Ghrelin, a newly discovered endogenous hormone that is produced by the stomach, and synthetic peptides have been identified recently as potent growth-hormone secretagogues. This effect is exerted through interaction with a specific G-protein-coupled receptor, GHS-R1a, which is expressed mainly in the hypothalamus-pituitary complex. A study of the peripheral distribution of GHS receptors has shown that it is also present in cardiovascular tissue, which has led to the exploration of the cardiovascular functions of ghrelin and synthetic, growth-hormone-releasing peptides. These ligands have several cardiovascular activities, including a cardioprotective effect against myocardial ischemia, and vasoactive and cardiotropic effects in both experimental models and humans. These effects are mediated by the interaction of these ligands with binding sites, including GHS-1Ra, for which the signalling pathways are not documented fully. Identification of the cardiac and vascular binding sites for ghrelin and synthetic, growth-hormone-releasing peptides will provide new perspectives for treating cardiovascular diseases with these ligands.