Ipamorelin is a synthetic, pentapeptide Growth Hormone Secretagogue (GHS) that selectively and potently stimulates the release of endogenous Growth Hormone (GH) from the anterior pituitary gland. It is a targeted therapeutic agent designed to mimic the action of ghrelin, the endogenous ligand for the Growth Hormone Secretagogue Receptor. Clinically, Ipamorelin is utilized to enhance endogenous GH secretion, supporting improvements in body composition, sleep quality, and tissue repair without significantly affecting cortisol or prolactin levels. Its high selectivity offers a cleaner physiological response.
Origin
Ipamorelin was developed in the late 20th century as part of the pharmaceutical effort to create more selective and safer Growth Hormone Secretagogues following the discovery of the ghrelin receptor. Its chemical structure was specifically engineered to avoid the non-selective side effects, such as increased appetite or elevated cortisol, sometimes seen with earlier GHS compounds. This development represents a refinement in peptide science for precise neuroendocrine modulation.
Mechanism
Ipamorelin functions by acting as a highly selective agonist at the Growth Hormone Secretagogue Receptor (GHSR-1a) in the pituitary gland. Its binding triggers a calcium-dependent release of stored GH from the somatotroph cells. Critically, its high selectivity for the GH release pathway means it does not significantly activate the receptors that mediate the release of other hormones, such as Adrenocorticotropic Hormone (ACTH) or prolactin, resulting in a more physiological and cleaner GH pulse.
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