Ipamorelin is a peptide-selective agonist of growth hormone releasing peptides/growth hormone secretagogue receptors (GHS) and a growth hormone secretagogue.
Ipamorelin is a pentapeptide (AIb-his-D-2-NAL-D-Phit-Lys-NH2) that has shown high GH-releasing potency and efficacy in vitro and in vivo. As a result of a major chemical program, ipamorelin was found in a range of compounds lacking Ala-Trp, the central dipeptide of growth hormone releasing peptide (GHRP) -1.
Ipamorelin, also known as NNC-26-0161, is a a ghrelin mimetic. Ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. Ipamorelin may ameliorate the symptoms in patients with POI. Ipamorelin accelerates gastric emptying in a rodent model of postoperative ileus through the stimulation of gastric contractility by activating a ghrelin receptor-mediated mechanism involving cholinergic excitatory neurons.
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In vitro experiments, ipamorelin released GH from primary rat pituitary cells with similar efficacy to GHRP-6. Pharmacological analyses using GHRP and growth hormone-releasing hormone (GHRH) antagonists clearly show that, like GHRP-6, Ipamorelin /Ipamorelin stimulates GH release through GHRP-like receptors.
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