Abstract: With the aggravation of the aging problem, the incidence of stroke has increased year by year, with the proportion of ischemic stroke accounting for the majority. In recent years, thrombolytic therapy and mechanical thrombectomy are the major clinical treatments for ischemic stroke, but with limited efficacy. Many patients suffer severe disability after the treatment which fails to further prevent brain tissue damage and neurological dysfunction caused by ischemia, probably due to the lack of adjuvant therapy with effective neuroprotective agents. At present, the majority of neuroprotective agents have no obvious effects in clinical trials. This review briefly described the various classes of neuroprotective agents for cerebral ischemic injury and cerebral ischemia-reperfusion injury and their disadvantages in clinical application, so as to accelerate the successful clinical application of neuroprotective agents and provide reference for the future treatment of cerebral ischemic stroke.