Ghrelin is a recently discovered small peptide released primarily from the stomach and reported to exert a strong growth hormone-releasing activity. Ghrelin and its receptors are widely distributed in the body. In addition to its well-known role in regulating metabolism and appetite, ghrelin has been proved to inhibit sympathetic excitation and proapoptotic cascades, protect against oxidative damage and modulateimmunity, inflammation and autophagy. Recent studies indicate that ghrelin has powerful cardiovascular protective effects such asregulating intracellular calcium concentration, protection of endothelial cells, decreasing blood pressure and ameliorating ischemia/reperfusion injury. Therefore, targeting the ghrelin receptor and ghrelin signaling hold great potential and clinical applications in the prevention and treatment of cardiovascular diseases.