ARA-290 Peptide: Multifunctional Pain Reliever

The ARA-290 peptide, a multifunctional pain reliever, is an 11-amino-acid chain isolated from the beta domain of the protein erythropoietin, which is responsible for the protein’s protective and reparative effects on damaged tissues.

Researchers once believed that this peptide’s only biological role was to increase the number of blood cells in the body. Still, a continued investigation has shown additional functions for this peptide, including neuroprotection and pain relief. Clinical trials are still being conducted to determine the peptide profile’s safety and efficacy, primarily for treating nerve pain, tissue, and wound healing.

Peptide’s History

Despite the lack of concrete evidence, it is known that the discovery of the Innate Repair Receptor (IRR) was the catalyst for the identification of the ARA-290 peptide.

Phase I and II clinical trials are complete, and phase III investigations are currently underway, especially for treating Sarcoidosis, an orphan neuropathy disease.

ARA-290 Peptide, a Multifunctional “Pain Reliever”

Around 38 trillion cells make up the average body, which is a known fact. Red blood cells, white blood cells, and platelets are the three primary types of human blood cells. Like the other two types, red blood cells are essential to human survival. Erythropoietin (EPO) is a protein in the body that controls the production and survival of red blood cells.

EPO’s primary role is to increase erythrocyte production in the body. When oxygen levels are low, more EPO is created; when they are optimal, less is produced; and the exact process by which this occurs is not yet known.

From the EPO protein, scientists have extracted a short peptide known as Cibinetide (also known as ARA-290 peptide). While ARA-290’s initial promise lay in its ability to aid blood-cell regulation, the compound’s broad features have led to its application in many other biological contexts. You can find everything you need to know about this novel peptide in this article.

Explaining the Workings Behind ARA-290 Peptide

Pathway of Innate Repair Receptors

Available information suggests that a protective receptor (TPR) pathway is triggered when tissue is injured. The EPO receptor beta subunit (CD131) is the major component of this TPR receptor, also known as the innate repair receptor.

When bound to this innate repair receptor, the peptide compound ARA-290 reduces nerve pain, allodynia-led, and inflammatory-related pain. It is widely assumed that this IRR-mediated pathway is the primary mode of action of the ARA-290 peptide.

Channel Blockade of the TRPV1 Subfamily

Most painful stimuli, including a wide range of thermal, chemical, and mechanical stimuli, are sensed by Transient Receptor Potential (TRP) channels in the nervous system. One of the TRP channels, TRPV1, is activated when a triggering substance is present. At the time of its activation, it causes the release of neuropeptides, which in turn causes the generation of action potential in the nervous system. Pain is the activation potential that causes this response.

Research published in 2016 demonstrated that the peptide ARA-290 is an antagonist to this TRPV1 channel. This discovery means that the peptide prevents the TRPV1 from triggering the release of neuropeptides that cause pain.

Several subsequent investigations have confirmed the peptide’s potential usefulness in alleviating pain, thanks to the first discovery.

Applications of the Peptide ARA-290 Peptide

The peptide Cibinetide (also known as ARA-290) has been found to have several beneficial biological effects.

• Controlling erythrocyte production and distribution
• Protecting and sustaining healthy blood vessel function
• When inflammatory cells were decreased, the peptide also reduced the discomfort.
• Having shown tissue-protecting effects
• Having an immunomodulatory effect
• Lessen the intensity of the discomfort

Studies in Non-Human Test Subjects

An Ischemic Attack on the Eye’s Retina

According to a recent study, ARA-290 may help prevent retinal ischemia by protecting the endothelial blood vessels. Retinal ischemia is a common cause of blindness and typically occurs due to numerous disorders threatening one’s eyesight. Retinal cell endothelial colony-forming cell (ECFC)  restoration is a potential treatment for this condition.

For the goal of this investigation, ECFC cells were transplanted into mouse models that had retinal ischemia generated into them. In order to test the peptide’s efficacy, some mice underwent transplanting while exposed to ARA-290 and others did not.

Once the investigation was completed, the peptide was found to lessen the inflammatory expression of interleukin cells in the retina. As a result, the presence of the peptide meant less inflammation and a quicker healing time after the transplant. This aspect confirmed that the ARA-290 peptide might effectively complement ECFC transplant therapy for repairing damaged retinal cells.

Studies Concerning the Safety of Tissues

Immunity to Inflammatory Cytokine Cells (During Transplantation)

Anti-inflammatory and cell-protective characteristics have been observed in erythropoietin cells. This investigation aimed to ascertain if the erythropoietin analog ARA-290 peptide shared the same characteristics.

When controlling blood sugar, the body relies on pancreatic islet cells. Professionals can effectively treat diabetes by replacing damaged pancreatic islet cells with healthy ones through islet cell transplantation. However, this transplantation has not shown any positive results thus far due to cellular damage and inflammatory reaction.

The islets of cells treated with a peptide were largely unharmed. As far as anyone could tell, the peptide shielded the islet cells from the cytokines and prevented their apoptosis. Thus, the ARA-290 peptide proved to be an effective agent in enhancing the transplant of pancreatic cells by shielding them from cytokines.

Safeguarding All Tissues

It is now well-established that the ARA-290 peptide connects with the protective tissue receptors (TPR), thereby protecting tissues from damaging inflammatory cells and eventual cellular death and promoting tissue homeostasis. In turn, this aids in maintaining a healthy immune system.

While both ARA-290 peptide and endogenous erythropoietin cells connect with TPR receptor cells, the latter causes detrimental cardiovascular and blood cell-related adverse effects, while the former does not. This peptide property aids tissue regeneration, reduces tissue morbidity, speeds up wound recovery and healing, and lessens scar formation.

Summary

Cibinetide, or ARA-290 peptide, is an 11-amino-acid fragment of the beta domain of the natural protein erythropoietin. The analog of erythropoietin, or peptide, is more valuable than the protein itself because it has similar properties to erythropoietin without the protein’s adverse side effects.

The peptide’s pain-relieving effects result from its ability to bind to the innate repair receptor (primary route) and block the TRPV1 cycle.

The peptide has shown promise in early research for treating autoimmune diseases, assisting in transplant procedures, and protecting against tissue and wound injuries. Due to the positive results of Phase I and II clinical studies with ARA-290 peptide in the treatment of Sarcoidosis, the peptide has been classified as an ‘orphan medication’ for treating Sarcoidosis and other rare diseases characterized by sensory deficits.

Visit this website if you are a researcher interested in buying ARA-290 for your studies.

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