Background Remifentanil is a novel, opioid receptor agonist which is commonly used during anesthesia procedure, and has protective effects against ischemia-reperfusion injury(IRI) in vital organs. Purpose To review the chemical properties and the characteristics of its pharmacokinetics, the protective effects against IRI and possible mechanisms. Content Many researches have reported that remifentanil can protect against heart, liver, nerve and kidney IRI in different animal models. The related mechanisms are far from clear. Opioid receptors, PKC/KATP channel, NO/NOS, and anti-apoptotic pathways are the most concerned in published articles. Trend Remifentanil maybe widely accepted as an effective drug for both perioperative analgesia and IRI protection.