Ipamorelin Selective Agonist describes the pharmacological action of the synthetic peptide Ipamorelin, which acts as a highly specific activator of the growth hormone secretagogue receptor (GHSR), also known as the ghrelin receptor. Its selectivity means it triggers the release of Growth Hormone (GH) from the pituitary gland with minimal or no significant impact on the secretion of other hormones like cortisol, prolactin, or ACTH. This targeted action is a clinical advantage for optimizing GH pulsatility while avoiding undesirable side effects.
Origin
Ipamorelin was developed in the field of peptide chemistry and endocrinology as a therapeutic agent to mimic the action of the endogenous gut hormone ghrelin. The ‘Selective Agonist’ designation highlights its precise binding and activation profile at the GHSR compared to earlier, less specific secretagogues. Its development focused on maximizing therapeutic benefit through specificity.
Mechanism
As a selective agonist, Ipamorelin binds directly to the GHSR on somatotroph cells in the anterior pituitary gland. This binding activates an intracellular signaling cascade, leading to the rapid and pulsatile release of stored GH. Crucially, its unique structure prevents it from significantly activating the receptors responsible for the release of stress hormones, maintaining the integrity of the HPA axis and providing a more physiological and safer means of boosting GH levels.
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