Source: Raun K. et al., European Journal of Endocrinology, 1998, Ipamorelin: The First Selective Growth Hormone Secretagogue
To determine the pharmacological profile of Ipamorelin – the first selective Growth Hormone Secretagogue (GHS) – and to evaluate its ability to stimulate growth hormone (GH) secretion without affecting other pituitary hormones such as ACTH, cortisol and prolactin.
Ipamorelin is a synthetic pentapeptide developed as a selective agonist of the GHS-R1a receptor, designed to provide more specific and safer GH stimulation compared to older GHRP peptides (such as GHRP-2 and GHRP-6), which often trigger nonspecific hormonal responses.
Type: preclinical and clinical experimental studies
Models: animal models (rats, pigs) and healthy volunteers
Interventions: administration of Ipamorelin at various doses
Comparative agents: GHRP-6 and GHRP-2
Measured parameters:
Serum growth hormone (GH) levels
ACTH, cortisol, prolactin and other hormone levels
Duration and intensity of hormonal response
Selectivity of Action
Ipamorelin induces a dose-dependent and selective increase in GH, without changes in ACTH, cortisol and prolactin levels.
Its profile differs from that of GHRP-6 and GHRP-2, which also activate other hormonal pathways.
Pharmacodynamics
A rapid GH peak is observed around 10 minutes after administration, with a short duration of action (30–60 minutes).
The effect is reproducible and stable with consecutive administrations, with no signs of desensitization.
Comparative Efficacy
Ipamorelin shows similar efficacy to GHRP-6 in terms of GH release, but with significantly better selectivity and safety.
Safety
No adverse effects on the adrenal axis or other endocrine systems were observed.
Good tolerability in animal and human models.
Ipamorelin is the first selective agonist of GHS-R1a, which stimulates only growth hormone without affecting other pituitary hormones.
It shows a dose-dependent, predictable and safe hormonal response.
Suitable for research on GH regulation, anabolic processes and models of GH deficiency.
The primary data come from early preclinical and Phase I studies.
No long-term clinical outcomes are available.
Ipamorelin is a promising selective GH secretagogue with an excellent safety profile.
Suitable for research applications in endocrinology and metabolic sciences.
Advantageous over classical GHRP peptides due to the lack of effect on ACTH and cortisol.