Recent studies have revealed that lysophosphatidylcholine (LPC) produces mechanical and metabolic derangements in perfused working rat hearts and Ca2+-overload in isolated cardiac myocytes. Thus, LPC possesses an ischemia-like effect on the heart. Therefore, a drug that possesses an anti-LPC action would protect or improve ischemia/reperfusion damage. We examined the effects of various anti-ischemic drugs on the Ca2+ overload induced by LPC. Our data suggest that a drug with high lipophilicity possesses a protective effect on cell injury induced by LPC, probably because of preservation of membrane integrity.