Ipamorelin (NNC 26-0161) is a synthetic pentapeptide considered the first highly selective growth hormone secretagogue (GHS). It acts via GHS-R1a receptors (ghrelin receptors) in the anterior pituitary without affecting other pituitary hormones.
OVERVIEW
Unlike other GHSs, Ipamorelin stimulates GH release without increasing prolactin, ACTH, or other pituitary hormones, making it a particularly selective candidate for clinical research. Its mechanism involves activation of phospholipase C (PLC), release of IP3 and DAG, and a rise in intracellular calcium leading to exocytosis of GH vesicles.
A clinical trial suggested GH levels rising to 80 mIU/l — over 60 times the placebo baseline — within 2 hours of administration.
RESEARCH AREAS
GH secretion — potential 60-fold increase vs. placebo (clinical trial, 8 subjects); half-life of 2 hours with peak at 0.67 h.
Bone density — possible increase in total bone mineral content (tibia, vertebrae) via hGH-mediated mechanisms (murine models, DEXA).
Digestion — apparent acceleration of gastric emptying and improvement of gastric smooth muscle contractility (murine models).
Nitrogen balance — potential 20% reduction in urea-N synthesis (CUNS) in catabolic states; improvement of nitrogen balance via IGF-1.
CHEMICAL DATA
| Molecular formula | C₃₈H₄₉N₉O₅ |
| Molecular weight | 711.86 g/mol |
| Other names | NNC 26-0161 |
| Form | Lyophilized powder |
| Purity | 99.01% HPLC |
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