The changes of t-PA, PAI-1 gene expression and t-PA activity were investigated in coronary arteries of Acute Myocardial Infarction (AMI) rat by nucleic acid molecular hybridization and spectrophotometric assay. The effect of preconditioning on t-PA and PAI-1 was observed in this model. The results indicated that: (1) Tissue t-PA activity in ischemia was significantly decreased than that in control (P < 0.01). t-PA activity was obviously increased in preconditioning group (P < 0.01 compared with ischemia group). (2) t-PA and PAI-1 mRNA expression in ischemia were higher than that in control, especially PAI-1 4.6 times higher than that in control), while PAI-1 expression lower in preconditioning rat. (3) In situ hybridization showed t-PA and PAI-1 were primarily expressed by endothelial cells in vessels of rat heart. These data suggested that abnormal expression of PAI-1 and t-PA was involved in AMI. This fibrinolytic depress was associated with high PAI-1 expression. Preconditioning may be effective to protect myocardium through decreasing PAI-1 mRNA expression.