Tissue-type plasminogen activator(tPA) is a highly specific serine proteinase that activates the zymogen plasminogen to the broad-specificity proteinase plasmin.Tissue-type plasminogen activator is found not only in the blood,but also in the central nervous system(CNS).There is a growing body of evidence demonstrating the participation of tPA in a number of physiological and pathological events in the CNS,as well as nonhemostatic roles of tPA in the CNS.This paper will focus on physiological function of tPA and its toxicological action in the CNS.