The specific biological action of Ipamorelin, a selective growth hormone secretagogue (GHS) peptide, which stimulates the pituitary gland to release endogenous growth hormone (GH). This pentapeptide is characterized by its high selectivity for the ghrelin/GH secretagogue receptor (GHSR) without significantly affecting the release of other pituitary hormones like cortisol or prolactin. Its clinical utility lies in safely augmenting the pulsatile secretion of GH.
Origin
Ipamorelin was developed in the late 20th century as part of research into synthetic peptides that could safely mimic the natural action of ghrelin, the endogenous ligand for the GHSR. Its mechanism represents a targeted pharmacological strategy to address age-related decline in growth hormone secretion.
Mechanism
Ipamorelin acts as an agonist at the GHSR, primarily located in the anterior pituitary. Upon binding, it triggers a calcium-dependent signaling cascade within the somatotroph cells, resulting in a robust, natural release of GH pulses. Critically, it does not significantly increase appetite or cortisol levels, distinguishing its clinical profile from earlier-generation GHS compounds.
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