Summary
Hexarelin is a methylated analog of GHRP-6 that releases growth hormone after injection, nasal or oral administration in people. It also binds CD36 in heart tissue, which has made it a research tool for GH-independent cardiac effects. GH response fades with continuous use.
Structure
His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2, a methylated GHRP-6 analog.
How it works
Hexarelin activates GHS-R1a and separately binds the scavenger receptor CD36 in the heart, where it has shown protective effects in animal models of ischaemia.
Research use cases
Areas where Hexarelin has been studied. Inclusion here does not mean it works for that purpose.
- GH release studies
- Cardioprotection research via CD36
What the research found
Routes of administration
In healthy volunteers, hexarelin released GH after intravenous, subcutaneous, intranasal and oral doses, with oral bioavailability far lower.1
Cardiac receptor
Hexarelin bound CD36 in heart membranes and raised coronary perfusion pressure in isolated rat hearts, independently of GH.2
Safety and open questions
Raises cortisol and prolactin. GH response diminishes with repeated dosing (tachyphylaxis).
Regulatory status
Not approved. Research compound.
Status was accurate when this page was last reviewed on October 26, 2026. Regulations change; check with the relevant authority before relying on it.
Hexarelin: common questions
Why does hexarelin stop working over time?
Continuous activation of the ghrelin receptor leads to desensitization. Studies of repeated dosing showed partial loss of GH response within weeks.
Is Hexarelin approved for human use?
Not approved. Research compound.
References
- Ghigo E, Arvat E, Gianotti L, et al. (1994). Growth hormone-releasing activity of hexarelin, a new synthetic hexapeptide, after intravenous, subcutaneous, intranasal, and oral administration in man. Journal of Clinical Endocrinology & Metabolism.
- Bodart V, Febbraio M, Demers A, et al. (2002). CD36 mediates the cardiovascular action of growth hormone-releasing peptides in the heart. Circulation Research.
Links open a PubMed search for the exact title, or the original source where one is given.