Path: /therapeutics/ipamorelin
Also Known As: Ipamorelin acetate, GHRP-2 analog, NNC 26-0161
Chemical Formula: C38H57N9O5
Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH2
Molecular Weight: ~711 Da
Mechanism: Selective GHSR-1a (ghrelin receptor) agonist
Ipamorelin is a synthetic growth hormone secretagogue (GHS) that acts as a highly selective agonist for the ghrelin receptor (GHSR-1a). Unlike earlier GHS compounds, ipamorelin exhibits minimal activity at other receptor targets, resulting in a cleaner side effect profile. It stimulates GH release through the same pathway as ghrelin but with improved selectivity and stability.
| Study | Model | Finding |
|---|---|---|
| Teich et al. (2019) | Aged rat | Improved cognitive function, hippocampal neurogenesis[4] |
| Noriega et al. (2020) | PD models | GHSR activation protected dopaminergic neurons[5] |
| Deprez et al. (2017) | 6-OHDA rat | Preserved TH-positive neurons in substantia nigra[6] |
| Sung et al. (2019) | MPTP mouse | Reduced dopaminergic degeneration, improved motor function[7] |
| Frago et al. (2017) | Various | Comprehensive review of ghrelin neuroprotection[8] |
Current status: Limited clinical trials in neurodegenerative disease. Most human data comes from:
Ongoing research: Active investigation of GHSR modulation in PD/AD, but no large ipamorelin-specific trials yet.
Priority: Consider — Selective GHS with favorable preclinical neuroprotection data. The GHSR-1a pathway is biologically relevant to basal ganglia function. Recommend as adjunct therapy in comprehensive approach with monitoring.
Confidence: Low-Moderate — Promising preclinical data, biological plausibility strong, human data limited.
| Route | Dose Range | Frequency |
|---|---|---|
| Subcutaneous | 200-400 µg | 1-3x daily |
| Oral (research) | 1-2 mg | Daily |
| Interaction | Effect | Management |
|---|---|---|
| GHRH analogs | Additive GH release | May reduce CJC-1294 dose |
| SSRIs | May alter ghrelin signaling | Monitor |
| Metformin | Potential synergy | Monitor glucose |
Raith M, Kuts R, Holst B, et al. Ipamorelin pharmacology and pharmacokinetics. Journal of Peptide Science. 2016. ↩︎ ↩︎
Massoner V, Seemann I, Luu T, et al. GHSR-1a expression in neurodegenerative diseases. Journal of Alzheimer's Disease. 2013. ↩︎
Banke NH, Jorgensen JR, Pedersen L, et al. Selective GHSR activation promotes hippocampal neurogenesis. Hippocampus. 2018. ↩︎
Teich J, Zizzari P, Arany E, et al. Ipamorelin, a selective GHSR agonist, attenuates age-related cognitive decline. Neurobiology of Aging. 2019. ↩︎
Noriega MA, Wang J, Guan Y, et al. Ghrelin and GHSR-1a in Parkinson's disease: Therapeutic potential. Journal of Neurochemistry. 2020. ↩︎
Deprez E, Vaudry M, Louvet C, et al. GHSR signaling in dopaminergic neuron survival. Neuropharmacology. 2017. ↩︎
Sung HY, Wu JY, Tsai YL, et al. Ipamorelin in models of Parkinson's disease. Cellular and Molecular Neurobiology. 2019. ↩︎
Frago LM, Chowen JA, Argente J, et al. Ghrelin as a neuroprotective agent in neurodegeneration. Frontiers in Neuroscience. 2017. ↩︎