Peptide Ipamorelin is a synthetic, selective Growth Hormone Secretagogue (GHS) that mimics the action of ghrelin, the endogenous ligand for the GH secretagogue receptor (GHSR). It functions by binding to the GHSR in the pituitary gland, resulting in a robust, pulsatile release of endogenous growth hormone (GH). Ipamorelin is valued in clinical practice for its high selectivity, meaning it typically stimulates GH release without significantly affecting the secretion of other hormones like cortisol, prolactin, or ACTH.
Origin
Ipamorelin was developed through medicinal chemistry efforts to create a stable, non-peptidyl mimetic of ghrelin with improved pharmacological properties. Its development marked a step toward safer, more targeted stimulation of the growth hormone axis.
Mechanism
The peptide selectively activates the GHSR on somatotroph cells in the anterior pituitary. This activation triggers an intracellular signaling cascade that strongly promotes the exocytosis of GH, leading to increased circulating levels of GH and subsequently IGF-1. Its lack of significant impact on cortisol or appetite pathways distinguishes it from other ghrelin mimetics, offering a cleaner physiological profile for therapeutic use.
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