Hexarelin dosing & administration

McDonald H, Peart J, Kurniawan ND, et al. · 2020

This study showed Hexarelin significantly improved heart function after simulated heart attack conditions. Treated mice had less heart scarring, lower inflammation markers, and better cardiac output—suggesting Hexarelin protects the heart through anti-inflammatory pathways involving the autonomic nervous system.

Huang Z, Lu X, Huang L, et al. · 2021

Hexarelin increased pulsatile (natural-rhythm) GH secretion in obese mice, leading to reduced visceral fat, less liver fat accumulation, and improved insulin sensitivity—all without changing IGF-1 levels. This suggests Hexarelin helps with metabolic health through direct GH effects.

Huang J, Li Y, Zhang J, 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, activated by binding to the GHSR-1a receptor on heart cells. The heart-protective effects were even slightly better than ghrelin.

Zambelli V, Rizzi L, Delvecchio P, et al. · 2021

Beyond heart benefits, Hexarelin showed anti-inflammatory effects in the lungs. It improved lung function, reduced immune cell infiltration, and prevented the scarring (fibrosis) that can occur after lung injury—showing its protective effects extend beyond the heart.

Mao Y, Tokudome T, Kishimoto I · 2014

This comprehensive review established that Hexarelin has direct cardiovascular effects through two different receptors: GHSR-1a and CD36. The CD36 pathway appears especially important for heart protection, making Hexarelin unique among GH secretagogues for cardiovascular support.

Ghigo E, Arvat E, Gianotti L, Imbimbo BP, Lenaerts V, Deghenghi R, Camanni F · 1994

In 12 healthy young volunteers, hexarelin stimulated GH release at 1-2 mcg/kg IV (2 mcg/kg maximally effective) and 1.5-3 mcg/kg subcutaneously, as well as intranasal (20 mcg/kg) and oral (20-40 mg) routes.

Ghigo E, Arvat E, Muccioli G, Camanni F · 1997

Review of the GHRP class in animals and humans: the GH-releasing effect is synergistic with GHRH, undergoes partial desensitization (more during continuous infusion, less during intermittent administration), and is blunted by inhibitory influences including glucose, free fatty acids, neurotransmitters and glucocorticoids.

Arvat E, Di Vito L, Gianotti L, Ramunni J, Boghen MF, Deghenghi R, Camanni F, Ghigo E · 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), and hexarelin combined with GHRH produced a true synergistic effect, with GH release greater than the arithmetic sum of each compound given alone.

Ghigo E, Arvat E, Gianotti L, Grottoli S, Rizzi G, Ceda GP, Boghen MF, Deghenghi R, Camanni F · 1996

Healthy elderly subjects given intranasal hexarelin 1.25 mg three times daily for 8 days, or oral hexarelin 20 mg three times daily for 15 days, maintained their GH response to the peptide; IGF-I and IGFBP-3 rose slightly and neither treatment induced any side effect. Intermittent administration did not desensitize the somatotrope response.

Bisi G, Podio V, Valetto MR, Broglio F, Bertuccio G, Del Rio G, Arvat E, Boghen MF, Deghenghi R, Muccioli G, Ong H, Ghigo E · 1999

In seven male volunteers studied by radionuclide angiocardiography, IV hexarelin raised left ventricular ejection fraction (70.7 vs 64.0%), rising at 15 min, peaking at 30 min and lasting to 60 min, with no change in mean blood pressure or heart rate. Equivalent GH exposure from rhGH did not do this, indicating a GH-independent positive inotropic effect.

Broglio F, Benso A, Valetto MR, Gottero C, Quaranta L, Podio V, Arvat E, Bobbio M, Bisi G, Ghigo E · 2001

Acute 2.0 mcg/kg IV hexarelin increased left ventricular ejection fraction in seven normal adults and in seven severely GH-deficient patients without changing blood pressure or heart rate, indicating a GH-independent positive inotropic effect mediated by myocardial GHRP receptors.

Deghenghi R, Cananzi MM, Torsello A, Battisti C, Muller EE, Locatelli V · 1994

The paper that introduced hexarelin, His-D-2Me-Trp-Ala-Trp-D-Phe-Lys-NH2, a GHRP analogue in which Trp was substituted with the chemically more stable 2-methyl-Trp. Given subcutaneously it elicited long-lasting GH release and was slightly more effective than GHRP-6.

Falls HD, Dayton BD, Fry DG, Ogiela CA, Schaefer VG, Brodjian S, Reilly RM, Collins CA, Kaszubska W · 2006

In pituitary cells expressing endogenous GHS-R, hexarelin produced a dose-dependent rise in intracellular calcium (EC50 1.7 nM). The receptor signals through the Gq/phospholipase C pathway, with calcium first released from intracellular stores and then sustained by influx of extracellular calcium; phosphatidylinositol hydrolysis was used to measure the signal.

Bresciani E, Pitsikas N, Tamiazzo L, Luoni M, Bulgarelli I, Cocchi D, Locatelli V, Torsello A · 2008

Hexarelin, acting at the GHS-R1a receptor that ghrelin also binds, stimulated food consumption maximally at 80 mcg/kg subcutaneously and maintained a significant orexigenic action throughout 8 weeks of once-daily treatment in both young and old rats, without changing body weight gain.

Feldt-Rasmussen U, Wilton P, Jonsson P · 2004

In the KIMS database of hypopituitary adults on GH replacement, the fluid retention-related adverse events recorded were headache, oedema and arthralgia; these were more frequent in patients under 65 than in older patients.

Massoud AF, Hindmarsh PC, Brook CG · 1996

In healthy adult males, IV hexarelin released GH dose-dependently with an ED50 of 0.48 mcg/kg and a plateau at 1.0 mcg/kg. Low-dose hexarelin (0.125 mcg/kg) co-administered with GHRH-(1-29)-NH2 produced massive GH release, far above either alone, with only a moderate prolactin rise and no cortisol rise.

Frieboes RM, Antonijevic IA, Held K, et al. · 2004

States that hexarelin is superior to GHRH and GHRP-6 in stimulating growth hormone release. In adult male patients with growth hormone deficiency, hexarelin altered EEG sleep against placebo, with a decrease in slow-wave sleep.