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Selective GHSR‑1a agonist that increases GH with minimal ACTH/cortisol elevation versus older GHRPs. Potential benefits include supporting lean mass, recovery and GH pulsatility in research settings. Generally better endocrine selectivity than earlier secretagogues, but long‑term outcomes data are limited.
Description
Ipamorelin is a synthetic pentapeptide and selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR‑1a). It is designed as a growth hormone secretagogue with high specificity for GH release and minimal activation of the hypothalamic–pituitary–adrenal axis. Pharmacologically, ipamorelin increases circulating GH in animals and humans with little to no associated rise in ACTH or cortisol compared with earlier GHRPs.
Chemical Structure / Identifiers
| Property | Detail |
| Sequence (pentapeptide) | Aib‑His‑D‑2‑Nal‑D‑Phe‑Lys‑NH₂ (Aib = aminoisobutyric acid; D‑2‑Nal = D‑2‑naphthylalanine) |
| Molecular Formula (free base) | C38H49N9O5 |
| Molecular Weight (free base) | ≈ 711.85 g/mol |
| CAS Number | 170851‑70‑4 |
| PubChem CID | 9831659 (parent compound); salts such as the acetate are listed separately |
| Primary Target | GHSR‑1a (ghrelin receptor) |
Primary Research Focus
• Selective GH release: robust growth hormone secretion in vitro and in vivo with minimal effects on ACTH/cortisol compared with GHRP‑2/6.
• Endocrine selectivity: little to no change in FSH, LH, PRL or TSH in animal studies at efficacious GH‑releasing doses.
• Clinical exploration: investigated for postoperative ileus; development in that indication was discontinued following limited efficacy.
• Mechanistic pathway: mimics ghrelin signaling through GHSR‑1a to stimulate somatotrophs and GH pulse amplitude/frequency.
Safety / Limitations
• Adverse events reported in studies include nausea, headache, flushing and injection‑site reactions; transient changes in blood pressure/heart rate may occur.
• Long‑term safety and efficacy data outside controlled trials are limited; not approved as a therapeutic for general clinical use. Research Use Only.
• While GH‑selective, endocrine responses are dose‑ and context‑dependent; co‑morbid HPA axis conditions warrant careful monitoring in research settings.
Key Publications / References
PubChem Compound Summary: Ipamorelin (CID 9831659). https://pubchem.ncbi.nlm.nih.gov/compound/Ipamorelin
Raun K et al. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998. PubMed: https://pubmed.ncbi.nlm.nih.gov/9849822/
Wikipedia overview: Ipamorelin (identifiers, pharmacology). https://en.wikipedia.org/wiki/Ipamorelin
Sigma‑Aldrich: Ipamorelin acetate (identifiers; CAS 170851‑70‑4; formula). https://www.sigmaaldrich.com/US/en/product/sigma/sml1322
Sinha DK et al. Beyond the androgen receptor: the role of growth hormone and its secretagogues (includes ipamorelin pathway context). PMC: https://pmc.ncbi.nlm.nih.gov/articles/PMC7108996/
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