Hexarelin

What Is Hexarelin?

Hexarelin, also known as Examorelin, is a synthetic analog of ghrelin and a growth hormone-releasing peptide. It is chemically similar to GHRP-6, distinguished by only two additional methyl groups. Hexarelin is highly selective and demonstrates activity after both oral and subcutaneous administration. Research on Hexarelin has heavily focused on its potential to enhance heart cell survival following nutrient deprivation and ischemia.

Hexarelin Structure

• Chemical Formula: His-D-2-Methyl-Trp-Ala-Trp-D-Phe-Lys-NH2

Hexarelin Effects

1. Protects the Heart

Hexarelin exerts a direct protective effect on the heart by engaging the CD36 receptor and the growth hormone secretagogue receptor (GHSR). Studies in rats suggest Hexarelin shields cardiac cells by limiting remodeling (a common issue in heart failure) and preventing apoptosis (programmed cell death).

In mice models, Hexarelin treatment resulted in improved heart function, increased heart cell survival, and reduced levels of malondialdehyde (a marker of cell death). Research on the analog GHRP-6 found that it reduces oxidative stress in heart failure and prevents myocardial remodeling. This mechanism is thought to involve the regulation of phosphatase and tensin homologue (PTEN) activity and the down-regulation of protein kinase B (Akt), both of which are critical for cell regeneration and survival, respectively.

GHRP-6's ability to reduce cardiac remodeling is potent enough to shift the balance of nervous system activity from sympathetic control (high heart rate, blood pressure) toward parasympathetic dominance. This shift improves immediate health outcomes and can decrease the need for long-term intervention. Studies also suggest GHRP-6 helps prevent cardiac remodeling secondary to surgical stress, showing a 40% reduction in scar size.

Hexarelin's cardioprotective mechanism is versatile and not limited to heart muscle or calcium homeostasis-related heart failure, suggesting it can protect the heart from various other insults. For example, research in diabetic rat models showed Hexarelin improved cardiac function related to the processing of sodium and potassium by heart muscle cells.

2. Improves Fat Measures

Dyslipidemia (abnormal blood fat levels) is a risk factor for diabetes. Research in rats indicates that the related peptide, GHRP-6, can reverse insulin resistance and improve lipid profiles, resulting in lower blood fats, reduced blood sugar, and diminished insulin resistance. This suggests a potential role for the peptide in ameliorating severe dyslipidemia.

3. Protects Muscle

Hexarelin also provides protection to skeletal muscle. Studies using rat models of cachexia (severe muscle wasting due to illness or chemotherapy) indicate that Hexarelin can protect muscle cells by regulating calcium flow and addressing mitochondrial dysfunction. Mitochondrial dysfunction depletes cellular energy, leading to cell death. Given that chemotherapy often disrupts calcium regulation—a main cause of muscle breakdown—research suggests that GHRP-6 can offset the alterations in calcium regulation and mitochondria responsible for this muscle destruction.

Hexarelin Heavily Researched

Cardiovascular disease is the leading cause of death in developed nations. Research utilizing peptides like Hexarelin is helping scientists uncover novel mechanisms of heart function in health and disease. This has opened the door to new treatments for challenging problems such as cardiac remodeling and heart failure. Hexarelin demonstrates moderate adverse effects, low oral, and excellent subcutaneous bioavailability in mice. Dosage per kilogram in mice does not translate to humans. Hexarelin for human application remains restricted to educational and scientific research only, not for human consumption.

Article Author

The referenced literature underwent research, compilation, and organization by Dr. Logan, M.D. Dr. Logan possesses a doctorate qualification from Case Western Reserve University School of Medicine alongside a B.S. in molecular biology.

Scientific Journal Author

Anne Moulin's research has been affiliated with the French National Centre for Scientific Research (CNRS). She is skilled in synthetic organic chemistry, peptide development, management, external manufacturing operations, quality control, regulatory control, drug delivery, and drug discovery. She has published multiple scholarly articles and studies. Anne Moulin is referenced as one of the leading scientists involved in the research and development of Hexarelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Peptide Sciences and this doctor. The purpose of citing this doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide. Anne Moulin is listed in [12] under the referenced citations.

Referenced Citations

J. Huang, Y. Li, J. Zhang, Y. Liu, and G. Lu, "The Growth Hormone Secretagogue Hexarelin Protects Rat Cardiomyocytes From in vivo Ischemia/Reperfusion Injury Through Interleukin-1 Signaling Pathway," Int. Heart J., vol. 58, no. 2, pp. 257–263, Apr. 2017. Y. Mao et al., "Hexarelin treatment in male ghrelin knockout mice after myocardial infarction," Endocrinology, vol. 154, no. 10, pp. 3847–3854, Oct. 2013. E. Aglio et al., "Modulation of PTEN by hexarelin attenuates coronary artery ligation induced heart failure in rats," Turk. J. Med. Sci., vol. 49, no. 3, May 2019. H. McDonald et al., "Hexarelin treatment preserves myocardial function and reduces cardiac fibrosis in a mouse model of acute myocardial infarction," Physiol. Rep., vol. 6, no. 9, p. e13699, 2018. X. Xu et al., "Chronic administration of hexarelin attenuates cardiac fibrosis in the spontaneously hypertensive rat," Am. J. Physiol. Heart Circ. Physiol., vol. 303, no. 6, pp. H703-711, Sep. 2012. X. Zhang, L. Qu, L. Chen, and C. Chen, "Improvement of cardiomyocyte function by in vivo hexarelin treatment in streptozotocin-induced diabetic rats," Physiol. Rep., vol. 6, no. 4, 2018. Y. Mao, T. Tokudome, I. Kishimoto, K. Otani, M. Miyazato, and K. Kangawa, "One dose of oral hexarelin protects chronic cardiac function after myocardial infarction," Peptides, vol. 56, pp. 156–162, Jun. 2014. Y. Ma, L. Zhang, J. N. Edwards, B. S. Launikonis, and C. Chen, "Growth hormone secretagogues protect mouse cardiomyocytes from in vitro ischemia/reperfusion injury through regulation of intracellular calcium," PloS One, vol. 7, no. 4, p. e35265, 2012. R. Muset et al., "Hexarelin, a Growth Hormone Secretagogue, Improves Lipid Metabolic Alterations in Nonobese Insulin Resistant Male MICK Mice," Endocrinology, vol. 159, no. 10, pp. 3174–3187, 01 2017. G. Singer et al., "Growth hormone secretagogues hexarelin and JMV2894 protect skeletal muscle from mitochondrial damages in a rat model of cisplatin-induced cachexia," Sci. Rep., vol. 7, 06 2017. E. Conte et al., "Growth hormone secretagogues prevent dysregulation of skeletal muscle calcium homeostasis in a rat model of cisplatin-induced cachexia," J. Cachexia Sarcopenia Muscle, vol. 8, no. 3, pp. 386–404, Jun. 2017. Torsello, Antonio & Bresciani, Elena & Tarrazzo, Laura & Bulgarelli, Ilaria & Caprioli, Simona & Moulin, Aline & Fehrentz, Jean-alain & Martinez, Jean & Deghenghi, David & Locatelli, Vittorio. (2008). Novel hexarelin analogs stimulate the secretion of peptide ligands of ghrelin receptor - characterization of endocrine and extraendocrine effects.