Due to the wide distribution of GHS-R1a in CNS and in periphery,and its involvement in several physiological functions, ligands modulatingGHS-R1a signaling pathways might be beneficial to the treatment ofnumerous disorders, including anorexia, cachexia, sarcopenia, gastrointestinaland metabolic diseases, neurological and neurodegenerative disorders,pain, and substance use disorders (Table 1).12,53 The effects of smallmolecules behaving as GHS-R1a agonists, antagonists, and inverse agonistson such pathologies will be discussed in this section. This evidence concerns the gene GHSR and metabolic disease.