Ipamorelin is a selective growth-hormone secretagogue that acts as an agonist at the ghrelin (GHS-R1a) receptor to stimulate pituitary somatotroph signaling in preclinical models. Compared with older GHS compounds, mechanistic studies indicate ipamorelin shows relative selectivity for growth-hormone release with reduced activity at pathways linked to ACTH or strong prolactin stimulation in many animal and cellular assays; pharmacology papers and structural receptor work place ipamorelin in the broader class of ghrelinergic secretagogues whose actions are mediated by G-protein coupled receptor signaling and downstream GH-IGF axis modulation in nonclinical systems.

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