ObjectiveThe aim of this study was to investigate the neuroprotective effects of intra-arterial administration of edaravone dexborneol in rats with acute ischemic stroke and determine the optimal dose. Materials and methodsFirstly, 120 male Sprague-Dawley rats (265–300 g) were selected to establish ischemic stroke models and were randomly divided into groups of sham-operation (Sham group), cerebral ischemia-reperfusion (IS group), permanent focal ischemia (PI group) and treatment (2MG group: 2 mg/kg, 4MG group: 4 mg/kg, 6MG group: 6 mg/kg) groups. There are 20 rats in each group, and ten rats in each group were randomly selected for Longa score and 2,3,5-triphenyl tetrazolium chloride staining to observe the changes in neurological function and the proportion of cerebral infarct volume in each group. Secondly, the remaining ten rats in each group were scored for Longa and tested for free radicals (hydroxyl radical; peroxynitrite; nitric oxide) and pro-inflammatory cytokines (interleukin 6; interleukin-1β; tumor necrosis factor-α). We monitored changes in the indicators in each group of rats. ResultsThere were no significant differences among the enrolled Sprague-Dawley rats concerning age, sex, and feeding conditions. Edaravone dexborneol could significantly reduce the cerebral levels of hydroxyl radical, interleukin 6, interleukin-1β, tumor necrosis factor-α, and their behavioral scores of acute ischemic stroke rats after a single dose in the carotid artery. The results suggested that 4 mg/kg might be an appropriate dose. ConclusionsA single intra-arterial administration of edaravone dexborneol can improve neurobehavioral function and alleviate cerebral injury in acute ischemic stroke rats through anti-inflammatory and free radical scavenging effects.