The ghrelin receptor is the target of growth hormone secretagogues, a class of synthetic peptide and non-peptide compounds that stimulate growth hormone (GH) release from the anterior pituitary. Ghrelin, the endogenous ligand for the ghrelin receptor, is predominantly secreted from X/A-like cells within the gastric mucosa and may be the source of the majority of circulating plasma ghrelin. Ghrelin stimulates gastric acid secretion and motility, and may have significant effects on appetite and energy. It is not only important for the acute regulation of food intake but also plays an important role in the regulation of long term energy homoeostasis. Ghrelin has a number of actions in cardiovascular system, consistent with the localization of receptors to cardiovascular tissue.