Hexarelin, a synthetic peptide that stimulates the release of growth hormone, has gained attention in medical research due to its powerful ability to protect the heart. Originally designed to induce the release of growth hormone (GH), it has additional advantages that go beyond this purpose. There is strong evidence suggesting that it can safeguard the heart, especially during and after ischemic events such as heart attacks. Let’s explore the evidence supporting Hexarelin’s cardioprotective benefits, outlining its action mechanisms, possible clinical uses, and the current research revealing its potential for treatment.

What is Ischemia-Reperfusion Injury?

Ischemic heart disease is a significant contributor to mortality and morbidity on a global scale. Myocardial ischemia occurs when coronary blood flow and oxygen availability are insufficient to meet the requirements of the heart. During acute myocardial infarction (AMI), the blockage of a coronary artery area results in the death of heart muscle cells (myocyte necrosis). 

The implementation of early reperfusion therapies has significantly decreased the number of deaths and illnesses among patients with acute myocardial infarction (AMI). If there is no reperfusion or collateral blood flow, total necrosis will occur. While reperfusion is essential for saving tissue, it can also result in additional issues such as reduced heart contractile function, arrhythmias, and permanent cell damage that can lead to necrosis and apoptosis. 

Growth Hormone Secretagogues (GHS) and Cardioprotection

Growth hormone secretagogues (GHS) are synthetic peptides that stimulate the release of growth hormone by binding to the G-protein coupled receptor (GHS-R). These peptides have been shown to have cardiovascular (CV) effects. Several investigations have shown that the synthetic hexapeptide, hexarelin (HEX), has protective properties against acute myocardial infarction (AMI), ischemia-reperfusion (IR) injury, and cardiac fibrosis. 

Preclinical disease models provide evidence that GHS has an indirect cardioprotective effect by modulating the autonomic nervous system both centrally and peripherally.

How does Hexarelin protects our heart?

Hexarelin exerts its cardioprotective effects by interacting with certain receptors and signaling pathways in the heart, which are closely related to numerous important mechanisms.

 1. CD36 receptor activation
It primarily protects the heart by activating the CD36 receptor. CD36 is a scavenger receptor that is extensively present in different tissues, including the heart. It has a vital function in the metabolism of fatty acids and the response to oxidative stress. It attaches to CD36, initiating a series of defensive signaling pathways, specifically the PI3K/Akt and MAPK pathways, which are crucial in decreasing apoptosis (cell death) and promoting cell survival during ischemia events.

The PI3K/Akt pathway, for example, supports cell viability by blocking pro-apoptotic molecules and increasing the effectiveness of anti-apoptotic proteins such as Bcl-2. Conversely, the MAPK pathway plays a role in cellular reactions to stress and has demonstrated the ability to mitigate inflammation and oxidative damage in the heart. Hexarelin modulates these pathways to alleviate the damage induced by IRI, hence conserving heart function and decreasing the likelihood of long-term problems.

2. Regulation of the Autonomic Nervous System
Hexarelin also affects the autonomic nervous system (ANS), which controls heart rate, blood pressure, and other essential cardiovascular processes. Following a heart attack, there can be a disruption in the equilibrium between the sympathetic and parasympathetic divisions of the autonomic nervous system (ANS), resulting in heightened strain on the heart. It has demonstrated the ability to tilt this equilibrium towards parasympathetic predominance, leading to a decrease in heart rate, decreased inflammation, and overall protection of the heart.

The control of the autonomic nervous system (ANS) is especially crucial in the context of heart failure, since heightened sympathetic activity can worsen the situation. Hexarelin promotes parasympathetic activity, which not only safeguards the heart during acute ischemia episodes but also enhances long-term cardiac health by diminishing chronic stress and inflammation.

Source: https://www.sciencedirect.com/science/article/pii/S0753332220303577

Potential Clinical Applications

Hexarelin has the potential to be used as a cardioprotective drug in a wider range of cardiovascular disorders, as continuing research is investigating its applications beyond its current uses. It’s capacity to diminish inflammation and oxidative stress renders it a potentially valuable therapeutic option for illnesses such as atherosclerosis and hypertension, in which these factors significantly contribute to the advancement of the disease.

Furthermore, Hexarelin’s ability to modulate the autonomic nervous system (ANS) indicates that it may have potential in the treatment of neurocardiogenic disorders, which include a disruption in the interaction between the heart and neurological system. This is due to it’s neuroprotective effects. The utilization of Hexarelin in the treatment of many disorders involving both the cardiovascular and neurological systems presents promising prospects.

In conclusion, Hexarelin is a promising therapeutic drug in the field of cardioprotection because to its capacity to activate protective signaling pathways, regulate the autonomic nervous system, and decrease inflammation. This makes it a viable tool for preventing and treating heart disease. Current evidence indicates that Hexarelin may have a significant impact on enhancing outcomes for patients with cardiovascular diseases. As scientific advancements progress, it has the potential to become a crucial component in the treatment of heart disease. It provides a fresh source of optimism for patients who are at risk of experiencing ischemia episodes and heart failure.

Learn Today… Prescribe Tomorrow!

At MedBridge Global, we see transformation mostly dependent on education. The only committed platform guaranteeing patients and professionals access to the most recent developments in medical science is ours. Whether you are looking for solutions or trying to give the greatest treatment, we lead you toward best health and lifespan. 

Joining our network allows practitioners to access tools, training, and a cooperative community encouraging excellence in patient care and practice success. 

 References

Mao, Y., Tokudome, T., & Kishimoto, I. (2014). The cardiovascular action of hexarelin. Journal of geriatric cardiology: JGC, 11(3), 253. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4178518/

Locatelli, V., Rossoni, G., Schweiger, F., Torsello, A., De Gennaro Colonna, V., Bernareggi, M., … & Berti, F. (1999). Growth hormone-independent cardioprotective effects of hexarelin in the rat. Endocrinology, 140(9), 4024-4031. https://academic.oup.com/endo/article/140/9/4024/2990623

Bodart, V., Febbraio, M., Demers, A., McNicoll, N., Pohankova, P., Perreault, A., … & Ong, H. (2002). CD36 mediates the cardiovascular action of growth hormone-releasing peptides in the heart. Circulation research, 90(8), 844-849. https://www.ahajournals.org/doi/10.1161/01.RES.0000016164.02525.B4