The incidence of acute and chronic cerebrovascular disease is high，whereas effective treatment in clinical practice is still lacking. The discovery of potential drug targets by further understanding the pathogenesis of cerebrovascular disease remains an important strategy. The brain microvasculature plays an important role as a delivery pipeline of oxygen and energy for the brain. The accumulating evidence indicated that cerebral microvascular system have unique structural and functional features，which are different from peripheral vascular system. Cerebral capillaries are important compo? nents of neurovascular units and constitute the blood-brain barrier. The inflammatory responses and oxidative/nitrosative stress are critical mechanisms that cause cerebral microvascular injury and dysfunction. The disease models in combined with in vivo imaging systems can be used to further analyze the spatiotemporal changes of related molecular events. Focusing on how to protect the integrity of brain microvascular structures and functions，this review also summarizes the progress and prospects of drug discovery for acute and chronic cerebrovascular diseases.