HEXARELIN (also known as Examorelin) is a synthetic analog of ghrelin and exhibits a high degree of similarity to GHRP-6. The only difference between Hexarelin and GHRP-6 is the inclusion of two methyl groups in the structure of GHRP-6. Like other ghrelin analogs, this peptide remains active both orally and sublingually and displays high selectivity in its mode of action.[1] It has been extensively studied in relation to cardiac cell survival after ischemia and nutrient deprivation.
MOLECULAR FORMULA: C47H58N12O6
MOLECULAR WEIGHT: 887.05 g/mol
SEQUENCE: His-2-Me-D-Trp-Ala-Trp-D-Phe-Lys-NH2
PUBCHEM: CID 6918297
CAS NUMBER: 140703-51-1
RECONSTITUTION: Required
HEXARELIN AND MUSCLE PROTECTION
The peptide has been observed to protect muscle cells and is not useful specifically for the heart alone. Studies in Hexarelin and GHRP-6 observe how the peptides may control calcium flow and mitochondrial dysfunction in muscles of rats suffering from cachexia (extreme weight loss due to illness or chemotherapy).[2] The researchers report that the secretagogue can “protect skeletal muscle from mitochondrial damage and improve lean mass recovery.” It also appears to keep muscle cells viable by maintaining mitochondrial integrity. Through its energy supply, Mitochondria help muscles carry out day-to-day functions. It has been observed that calcium ion regulation is often disturbed due to chemotherapy and is one of the principal causes for altered muscle mass and lean body mass during cancer treatment. However, Hexarelin and GHRP-6 may help to reestablish proper calcium regulation post-chemotherapy.
HEXARELIN AND CARDIAC FUNCTIONS
Hexarelin appears to affect the heart through its association with the CD36 receptor and the growth hormone secretagogue receptor (GHSR). Research conducted on murine models observe that the peptide appears to protect cardiac cells from injury in the backdrop of cardiac arrest.[3] The scientists even note that hexarelin “may be a promising therapeutic agent for some cardiovascular conditions.” Researchers suggest that the peptide interacts with the aforesaid receptors and prevents apoptosis of the cardiac cells. The peptide may help improve cardiac function, increasing the number of surviving cardiac cells and reducing the levels of malondialdehyde (cardiac cell death marker). Interestingly, the study also suggested GHRP-6 to be partially superior in function compared to ghrelin. Hexarelin has also been observed to ameliorate oxidative stress in cardiac cells during cardiac failure as well as to prevent myocardial remodeling in rats.[4] Cardiac remodeling causes a decrease in cardiac function and can be fatal. However, GHRP-6 or Hexarelin treated rats appeared to show significant improvement in their cardiac function compared to the untreated controls. The molecular mechanisms underlying the function of the peptide involve an increase of phosphatase and tension homologue (PTEN) activity and subsequent reduction in protein kinase B levels. While PTEN regulates cellular regeneration, protein kinase B helps to modulate cell survival. GHRP-6 and Hexaralin may mediate cardiac remodeling by switching the nervous system response from sympathetic (includes increased blood pressure, heart rate, etc.) to parasympathetic. This regulation would help to improve short-term health and reduce the need for prolonged cardiac medication. Moreover, when treated with the peptide following cardiac arrest, studies with rat models observed a significant decrease in scar tissue arising from cardiac tissue healing.
The peptide may have the potential for assisting in numerous cardiac damages as its mode of action is not specific to protection against heart attack. Studies in rat models of diabetes have also observed Hexarelin to potentially improve cardiac function by altering the processing of calcium and potassium by cardiac muscle cells.[5]
HEXARELIN AND FAT
Dyslipidemia is the physiological condition of elevated fat levels in the blood. Interestingly, it also happens to be an independent contributing factor for the onset of diabetes, even in lean and externally fit individuals. A detailed understanding of the condition throws light on the association of human physiology with modern diets. GHRP-6 and Hexarelin studies have observed the peptides’ potential to correct dyslipidemia in the backdrop of insulin resistance (the first step in the pathway to diabetes).[6] The peptide may also help to reduce blood sugar and insulin resistance in rats. In future, it may be a potential alternative to the existing lipid medications to treat severe dyslipidemia.
Cardiac disorders are the leading cause of death in most developed countries. Peptides such as Hexarelin have helped scientists explore the complexities of cardiac conditions, which eventually lead to cardiac failure and death. Studies involving the peptide have revealed a number of new pathways for understanding the role of the heart in health and disease.[7] Hexarelin has the potential to be used as a part of novel therapies for addressing serious physiological conditions. These include cardiac remodeling issues, which have been challenging to address in the past. Studies in Hexarelin report the peptide to exhibit moderate side effects, low oral bioavailability, and excellent subcutaneous bioavailability in mice models of research. Per kg dosage in mice does not match up to humans.
