GHRP-6 acts as a potent and selective agonist of the growth hormone secretagogue receptor (GHS-R1a), a G protein-coupled receptor primarily located in the hypothalamus and pituitary gland. Upon binding to this receptor, GHRP-6 triggers an intracellular signaling cascade involving phospholipase C (PLC) activation and calcium mobilization, leading to GH release from anterior pituitary somatotrophs. Unlike GHRH, which acts via the GHRH-R, GHRP-6 potentiates GH response even in the presence of somatostatin (GH inhibitor). Additionally, it stimulates cortisol and prolactin release and has orexigenic effects (increased appetite) mediated by activation of NPY/AgRP neurons in the hypothalamus.
- Target receptor: GHS-R1a (ghrelin receptor)
- Primary mechanism: PLC activation, intracellular calcium increase, GH release
- Additional effects: Stimulation of cortisol, prolactin, and appetite