Cerebral ischemia is known as a major problem in the world. Transient global cerebral ischemia causes loss of pyramidal cells of brain cortex following global ischemic/reperfusion. Recently, using immunophilin ligands has been considered as a potential and appropriate strategy for neuroprotection. Since it was observed that tacrolimus (FK506), a useful immunosuppressant used in organ transplantation, provides neuroprotection and prevents neuronal damage,the importance of immunophilins in the development of neuroprotectors has emerged.