Background　Peroxisome proliferator-activated receptors(PPARs) regulate the transcription of genes involved in energy metabolism and inflammation. As a target for the treatment of hypoglycemia in diabetes mellitus type 2, the γ subtype of PPARs alleviates myocardial ischemia/reperfusion injury(MI/RI), and maintains normal cardiac function. 　Objective　To review the relevant mechanisms underlying the protective effects of peroxisome proliferator-activated receptor-γ(PPAR-γ) agonists on MI/RI.　Content　PPAR-γ agonists and their pharmacological effects were first summarized. A series of evidence demonstrates that in MI/RI, PPAR-γ agonists reduce myocardial infarction area, and improve cardiac function, through both PPAR-γ-dependent and-independent pathways, involving anti-inflammatory, anti-oxidant, anti-apoptotic reactions.　Trend　Targeting PPAR-γ provides a new myocardial protection strategy against MI/RI. Additionally, new drugs with improved selectivity to PPAR-γ are highly demanded.