【摘要】：[Objectives] To explore the protective effect of Sanguis Draconis flavones(SDF) on rat focal cerebral ischemia-reperfusion injury(CIRI) models established by middle cerebral artery occlusion(MCAO). [Methods] A total of 60 healthy adult male Sprague-Dawley rats were selected. They were evenly and randomly divided into sham group, model group, edaravone group(12 mg/kg) and SDF group(360 mg/kg), and administered intragastrically and intraperitoneally. The middle cerebral artery of each rat was blocked by suture-occluded method to establish a CIRI model. After ischemia for 2 h and reperfusion for 48 h, the pathological injury on the ischemic side was observed by HE staining; the neuron and myelin sheath structure was observed by transmission electron microscopy; the expression of G protein-coupled receptor kinase 2(GRK2) was preserved by immunohistochemistry; and the transfer of GRK2 was detected by western-blot. [Results] After 48 h of CIRI, the nuclei of the penumbral cortical neurons shrank, the chromatin was unevenly distributed, the nuclear membrane was dissolved and the mitochondria in the cytoplasm were swollen and vacuolated. The myelin layer was disordered. With this change, the distribution of GRK2 subcellular cells in the penumbra of the injured lateral cortex transferred from the cytoplasm to the membrane. SDF can effectively restore neuronal and myelin sheath structural damage and reduce the functional(membrane coupling) expression of GRK2. [Conclusions] GRK2 may be an effective target for SDF to protect the impaired blood-brain barrier(BBB) in CIRI.