Hexarelin is a synthetic GHRP with the potential to provide cardioprotection in test subjects. This peptide may be utilized in a lab setting to explore the roles of ghrelin, which requires acylation to bind to GHS-R1a and consists of twenty-eight (28) amino acids. Hexarelin gets part of its name from hexapeptide as the peptide is made of 6 amino acids. The other part of its name is derived synthetic analog of ghrelin. Hexa(six) and (gh)relin, hexarelin.
Autophagy management is considered a contributor to cardioprotection. One study investigated the function of potential governing mechanisms and autophagy, and suggested that heart muscle cells’ hypertrophy, cell death, and oxidative stress were all inhibited by Hexarelin treatment. Hexarelin peptide appeared to manage the upward autophagy signalling by slowing the mTOR phosphorylation. Researchers of this study proposed that Hexarelin may reduce hypertrophy of heart muscle cells and cell death.
Hexarelin is used primarily to stimulate the pituitary gland, causing the production of growth hormones. Similar to its growth hormone-releasing peptide counterparts, it may act to inhibit somatostatin functions while elevating GH levels by magnifying the GHRH signal transduction pathway.
Hexarelin Peptide Structure, Weight
Hexarelin has a molecular structure of C47H58N12O6 and a molecular weight of 887 grams per mole. Its sequence is His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2, and it has a chemical abstract service (CAS) registry of 140703-51-1. 
Hexarelin Mechanism of Action
Hexarelin appears to function using receptors at both the hypothalamic and pituitary levels to potentially promote GH discharge in non-human test subjects. Researchers hypothesize that the release of growth hormone using PKC signaling is affected by Hexarelin. It may copy the ghrelin function by attaching to GHS-R1a. It also attaches to and fires up the cardiac receptors.
Hexarelin appears to enact adrenocorticotropin and prolactin cortisol-releasing activity, similar to other growth hormone releasing peptides. Thyroid-stimulating hormone, luteinizing hormone, IGF-1, follicle-stimulating hormone, and plasma glucose are all reportedly unaffected by the administration of Hexarelin.
Hexarelin and Other GHRPs
Upon data examination, Hexarelin appears to contain unique aspects absent in other GHRPs. On a microgram to microgram level comparison, Hexarelin has been reported to exceed the other GH releasing peptides in performance in a lab setting. Though it requires further scientific investigate, initial studies report an increased, accelerated desensitization rate as opposed to other research peptides, but the rate and extent of this are still being studied.
Hexarelin has presented the potential use for joint restoration, protection, and healing, neural protection, muscle fiber size increase, and enhanced strength when administered on non-human lab subjects. The peptide is also thought to decrease overall fatty tissue, which helps the subjects lose fat. Any form of growth is solely a result of the rise in hormone levels; gastric draining does not appear to be accelerated, and appetite is not stimulated.
Hexarelin Peptide Research
Researchers generally cease Hexarelin administration within 2 weeks of initial administration on test subjects. Doing otherwise may lead to an insignificant rise in GH because of the increased desensitization. A study opposing this practice was conducted. The experiment was performed on non-human test subjects to examine Hexarelin’s desensitization rate in daily administration. The subjects’ blood was drawn four (4) times over sixteen (16) weeks and analyzed. Upon evaluation, the researchers concluded that Hexarelin presented an insignificant difference in desensitization after the first and fourth week of administration.
Non-human subjects that were administered Hexarelin presented muscle size increases resulting from new myocytogenesis. A number of subjects were reported to exhibit more youthful appearances. Hexarelin also displayed accelerated injury recovery and, in some cases, was observed to have benefited the heart. Non-human subjects without the ability to generate their own HGH naturally, were administered. The peptide is also researched for its potential to enhance skin elasticity, and has been suggested by researchers to exhibit properties that encompass:
- injury prevention and recovery
- reduction of fat
- muscle building
- skin elasticity
Hexarelin has been suggested to provide a variety of properties, with its most prominent potential actions in fat regulation, cardiac protection, and muscle mass preservation.
Initial research supports Hexarelin’s potential as a CD36 agonist, a protein involved in lipolysis control, and management of fatty acid breakdown. Treating the cultured murine adipose with Hexarelin resulted in CD36 activation, which scientists reported drew out the reduced expression of PEPCK.  Since PEPCK is linked to the breakdown of fatty acids, this implies that this process is regulated by CD36, and is thus activated by this peptide.
Abnormal amounts of fat in the blood are referred to as dyslipidemia. Its impact on human physiology is crucial to fighting the rising health concerns linked to modern diets. Rodent research suggests that growth hormone-releasing peptide 6 (GHRP-6) may inhibit dyslipidemia in an insulin resistance setting while lowering blood sugar and insulin resistance at the same time. Hexarelin could potentially provide an alternative to the lipid medications we currently use to treat severe dyslipidemia.
Hexarelin Research in Cardiovascular Function
Researchers suggest Hexraelin may be linked to positive effects on cardiac tissues, especially in instances of disease or injury. Study results support Hexarelin’s potential ability to relieve lesion formation in rodent atherosclerosis models. Hexarelin appears to affect the heart directly by attaching to the CD36 receptor and the GHSR. Rodent studies suggest that the peptide guards heart cells against injury heart attack settings by attaching to these receptors and inhibiting cells from going through programmed cell death (aka apoptosis). Hexamorelin treated rodents presented a higher number of surviving heart cells, reduced formation of malondialdehyde (an indicator of heart cell death), and better cardiac function.
Another study found that Hexarelin appeared to decrease oxidative stress in cardiac failure and inhibit remodeling of heart muscles from occurring. Remodeling is a process having to do with a decrease in cardiac function and morbidity.  GHRP 6 treated rodents in this study showed major enhancements in heart function. The processes are considered to be arbitrated by Hexarelin/GHRP 6 down regulation of protein kinase B expression and up-regulation of PTEN activity.
Since the mechanism that Hexarelin uses to protect cardiac cells is not particular to the damage mechanism in myocardial infarctions, scientists suppose that Hexarelin may be utilized to protect the heart from further injuries. A study on rodents reported that the peptide appeared to enhance cardiac function in a diabetes model by manipulating the way potassium and calcium are processed by myocardial cells.
Hexarelin Peptide and Muscle Mass
Hexarelin may provoke a rise in calcium influx by activating the GHS-R1a, though it might not have this impact on skeletal muscle. Hexarelin has been reported by researchers to host an ability to improve isolated skeletal muscle contractility of rats in a way that is significantly calcium-independent and dose-dependent.
Rodent studies of cachexia models have suggested that Hexarelin may also protect myocytes by managing calcium flow and mitochondrial dysfunction. Mitochondria are the power plants of cells. Without them, cells can’t generate the energy necessary to perform normal function and will die eventually. Calcium dysregulation is a major reason why lean body mass and muscle mass are impacted during cancer treatment.
Hexarelin Peptide Safety Profile
Researchers report some unintended and adverse affects exhibited in research subjects. Commonly observed side effects with Hexarelin may be due to its impact on prolactin, cortisol, and ACTH. Those effects reported included:
- Low libido
- Tingling or numbness in extremities
- Elevated cortisol levels
- Water retention
- Carpal tunnel-like symptoms
- Elevated prolactin levels
- Excessive sleepiness
- Reduced insulin sensitivity
Researchers can buy Hexarelin and other high quality peptides for research only by visiting Core Peptides. The peptide is available strictly for laboratory and research purposes, and is not available for human use.
- National Center for Biotechnology Information. PubChem Database. Examorelin CID 6918297. 2020.
- Ma Y, et al. Growth hormone secretagogues protect mouse cardiomyocytes from in vitro ischemia/reperfusion injury through regulation of intracellular calcium. PLoS One Journal, 2012.
- Wan Z, et al. FAT/CD36 regulates PEPCK expression in adipose tissue. American journal of physiology. Cell physiology, 2013.
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Dr. Marinov (MD, Ph.D.) is a researcher and chief assistant professor in Preventative Medicine & Public Health. Prior to his professorship, Dr. Marinov practiced preventative, evidence-based medicine with an emphasis on Nutrition and Dietetics. He is widely published in international peer-reviewed scientific journals and specializes in peptide therapy research.