Home Compounds Growth Hormone Axis Hexarelin
Growth Hormone Axis Research Moderate Evidence

Hexarelin

Potent synthetic hexapeptide GH secretagogue — among the most potent GHS-R1a agonists. Studied for cardiac repair beyond GH axis effects via direct CD36 receptor activity. Orphan drug potential for growth hormone deficiency.

GHRPhexapeptideGH releasecardiacCD36secretagoguepotent
Half-life
30–45 minutes; pulsatile dosing required to avoid desensitization
SKUs
2
Evidence
Moderate Evidence

Hexarelin is a synthetic hexapeptide and one of the most potent growth hormone releasing peptides (GHRPs) developed. It activates the ghrelin receptor to stimulate strong GH pulses and has also been studied for direct cardiac protective effects independent of GH. It is not FDA-approved and is used primarily as a research tool.

Growth Hormone Research
Hexarelin produces among the most potent GH responses of the GHRP compounds. Research has used it to study GH axis dynamics, pituitary reserve, and the effects of strong GH stimulation on body composition and IGF-1 levels.
Cardiovascular Research
Notably, hexarelin has been studied for cardiac effects that appear to be independent of its GH-stimulating activity. Research in animal models of heart failure showed protective effects on cardiac function, attributed to direct ghrelin receptor activation in cardiac tissue. Human cardiac studies are limited.
GH Axis Desensitization
An important research finding with hexarelin is that it produces rapid desensitization with repeated daily use — the pituitary becomes less responsive and GH responses diminish. This is different from compounds like ipamorelin and makes intermittent use patterns more relevant for research applications.
  • Very potent GH stimulation compared to other GHRP compounds.
  • Cardiac protective effects in animal heart failure models, likely via direct receptor activation.
  • Documented desensitization with frequent repeated dosing in research subjects.
  • Not FDA-approved; no pharmaceutical development resulted in an approved product.

The rapid desensitization with daily use is an important practical limitation compared to other GH secretagogues. The cardiac research is primarily preclinical and has not been confirmed in large human trials. Like other GHRPs, it also stimulates cortisol and prolactin. Its potency means dosing precision matters more than with weaker compounds.

Hexarelin activates the ghrelin receptor in the pituitary gland, which triggers a burst of GH release. Compared to earlier GHRP compounds, hexarelin produces a larger GH pulse for the same dose. Interestingly, the same receptor also exists in heart muscle cells. When hexarelin activates these cardiac ghrelin receptors, it triggers cell survival and protective signaling in the heart independently of any GH that gets released. This dual action — pituitary GH stimulation and direct cardiac receptor activation — makes hexarelin somewhat unique among the GHRP family. The desensitization that occurs with daily use is thought to result from receptor downregulation in the pituitary, which recovers with a break from dosing.

Not FDA-approved. Cortisol and prolactin are stimulated alongside GH. The cardiac research suggests direct cardiac receptor activity, which could have unknown implications with repeated use in people with cardiac conditions. The rapid pituitary desensitization with daily use affects research protocols significantly. Standard GH-related safety considerations apply.

Moderate Evidence

This compound has been studied in Phase 1 or Phase 2 human trials. Evidence is encouraging but more large-scale trials are needed.

Published Research Ranges
1–2mcg/kg per injection; 200mcg maximum typical dose in research; cycling recommended
Research Context Only: These are ranges reported in published scientific studies for educational reference. They are not dosing recommendations. This is not medical advice. Always consult a qualified healthcare professional.

Sources listed here are from the platform research library. All links open the original publication. No citations are generated by AI.

Hexarelin, a GH-Releasing Peptide, and Cardioprotection: Receptor Involvement
Cardiovascular Research • 2005  • DOI: 10.1016/j.cardiores.2005.06.025
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Hexarelin Stimulates GH Release and Displays Cardiac-Specific Effects Independent of GH
Journal of Clinical Endocrinology & Metabolism • 1999  • DOI: 10.1210/jcem.84.2.5468
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Hexarelin Reduces Cardiac Ischemia-Reperfusion Injury via CD36
Endocrinology • 2004  • DOI: 10.1210/en.2003-1430
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Sex steroids, GHRH, somatostatin, IGF-I, and IGFBP-1 modulate ghrelin's dose-dependent drive of pulsatile GH secretion in healthy older men
 • 2012  • DOI: 10.1210/jc.2012-2567
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Acute cardiovascular and hormonal effects of GH and hexarelin, a synthetic GH-releasing peptide, in humans
 • 1999  • DOI: 10.1007/bf03343555
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Hexarelin induced growth hormone release is influenced by exogenous growth hormone
 • 1995  • DOI: 10.1111/j.1365-2265.1995.tb02927.x
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Hexarelin decreases slow-wave sleep and stimulates the secretion of GH, ACTH, cortisol and prolactin during sleep in healthy volunteers
 • 2004  • DOI: 10.1016/s0306-4530(03)00152-5
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Cardiac effects of hexarelin in hypopituitary adults
 • 1999  • DOI: 10.1016/s0014-2999(99)00537-3
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Lipid oxidation in pathophysiology of atherosclerosis: Current understanding and therapeutic strategies
 • 2022  • DOI: 10.1016/j.ijcrp.2022.200143
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Targeting the Ghrelin Receptor as a Novel Therapeutic Option for Epilepsy
 • 2021  • DOI: 10.3390/biomedicines10010053
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Danger-Sensing/Patten Recognition Receptors and Neuroinflammation in Alzheimer's Disease
 • 2020  • DOI: 10.3390/ijms21239036
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Acylated Ghrelin as a Multi-Targeted Therapy for Alzheimer's and Parkinson's Disease
 • 2020  • DOI: 10.3389/fnins.2020.614828
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Targeting GPCRs Against Cardiotoxicity Induced by Anticancer Treatments
 • 2019  • DOI: 10.3389/fcvm.2019.00194
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Dynamic role of the transmembrane glycoprotein CD36 (SR-B2) in cellular fatty acid uptake and utilization
 • 2018  • DOI: 10.1194/jlr.r082933
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Skeletal muscle wasting in chronic heart failure
 • 2018  • DOI: 10.1002/ehf2.12387
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Muscle wasting and sarcopenia in heart failure and beyond: update 2017
 • 2017  • DOI: 10.1002/ehf2.12237
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Cell Death in the Developing Brain after Hypoxia-Ischemia
 • 2017  • DOI: 10.3389/fncel.2017.00248
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Intended or Unintended Doping? A Review of the Presence of Doping Substances in Dietary Supplements Used in Sports
 • 2017  • DOI: 10.3390/nu9101093
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Synthetic Growth Hormone-Releasing Peptides (GHRPs): A Historical Appraisal of the Evidences Supporting Their Cytoprotective Effects
 • 2017  • DOI: 10.1177/1179546817694558
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Antifibrotic activity of acylated and unacylated ghrelin
 • 2015  • DOI: 10.1155/2015/385682
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CD36, a scavenger receptor implicated in atherosclerosis
 • 2014  • DOI: 10.1038/emm.2014.38
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Pathophysiogenesis of mesial temporal lobe epilepsy: is prevention of damage antiepileptogenic?
 • 2014  • DOI: 10.2174/0929867320666131119152201
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Neuroactive peptides as putative mediators of antiepileptic ketogenic diets
 • 2014  • DOI: 10.3389/fneur.2014.00063
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Intranasal administration of oxytocin: behavioral and clinical effects, a review
 • 2013  • DOI: 10.1016/j.neubiorev.2013.04.012
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Clinical review: The human experience with ghrelin administration
 • 2013  • DOI: 10.1210/jc.2012-4247
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Adult growth hormone deficiency - benefits, side effects, and risks of growth hormone replacement
 • 2013  • DOI: 10.3389/fendo.2013.00064
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Potential biomarkers of insulin resistance and atherosclerosis in type 2 diabetes mellitus patients with coronary artery disease
 • 2013  • DOI: 10.1155/2013/698567
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Ghrelin and ghrelin receptor modulation of psychostimulant action
 • 2013  • DOI: 10.3389/fnins.2013.00171
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Hormone replacement therapy and physical function in healthy older men. Time to talk hormones?
 • 2012  • DOI: 10.1210/er.2012-1002
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Ghrelin - a pleiotropic hormone secreted from endocrine x/a-like cells of the stomach
 • 2012  • DOI: 10.3389/fnins.2012.00024
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Interleukin-2 Transiently Inhibits Pulsatile Growth Hormone Secretion in Young but not Older Healthy Men
 • 2021  • DOI: 10.1210/clinem/dgab484
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Growth hormone status during long-term hexarelin therapy
 • 1998  • DOI: 10.1210/jcem.83.5.4812
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Effect of ghrelin on mortality and cardiovascular outcomes in experimental rat and mice models of heart failure: a systematic review and meta-analysis
 • 2015  • DOI: 10.1371/journal.pone.0126697
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Cisplatin-Induced Muscle Wasting and Atrophy: Molecular Mechanism and Potential Therapeutic Interventions
 • 2025  • DOI: 10.1002/jcsm.13817
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Ghrelin, Neuroinflammation, Oxidative Stress, and Mood Disorders: What Are the Connections?
 • 2025  • DOI: 10.2174/1570159x22999240722095039
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Once upon a time: the glucagon stimulation test in diagnosing adult GH deficiency
 • 2024  • DOI: 10.1007/s40618-024-02322-5
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Preclinical Ultrasonography in Rodent Models of Neuromuscular Disorders: The State of the Art for Diagnostic and Therapeutic Applications
 • 2023  • DOI: 10.3390/ijms24054976
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The Interplay between Ghrelin and Microglia in Neuroinflammation: Implications for Obesity and Neurodegenerative Diseases
 • 2022  • DOI: 10.3390/ijms232113432
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Effect of Ghrelin on the Cardiovascular System
 • 2022  • DOI: 10.3390/biology11081190
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Toxicological Characterization of GHB as a Performance-Enhancing Drug
 • 2022  • DOI: 10.3389/fpsyt.2022.846983
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Growth Hormone Response to L-Arginine Alone and Combined with Different Doses of Growth Hormone-Releasing Hormone: A Systematic Review and Meta-Analysis
 • 2022  • DOI: 10.1155/2022/8739289
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The molecular signaling of exercise and obesity in the microbiota-gut-brain axis
 • 2022  • DOI: 10.3389/fendo.2022.927170
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Ghrelin-Mediated Regeneration and Plasticity After Nervous System Injury
 • 2021  • DOI: 10.3389/fcell.2021.595914
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We are ageing
 • 2014  • DOI: 10.1155/2014/808307
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CD36 as a therapeutic target for endothelial dysfunction in stroke
 • 2012  • DOI: 10.2174/138161212802002760
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Ghrelin and cardiovascular diseases
 • 2010  • DOI: 10.2174/157340310790231662
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Hexarelin Signaling to PPARgamma in Metabolic Diseases
 • 2008  • DOI: 10.1155/2008/364784
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Ghrelin: a new player in the control of gastrointestinal functions
 • 2005  • DOI: 10.1136/gut.2004.062604
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Growth hormone in obesity
 • 1999  • DOI: 10.1038/sj.ijo.0800807
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GH-independent cardiotropic activities of hexarelin in patients with severe left ventricular dysfunction due to dilated and ischemic cardiomyopathy
 • 2002  • DOI: 10.1016/s1388-9842(01)00223-9
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Growth hormone-releasing hormone attenuates amyloid deposition and neuroinflammation in Alzheimer's disease models
 • 2026  • DOI: 10.1038/s41419-026-08699-w
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Growth Hormone-Releasing Peptide-6 (GHRP-6) Ameliorates Post-Infarct Ventricular Remodeling and Systolic Dysfunction in a Model of Permanent Coronary Ligation
 • 2026  • DOI: 10.3390/ph19030468
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Hexarelin promotes the survival of retinal ganglion cells after optic nerve transection
 • 2026  • DOI: 10.4103/ijp.ijp_176_24
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Ghrelin Receptor Deletion or Pharmacological Inhibition Improves Muscle Function in Aging Male Mice
 • 2026  • DOI: 10.1111/acel.70472
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Lipoprotein(a)/CD36 Interaction Drives IL-6/RhoA-GTP Signaling and miRNA Epigenetic Regulation in Coronary Artery Spasm
 • 2025  • DOI: 10.3390/ph18091384
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Pharmacological targeting of the hyper-inflammatory response to SARS-CoV-2-infected K18-hACE2 mice using a cluster of differentiation 36 receptor modulator
 • 2024  • DOI: 10.3389/fphar.2024.1303342
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Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway
 • 2023  • DOI: 10.1186/s40001-023-01318-w
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Growth hormone secretagogues modulate inflammation and fibrosis in <i>mdx</i> mouse model of Duchenne muscular dystrophy
 • 2023  • DOI: 10.3389/fimmu.2023.1119888
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Physiactisome: A New Nanovesicle Drug Containing Heat Shock Protein 60 for Treating Muscle Wasting and Cachexia
 • 2022  • DOI: 10.3390/cells11091406
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Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity
 • 2021  • DOI: 10.3390/ph14050444
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60 sources · Platform research library · Not generated by AI

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Research Education Only: This profile is for educational purposes only. All information is sourced from published scientific literature. This is not medical advice. Not for human consumption. Consult qualified medical professionals for any health decisions.