Background A large number of opioid receptors, such as μ receptor, κ receptor, δ receptor, ε receptor, σ receptor and λ receptor exist in various organs widely. Each of them has their own endogenous ligand and functions respectively. Its protective effects in ischemia/reperfusion（I/R）- induced organ injury have aroused wide attention in medical field. Objective This review introduces the new progress on the protective effects of pharmacological preconditioning with opioid receptor agonists in I/R-induced organ injury. Content Opioid receptor agonists have been proved to simulate ischemic preconditioning（IPC）, attenuate the degree of ischemia/reperfusion injury(I/RI) and protect many organs’ functions, such as heart, brain, liver, kidney and so on. Trend Study of opioid receptors on protective effects in I/R-induced organ injury has made some progress. It provides a new method for study on IPC. However, these studies were still based on animal experiments at present．More clinical practices are needed to prove the mechanisms and effects of opioid receptor agonists．