Peptide Hexarelin (also known as Examorelin) is a potent Growth hormone secretagogue (GHS), Ghrelin mimetic and agonist of the Growth hormone secretagogue receptors (GHSR). It is a hexapeptide, which was derived from GHRP-6, with the amino acid sequence His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2, chemical formula C47H58N12O6 and molecular mass 887.04022 g/mol. Hexarelin belongs to the Growth hormone-releasing peptides (GHRPs) family, a group of small synthetic peptides that stimulate the growth hormone secretion by the pituitary gland, and like other Ghrelin mimetics, act through own specific (Ghrelin) receptor – GHSR, independent from GHRHR (Growth-hormone-releasing hormone receptor).
Scientific Studies and Hexarelin results
Hexarelin substantially and dose-dependently increases plasma levels of growth hormone (GH) in both, animals and humans. Hexarelin does not affect plasma levels of glucose, luteinizing hormone (LH), follicle-stimulating hormone (FSH), or thyroid-stimulating hormone (TSH), however similarly to GHRP-2 and GHRP-6 peptides, it slightly and dose-dependently stimulates the release of prolactin, adrenocorticotropic hormone (ACTH), and cortisol in humans.
Hexarelin releases more Growth hormone than does Growth hormone-releasing hormone (GHRH), and produces synergistic effects on GH release in combination with GHRH, resulting in “massive” increases in plasma GH levels even with only low doses of Hexarelin. Also has been shown, that Hexarelin was able to reverse diet-induced catabolism. The stimulatory effect of hexarelin on GH secretion decreases in middle age, but persists in the elderly. A partial and reversible tolerance to the Growth hormone-releasing effects of Hexarelin occurs in humans with long-term administration (50–75% decrease in efficacy over the course of weeks to months).
Hexarelin and cardioprotective activity
Hexarelin has cardioprotective activity in common cardiovascular conditions such as cardiac fibrosis, ischemic heart disease, cardiac dysfunction, and atherosclerosis. These beneficial effects seem to be mediated through the direct binding and activation of its cardiac receptors CD36 (Cluster of differentiation 36) and GHS-R1a (Growth hormone secretagogue receptor transcript 1a). Since Hexarelin is a chemically stable synthetic Growth hormone secretagogue with more potent cardiac effects than its natural analog Ghrelin, it can be a potential alternative to Ghrelin as a promising therapeutic agent for the treatment of cardiovascular diseases.
Initial studies documented cardioprotective effects of the hexapeptide Hexarelin in ischemic reperfusion injury in hearts isolated from hypophysectomized rats. 2-week treatment with Hexarelin and Growth hormone improved stroke volume and decreased total peripheral resistance in rats subjected to experimental myocardial infarction.
In human trials, acute treatment with Hexarelin increased the LV ejection fraction in normal and GH-deficient subjects but not in cases of severe dilated cardiomyopathy. In patients with coronary artery disease undergoing bypass surgery, the acute administration of hexarelin, but not of rGH or GH-releasing hormone, caused a rapid increase in the LV ejection fraction, cardiac index and cardiac output.
Growth hormone-releasing peptides-mediated cardiotropic and cytoprotective effects are superior to those shown by the exogenous administration of GH and are not shared by Growth hormone releasing hormone (GHRH). However, although these studies suggest GH-independent actions of Hexarelin, in some cases, the effects of Hexarelin and exogenous GH were similar and the relationship between hexarelin and serum levels of IGF-1 and GH was not completely defined. However, as current evidence is mainly from experimental animal models or in vitro cell lines, clinical trials aimed to extend the application of Hexarelin in human subjects and observe its efficacy and potential side effects are warranted.
Hexarelin promotes muscle mass growth
Hexarelin promotes muscle mass growth and strength, and when is combined with anabolic steroids, their mutual effects in this direction are synergistically improved. Androgenic hormones Testosterone, Testosterone enanthate, and Ethinylestradiol (though not Oxandrolone), have been found to significantly potentiate the GH-releasing effects of Hexarelin in humans. It is for this reason that Hexarelin is also abused by bodybuilders, weightlifters and strength athletes.
Hexarelin was developed by Mediolanum Farmaceutici. He reached phase II clinical trials for the treatment of Growth hormone deficiency (GHD) and congestive heart failure but did not complete development and was never marketed. The therapeutic potential of hexarelin requires further investigation.
Scientifically investigated possible benefits of Hexarelin
- Has cardioprotective activity and helps in cardiovascular conditions such as cardiac fibrosis, ischemic heart disease, cardiac dysfunction or atherosclerosis
- Increased lean muscle mass, promoting muscle growth, strength and performance
- Supports the recovery of muscle fibers and tissues, it can help in the healing of joints
- Can help strengthen and improve the nervous system
- Anti-aging and rejuvenating effects
- Improved overall regeneration
- Helps increase bone density
- Strong anti-catabolic effect
- Support fat burning
- Cytoprotective effects
Hexarelin possible side-effects
- Skin irritation at the injection site
- Carpal tunnel syndrome
- Increased prolactin levels and gynecomastia risk (stimulates prolactin to a higher degree than other Growth hormone relasing peptides)
- Increased cortisol levels (that may pose issue in the weeks immediately following cessation of Hexarelin therapy)
- Reduced insulin sensitivity
- Water retention
What is Hexarelin?
Hexapeptide Hexarelin belongs to the Growth hormone-releasing peptides (GHRPs) family. It is a potent Growth hormone secretagogue which was derived from GHRP-6.
What does Hexarelin do?
Hexarelin substantially and dose-dependently increases plasma levels of growth hormone (GH) in both, animals and humans. It also has cardioprotective activity in common cardiovascular conditions such as cardiac fibrosis, ischemic heart disease, cardiac dysfunction, and atherosclerosis.
Does Hexarelin promote muscle growth?
Hexarelin promotes muscle mass growth and strength, and when is combined with anabolic androgenic steroids, their mutual effects in this direction are synergistically improved
In the scientific studies and clinical trials performed, the optimal dose of Hexarelin is often reported as 1 mcg per 1 kg body weight 3 times daily.