Abstract

Growth hormone secretagogues (GHS) are synthetic molecules that promote secretion of growth hormone by activation of the GHS receptor (GHSR). Ghrelin is the endogenous ligand of this receptor, which was isolated from gastric mucosa. This peptide is widely expressed in different tissues and has a broad spectrum of effects. This review summarises: i) structure and pharmacokinetics of the more important GHS; ii) structure, distribution and subcellular pathways of ghrelin; iii) structure, distribution and signal transduction of the GHS receptors; and iv) effects of GHS in different tissues and organs and the potential therapeutic role of ghrelin and GHS. There are increasing evidences that GHS and ghrelin have a wide range of actions both in physiological and pathological conditions. Potential therapeutic applications of these GHS are constantly increasing and clinical trials are needed to establish usefulness of these compounds.