MetabolicWADA Prohibited
Hexarelin
Synonyms: His-D-Mrp-Ala-Trp-D-Phe-Lys-NH2
Sequence: His-D-Mrp-Ala-Trp-D-Phe-Lys-NH2
Critical Safety & Regulatory Notice
Hexarelin is classified as a regulated, unapproved, or research-only substance. Doping/Regulatory Status: Not FDA approved. Strictly prohibited by WADA.. Clinical safety profiles for human use are deficient or not approved.
History & Discovery Timeline
Hexarelin was developed in the early 1990s as a highly potent growth hormone secretagogue peptide. It was investigated for growth hormone deficiency and cardiovascular rehabilitation.
What it is: Hexarelin is a synthetic hexapeptide (His-D-Mrp-Ala-Trp-D-Phe-Lys-NH2) belonging to the ghrelin receptor agonist family. It is classified under the Metabolic category.
Proposed Mechanisms & Research Findings: It acts as a potent agonist at the ghrelin receptor, stimulating robust growth hormone secretion. It also interacts with cardiac s, demonstrating cardioprotective effects in animal models.
Regulatory & Safety Status: It is not FDA approved. Clinical development was suspended due to rapid receptor desensitization (tachyphylaxis). Gray-market injectables carry risks of hormone dysregulation and purity issues.
Athletic & Anti-Doping Status: Hexarelin is strictly prohibited by WADA under Section S2. Any detection in athletes results in long-term bans.
Understanding Hexarelin Key Facts
Primary Target System:NEUROENDOCRINE, CARDIOVASCULAR, IMMUNE
Residue Count / Length:9 Amino Acids
Primary Action & Category:Ghrelin Receptor Agonist (Metabolic)
Primary Receptors:Growth Hormone Secretagogue Receptor (GHSR), CD36 Receptor, Macrophage scavenger receptors

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