Growth Hormone
Not Approved
Growth Hormone Secretagogue

Hexarelin

Hexapeptide Growth Hormone-Releasing Peptide

Hexarelin, a synthetic hexapeptide growth hormone-releasing peptide, represents one of the most potent growth hormone secretagogues available for research purposes. This investigational compound works by binding to growth hormone secretagogue receptors (GHSR) in the pituitary gland, mimicking the action of ghrelin but with significantly enhanced potency and selectivity. Unlike many other growth hormone-releasing peptides, Hexarelin maintains its effectiveness even with repeated administration and can stimulate GH release in the presence of somatostatin, making it particularly valuable for research into growth hormone deficiency, muscle wasting conditions, and age-related hormonal decline. While not FDA-approved for therapeutic use, Hexarelin has garnered significant attention in the research community for its potential applications in studying muscle growth, fat loss, bone density, and cardiovascular health, positioning it as a crucial tool for advancing our understanding of growth hormone physiology and its therapeutic potential.

Reviewed by PeptideGuide Research TeamLast updated February 15, 2026

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Molecular structure diagram of Hexarelin showing hexapeptide sequence
Dosage
1-2 mg per day
Half-life
55-70 minutes
Route
Subcutaneous Injection
Cycle
4-12 weeks
Safety
Use With Caution

Mechanism of Action

Hexarelin operates through a sophisticated mechanism that targets the growth hormone secretagogue receptor (GHSR), also known as the ghrelin receptor, located primarily in the anterior pituitary gland and hypothalamus. As a synthetic hexapeptide, Hexarelin mimics the action of ghrelin, the body's natural 'hunger hormone,' but with significantly enhanced potency and selectivity for growth hormone release. Upon administration, Hexarelin binds to GHSR with high affinity, triggering a cascade of intracellular signaling events that culminate in the release of growth hormone from somatotroph cells in the anterior pituitary. This mechanism bypasses the natural growth hormone-releasing hormone (GHRH) pathway, providing an alternative route for GH stimulation. The peptide's unique structure allows it to resist degradation by peptidases, resulting in a longer half-life compared to endogenous ghrelin. Additionally, Hexarelin demonstrates the ability to stimulate growth hormone release even in the presence of somatostatin, the natural GH inhibitor, making it particularly effective in situations where normal GH regulation is compromised. The compound also exhibits some selectivity for growth hormone release over other pituitary hormones, though it can influence prolactin and ACTH levels to a lesser degree. This targeted mechanism makes Hexarelin a potent tool for research into growth hormone physiology and potential therapeutic applications in conditions characterized by GH deficiency or muscle wasting disorders.

Potential Benefits

Hexarelin's primary benefits stem from its potent ability to stimulate endogenous growth hormone production, which cascades into numerous physiological improvements. Research has demonstrated that Hexarelin can significantly increase lean muscle mass and reduce body fat composition through enhanced protein synthesis and lipolysis. The peptide's growth hormone-releasing properties contribute to improved bone density, enhanced wound healing, and better sleep quality, as growth hormone plays crucial roles in tissue repair and regeneration during rest periods. Studies have also indicated potential cardiovascular benefits, including improved cardiac function and protection against ischemia-reperfusion injury, though these effects require further clinical validation. Beyond its growth hormone-stimulating properties, Hexarelin has shown promise in addressing age-related decline in GH production, which naturally decreases by approximately 14% per decade after age 30. This makes it particularly relevant for research into age-related muscle wasting (sarcopenia) and metabolic dysfunction. The peptide's ability to maintain effectiveness even with repeated administration, unlike some other growth hormone secretagogues that show desensitization, adds to its research value. Additionally, preliminary studies suggest Hexarelin may have neuroprotective properties and could influence cognitive function, though these areas require extensive further investigation to establish clinical relevance.

Common Use Cases

Growth Hormone Deficiency
Muscle Wasting
Bodybuilding
Anti-aging therapies

Dosage & Administration

Research protocols for Hexarelin typically follow a structured approach based on body weight and study objectives. Most studies employ doses of 1-2 mcg per kilogram of body weight, administered subcutaneously 1-3 times daily. For practical application, this means a 70kg individual would receive approximately 70-140 mcg per dose. The peptide is usually supplied as a lyophilized powder requiring reconstitution with bacteriostatic water at a typical concentration of 2mg per vial. Timing is crucial in research protocols, with many studies administering doses on an empty stomach, either upon waking, before meals, or before bedtime to align with natural growth hormone rhythms. A common research protocol involves a 4-6 week cycle followed by a 2-4 week rest period to assess effects and prevent potential receptor desensitization. Some studies have explored higher doses up to 200-300 mcg, though these may increase side effect risks without proportional benefits. Injection site rotation is important to prevent tissue irritation, with common sites including the abdomen, thigh, and upper arm. Proper storage is essential, with reconstituted solutions typically stable for 2-4 weeks when refrigerated. Research protocols emphasize the importance of consistent timing and dosing to maintain stable hormone levels and accurate data collection. It's crucial to note that these are research parameters and should not be interpreted as therapeutic recommendations.

Safety Information

Common Side Effects

Injection site reactions
Increased appetite
Joint pain

Contraindications

Pregnancy
Breastfeeding
Active cancer

Drug Interactions

Corticosteroids, Insulin, Antidiabetic medications

Long-Term Safety

Long-term use of Hexarelin may lead to desensitization of the growth hormone secretagogue receptor, reducing effectiveness over time.

Research & Clinical Evidence

Clinical research on Hexarelin has primarily focused on its growth hormone-releasing properties and potential therapeutic applications, though human studies remain limited. Early phase I and II trials demonstrated that Hexarelin effectively stimulates growth hormone release in both healthy individuals and those with growth hormone deficiency, with peak GH levels occurring 15-60 minutes post-administration. A notable study by Ghigo et al. (1994) showed that Hexarelin produced more potent GH release compared to GHRH in both young and elderly subjects, maintaining effectiveness even with repeated dosing over several weeks. Research by Arvat et al. (1995) demonstrated that Hexarelin could stimulate GH release even in the presence of somatostatin, highlighting its unique mechanism of action. Cardiovascular research has shown promising results, with studies by Tivesten et al. (2000) indicating potential cardioprotective effects in animal models of ischemia-reperfusion injury. However, long-term safety data remains limited, with some studies noting potential effects on cortisol and prolactin levels. A significant limitation in current research is the lack of large-scale, long-term human clinical trials, with most studies involving small cohorts and short duration protocols. The compound's research status means that while preliminary data is encouraging, comprehensive safety and efficacy profiles have not been established through rigorous clinical trial processes required for therapeutic approval.

Frequently Asked Questions

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Synergistic With

Categories

Growth Hormone
Anti-Aging
Metabolic