Neuroimaging in ischemic stroke continues to be one of the most developing fields in nuclear medicine. Many studies have established the efficacy of blood flow and metabolism measurements in acute ischemic stroke. Although the release of recombinant tissue plasminogen activator in clinical practice has minimized the use of SPECT or PET in the first few hours of ischemic stroke onset, implementing these techniques into a set of initial examinations is still beneficial to exclude risky patients for reperfusion therapy beyond several hours after onset. Rescuing of viable tissue suffering ischemic penumbra is an important target of early therapeutic strategy. Ischemic penumbra can be visualized by means of perfusion imaging, central type benzodiazepine receptor imaging, and hypoxy imaging. In the later phase of subacute ischemic stroke, inflammation and apoptosis can be visualized by means of peripheral-type benzodiazepine receptor imaging and annexin V imaging, respectively. Imaging of the penumbra and cellular responses will help evaluate the effects of drugs and interventions for ischemic stroke, suggesting its potential as a marker of the efficacy of future therapeutic regimens.