Monoamine oxidase (MAO) inhibitors have been used for many years in the treatment of psychiatric and neurological disorders. More recently, some of these drugs and their analogues have been shown to have neuroprotective and neurorescue effects in several models of neurologic insult, including in vitro and in vivo models of cerebral ischemia. This review will discuss current evidence regarding these aspects of l-deprenyl, tranylcypromine, phenelzine, and some structurally related drugs.