MetabolicWADA Prohibited
Ipamorelin
Synonyms: NNC 26-0161
Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH2
Critical Safety & Regulatory Notice
Ipamorelin is classified as a regulated, unapproved, or research-only substance. Doping/Regulatory Status: Not FDA approved. Prohibited by WADA under Section S2.. Clinical safety profiles for human use are deficient or not approved.
History & Discovery Timeline
Ipamorelin was developed by Novo Nordisk in the late 1990s (specifically 1998) as a selective growth hormone secretagogue designed to treat post-operative ileus.
What it is: Ipamorelin is a synthetic pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) belonging to the growth hormone secretagogue class. It is categorized under Metabolic.
Proposed Mechanisms & Research Findings: It acts as a selective agonist of the ghrelin receptor (growth hormone secretagogue receptor), triggering growth hormone release from the pituitary gland. Unlike GHRP-2 or GHRP-6, it does not elevate cortisol or prolactin levels.
Regulatory & Safety Status: It is not FDA approved. Clinical development was halted after Phase II trials. Sourcing gray-market injectables poses serious endocrinological risks and contamination hazards.
Athletic & Anti-Doping Status: Ipamorelin is strictly prohibited by WADA under Section S2. Use is classified as a doping violation and is heavily screened in drug tests.
Understanding Ipamorelin Key Facts
Primary Target System:NEUROENDOCRINE, CNS, IMMUNE
Residue Count / Length:9 Amino Acids
Primary Action & Category:Ghrelin Receptor Agonist (Metabolic)
Primary Receptors:Growth Hormone Secretagogue Receptor (GHSR), Hypothalamic Ghrelin Receptors, Gastrointestinal Myenteric Plexus Sites

Figure 1: Detailed molecular mechanism pathways of Ipamorelin (click to enlarge).