazepam could obviously decrease the production of glutamate, asparate, MDA and increase the synthesis and release of GABA, SOD and GSH PX. It was concluded that diazepam exerted its protective effects on neurons through complex mechanisms of regulating the synthesis and release of excitotary/inhibitory amino acids and free radicals. The protective effect and mechanism of diazepam on ischemia neurons during cerebral ischemia and reperfusion were studied. Sixty three Wistar rats were divided into nine groups: control group, ischemia groups including subgroups of is3h, is3h / rep1h, is3h / rep2h , is3h / rep3h, diazepam treated groups, including subgroups of is3h, is3h / rep1h, is3h / rep2h, is3h / rep3h with Zea longa’s animal model of middle cerebral artery occlusion. The comparison between the ischemia group and diazepam treated group showed that diazepam could obviously reduce the production of glutamate, asparate, MDA and increase the synthesis and release of GABA, SOD and GSH PX. It was done that diazepam exerted its protective effects on neurons through complex mechanisms of regulating the synthesis and release of excitotary / inhibitory amino acids and free radicals.