Ipamorelin Peptide: Dosage, Benefits, Side Effects
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What Is Hexarelin Peptide?
What Is Hexarelin Peptide?
What Is Hexarelin Peptide?
Hexarelin is a synthetic growth hormone secretagogue that mimics the action of ghrelin, a natural peptide hormone involved in appetite regulation and growth hormone release. The compound was first synthesized in the 1990s by researchers seeking potent stimulators of growth hormone secretion for therapeutic applications. Hexarelin has a hexapeptide structure (hence “hex”-) with a sequence that optimizes binding to the growth hormone secretagogue receptor (GHSR). Once bound, it triggers intracellular signaling pathways that culminate in the release of growth hormone from the pituitary gland.
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What is Hexarelin Peptide?
Hexarelin belongs to the class of peptides known as growth hormone secretagogues. Its chemical name is 2-1-(D-Phe)-3-(D-Leu)-5-(N-α-Boc-Lys)-4-(S)-2,6-dimethylpiperidinyl-2-propoxycarbonyl-4-hydroxy-hexanamide. The peptide’s structure allows it to bind with high affinity to GHSR-1a receptors located throughout the body, especially in the pituitary and cardiac tissues.
Key features:
Potency – Hexarelin is among the most potent GH secretagogues discovered, producing significant increases in circulating growth hormone levels at low doses.
Selectivity – It shows a strong preference for GHSR-1a over other receptor subtypes, reducing off-target effects.
Stability – The peptide’s design confers resistance to enzymatic degradation, giving it a relatively long duration of action.
Because of these properties, hexarelin has attracted interest as both a research tool and a potential therapeutic agent for conditions related to growth hormone deficiency or tissue repair.
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Hexarelin half-life
The plasma half-life of hexarelin is approximately 30–60 minutes when administered intravenously. Oral administration leads to rapid degradation by gastrointestinal enzymes, so parenteral routes (intramuscular or subcutaneous) are preferred for clinical and research use. The relatively short half-life necessitates multiple daily injections or the development of sustained-release formulations for long-term therapy.
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What does hexarelin do?
Hexarelin’s biological effects stem largely from its stimulation of growth hormone release, but it also exerts direct actions on cardiac and other tissues. Below are key physiological responses:
Inotropic effect
In heart muscle cells (cardiomyocytes), hexarelin activates GHSR-mediated signaling cascades that increase intracellular calcium levels. This enhances contractile force, producing a positive inotropic effect. Studies in animal models have shown improved cardiac output and ejection fraction after hexarelin treatment.
Inhibition of apoptosis
Hexarelin can reduce programmed cell death in various tissues. By upregulating anti-apoptotic proteins (such as Bcl-2) and downregulating pro-apoptotic factors, the peptide protects cells from oxidative or ischemic stress. This property is particularly valuable in neuroprotection and cardioprotection research.
Reduce Ischemia-reperfusion injury
During episodes of blood flow restoration after an ischemic event (e.g., heart attack), tissue damage can be exacerbated by reactive oxygen species. Hexarelin has been shown to attenuate this reperfusion injury, likely through its anti-apoptotic and antioxidant actions, leading to better preservation of myocardial tissue.
Inhibit cardiac fibrosis
Chronic cardiac remodeling often involves fibrotic deposition that stiffens the heart wall. Hexarelin interferes with fibroblast activation and collagen synthesis pathways, thereby limiting fibrosis in experimental models of heart failure or hypertrophy.
Reduce Atherosclerosis
In vascular studies, hexarelin reduces endothelial dysfunction and lipid accumulation within arterial walls. By modulating inflammatory cytokines and improving nitric oxide availability, the peptide slows atherogenic processes, offering potential cardiovascular protective benefits.
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Hexarelin vs Ipamorelin
Potency – Hexarelin induces higher peak growth hormone levels than ipamorelin at comparable doses.
Selectivity – Both peptides target GHSR-1a; however, ipamorelin has a slightly cleaner side-effect profile with minimal impact on cortisol or prolactin.
Clinical use – Ipamorelin is favored for its lower risk of appetite stimulation and is often used in anti-aging protocols. Hexarelin remains primarily a research tool due to its broader systemic effects.
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Hexarelin vs tesamorelin
Tesamorelin, another GHSR agonist, is approved for treating HIV-associated lipodystrophy. Compared with hexarelin:
Duration – Tesamorelin has a longer half-life (~3 hours), allowing once-daily dosing.
Side effects – Tesamorelin’s side effect profile includes edema and arthralgia; hexarelin may provoke more pronounced increases in GH but less systemic fluid retention.
Regulatory status – Hexarelin is not approved for clinical use, whereas tesamorelin has FDA approval.
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Hexarelin vs Sermorelin
Sermorelin is a growth hormone-releasing hormone (GHRH) analogue that stimulates endogenous GH secretion indirectly. Differences:
Mechanism – Sermorelin works via GHRH receptors; hexarelin directly targets GHSR.
Efficacy – Hexarelin typically produces larger GH surges, but sermorelin’s action is more physiological and may be preferable for long-term therapy.
Side effects – Hexarelin can increase appetite, while sermorelin rarely affects hunger.
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Hexarelin vs CJC 1295
CJC 1295 is a GHRH analogue with an extended half-life due to a PEGylated linker. Compared to hexarelin:
Longevity – CJC 1295 provides sustained GH release for up to 24 hours; hexarelin requires multiple daily injections.
Cardiac effects – Hexarelin shows more pronounced direct cardiac actions, whereas CJC 1295’s benefits are largely mediated by GH.
Clinical application – CJC 1295 is used in research on muscle wasting and metabolic disorders; hexarelin remains experimental.
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Hexarelin vs MK 677
MK 677 (ibutamoren) is a non-peptide ghrelin mimetic that binds GHSR and also acts as an oral GH secretagogue. Key distinctions:
Route – MK 677 is orally active; hexarelin must be injected.
Pharmacokinetics – MK 677 has a longer half-life (~24 hours), allowing once-daily dosing.
Side effects – MK 677 can cause increased appetite and water retention; hexarelin’s side effects are similar but may include transient tachycardia.
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Hexarelin vs GHRP-2
GHRP-2 is a growth hormone releasing peptide that also targets GHSR. Comparisons:
Potency – Hexarelin generally elicits stronger GH responses.
Cardiac influence – Both peptides have inotropic effects, but hexarelin’s effect on cardiac remodeling appears more robust.
- Clinical status – Neither is approved for medical use; both are mainly used in research settings.
What is hexarelin used for?
Although not yet clinically licensed, hexarelin has shown promise in several therapeutic areas. Research highlights include:
Preserve cardiac morphology and function
In animal models of heart failure or myocardial infarction, hexarelin administration preserved left ventricular wall thickness, improved ejection fraction, and reduced scar tissue formation.
Reduce bone loss
Hexarelin stimulates osteoblast activity while inhibiting osteoclast-mediated resorption. In osteoporosis studies, treatment maintained bone mineral density and increased trabecular thickness in mice.
Alleviate apoptosis
By modulating apoptotic pathways, hexarelin protects neurons from excitotoxic damage in models of neurodegenerative disease and mitigates cardiomyocyte loss after ischemic injury. This suggests potential applications in stroke prevention and cardiac rehabilitation protocols.
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Hexarelin remains an exciting but experimental peptide with diverse biological effects centered around growth hormone secretion and tissue protection. Ongoing research will determine whether its promising preclinical profile can translate into safe, effective therapies for human disease.
