2020
This study showed hexarelin significantly improved heart function under conditions that mimic a heart attack. Treated mice had less heart scarring, lower inflammation markers, and better cardiac output (how much blood the heart pumps). This suggests hexarelin protects the heart through anti-inflammatory pathways involving the autonomic nervous system (the body's automatic control system).
McDonald H, Peart J, Kurniawan ND, et al.
2021
Hexarelin increased pulsatile (natural-rhythm) GH release in obese mice, leading to less visceral (belly) fat, less fat buildup in the liver, and better insulin sensitivity (how well the body responds to insulin), all without changing IGF-1 levels. This suggests hexarelin helps metabolic health through direct GH effects.
Huang Z, Lu X, Huang L, et al.
2017
Hexarelin protected heart cells from damage caused by blocked and restored blood flow. It worked by reducing harmful inflammation through the IL-1 pathway (an inflammation signal), switched on when it attaches to the GHSR-1a receptor on heart cells. The heart-protecting effects were even slightly better than ghrelin's.
Huang J, Li Y, Zhang J, et al.
2021
Beyond heart benefits, hexarelin showed anti-inflammatory effects in the lungs. It improved lung function, reduced the number of immune cells moving in, and prevented the scarring (fibrosis) that can follow lung injury, showing its protective effects reach beyond the heart.
Zambelli V, Rizzi L, Delvecchio P, et al.
2014
This broad review established that hexarelin acts on the cardiovascular system directly through two receptors (docking sites): GHSR-1a and CD36. The CD36 route seems especially important for heart protection, which makes hexarelin unique among GH-releasing drugs for heart support.
Mao Y, Tokudome T, Kishimoto I
1994
In 12 healthy young volunteers, hexarelin triggered GH release at 1-2 mcg/kg IV (into a vein; 2 mcg/kg worked best) and 1.5-3 mcg/kg subcutaneously (under the skin), and also through the nose (intranasal, 20 mcg/kg) and by mouth (oral, 20-40 mg).
Ghigo E, Arvat E, Gianotti L, Imbimbo BP, Lenaerts V, Deghenghi R, Camanni F
1997
Review of the GHRP class (GH-releasing peptides) in animals and humans. The GH-releasing effect is synergistic with GHRH (the combined effect is bigger than the sum of the parts). It partly desensitizes (the body responds less over time), more with continuous infusion and less with on-and-off dosing. It is also blunted by inhibiting influences including glucose, free fatty acids, neurotransmitters (brain messengers) and glucocorticoids (steroid hormones).
Ghigo E, Arvat E, Muccioli G, Camanni F
1997
In six normal young volunteers, hexarelin 2 mcg/kg IV released more GH than GHRH (AUC 2200.8 vs 792.2 mcg/L/h; AUC is the total amount released over time). Hexarelin combined with GHRH produced a true synergistic effect: GH release was greater than the arithmetic sum of each compound given alone.
Arvat E, Di Vito L, Gianotti L, Ramunni J, Boghen MF, Deghenghi R, Camanni F, Ghigo E
1996
Healthy elderly subjects were given hexarelin through the nose, 1.25 mg three times daily for 8 days, or by mouth, 20 mg three times daily for 15 days. They kept their GH response to the peptide. IGF-I and IGFBP-3 (a carrier protein for IGF-I) rose slightly and neither treatment caused any side effect. On-and-off dosing did not cause the somatotrope (GH-making cell) response to desensitize.
Ghigo E, Arvat E, Gianotti L, Grottoli S, Rizzi G, Ceda GP, Boghen MF, Deghenghi R, Camanni F