Ghrelin is a peptide produced predominantly in the stomach and intestines, and is a natural growth hormone (GH) secretagogue-receptor ligand. It is able to stimulate GH release, but it also exhibits an important role in conditions related to processes regulating nutrition, body composition and growth, and heart, liver, thyroid or kidney dysfunction. Drug discovery efforts initially focused on ghrelin-receptor agonists, known as GH secretagogues, to be used as anabolic agents, but none of them reached the market.The latest developments in this field are constituted by the discovery of new nonpeptidic compounds endowed with interesting properties: oxindole agonists are able to exert an increase in the fat-free mass, while ghrelin was reported to increase the fat mass gain, and triazole- and 2,4-diaminopyrimidine-based antagonists were shown to be able to reduce food intake, without inhibition of GH secretion stimulated by an agonist to the ghrelin receptor. Other antagonist compounds (quinazolinones) were discovered as antiobesity/antidiabetic agents. Moreover, inverse agonists have been discovered that are able to reduce weight gain.Taking into account the great number of pathological conditions related to ghrelin, and the discovery of several compounds able to modulate the ghrelin receptor, its importance in the field of medicinal chemistry research is set to increase significantly.