Sarpogrelate, a 5-HT2 receptor blocker, may have a preconditioning-like effect in patients with coronary artery disease.

Background: Sarpogrelate, a serotonin receptor blocker, increases collaterals via a platelet anti-aggregation effect and/or vasodilatation. However, a recent report showed a preconditioning effect of sarpogrelate that enhances the translocation of PKC-epsilon of cardiomyocytes, followed by opening of the mitochondrial K(ATP) channel via inhibition of serotonin release from platelets during ischemia, protecting against cellular injury in rabbit hearts without collaterals. The present study used a percutaneous coronary intervention (PCI) model to define the protective effect of sarpogrelate against ischemic injury and its mechanism in human coronary artery disease.