Ghrelin, a gastric peptide involved in growth hormone release and energy homeostasis, is the endogenous ligand of the growth hormone secretagogue receptor type 1a (GHS-R1a), a G-protein coupled receptor mainly expressed in the pituitary and hypothalamus. This receptor mediates the main ghrelin-stimulated endocrine actions and some of the nonendocrine actions. However, a number of nonendocrine actions associated with ghrelin appear to be mediated by various GHS-R1a-related receptor subtypes, which are widely distributed in the central and peripheral tissues. This review summarises data concerning the localisation, regulation and function of GHS-R1a, as well as related receptors.