Contents: Pinealon (20mg)
Form: Lyophilized powder
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Pinealon is a short synthetic peptide composed of three amino acids Glu-Asp-Arg, also called the EDR peptide.(2) Pinealon is suggested to impact the central nervous system which may lead to behavior modification, while also possibly protecting neurons and various other cell types from oxidative stress. The main potential of this peptide is its proposed ability to penetrate the blood brain barrier, cellular membrane, and nuclear membrane. It may also possibly interact directly with DNA molecules.
Pinealon tripeptide is isolated from another chemical compound, Cortexin.(2) Cortexin is a polypeptide with a particularly low molecular weight. Due to this low weight Cortexin has been suggested by researchers to possibly cross the blood brain barrier and produce possible stimulatory action on the neurotransmitters in the brain.(3)
The neuroprotective (protecting neurons and neurotransmitters) and anti-apoptotic (cell death inhibition) potential of the Pinealon peptide has been posited by researchers to be exerted via the MAPK / ERK signaling pathway.(2) The ERK signaling cascade may play a role in the phosphorylation of the substrates, which may lead to elevated neuron plasticity and increased cellular stress. In turn, this action may lead to cellular apoptosis. Similarly, MAPK signaling has been suggested by scientists to lead to some metabolic disorders and inflammatory reactions. Researchers suggest that Pinealon has the potential to reduce the synthesis of reaction oxygen species (ROS) at the cell granular level. ROS is considered to be a messenger to MAPK and ERK signaling pathways, and the reduced synthesis may lead to reduction in signaling reactions, which in turn may prevent cellular stress and cell death.(2)
Studies on Pinealon have suggested concentration-dependent potential actions of the peptide. At lower concentrations, the peptide may restrict the synthesis and subsequent accumulation of ROS and cell death; while at higher concentrations, the peptide might lead to a modulation of the cell cycle. Researchers reporting this apparent correlation in peptide presence have suggested that it may exerts antioxidant potential at lower concentrations while possibly interacting with the cell genome and altering the cell cycle.(4)
Research and Clinical Studies
Pinealon Peptide and Anti-Aging
The main purpose of this clinical study was to analyze the cellular and metabolic aspect of the synthetic tripeptides including Pinealon and a similar peptide called Vesugen. As part of this study,(5) 32 test subjects with poly-morbidity and organic brain syndrome were observed. Both peptides demonstrated anabolic potential, researchers reported improvement in the functioning of the central nervous system and other vital organs. The peptides did not appear to affect the degree of chromatin condensation, which the researchers indicated may suggest that the peptides do not exhibit any impact on cellular levels.
Another separate study(6) has suggested that the Pinealon peptide may act on the muscle cells, modulating the levels of irisin. Irisin is considered by scientists to be central to muscle cell protection and mainly secreted during exercise. Irisin may lead to the burning of excessive fat, and is assumed by researchers to induce an elongation of telomere (DNA cap) as well. By potentially increasing irisin levels, Pinealon may boost protection of DNA telomeres and thereby counteract aging action to some degree.
Pinealon Peptide and Prenatal Hyperhomocysteinemia
Scientists characterize hyperhomocysteinemia by the excessive concentration of homocysteine (HC) amino acid in the blood, indicating extreme vitamin deficiency, which might lead to increased risk of neurological deterioration.(7) The main goal of this study(8) was to determine the potential of Pinealon on experimentally induced hyperhomocysteinemic pregnant female rats. The female rats were given methionine from their second trimester onwards which appeared to lead to increased concentration of homocysteine (HC) levels. The rat offspring from the healthy mice and the experimental mice were then observed for this study. Upon analysis, it was suggested by the researchers that the peptide did not appear to reduce or inhibit the development of homocysteine in the offspring, however, there appeared to be some action seen in the peptide rats, as they appeared to exhibit increased cognitive functions. The researchers suggested that the peptide did not appear to induce metabolism of homocysteine, but did apparently lead to reduced toxic action of the compound.
Pinealon Peptide and Serotonin Expression
Studies(9) were conducted on the isolated brain cell cultures where the Pinealon peptide was presented. Upon analysis, it was suggested that the peptide might stimulate levels of serotonin expression in the cell cultures. Through the molecular docking method, it was suggested by the researchers that the peptide appeared to regulate the synthesis of 5-typtophan hydroxylase enzyme involved in the synthesis of serotonin. Scientists consider serotonin to be a key mood stabilizing hormone, and further studies are being conducted to observe the potential of Pinealon on serotonin synthesis.
Pinealon Peptide and Anti-apoptotic Properties
Studies(10) have suggested that Pinealon peptide may impact the levels of the caspase 3 enzyme. Scientists consider caspase 3 enzyme to be an initiator of cell apoptosis, or controlled cell death. When Pinealon peptide was presented in experimental rat models with ischemic stroke, the peptide appeared to modulate the levels of this enzyme, which thereby shut down the pathway of cellular death. This in turn reportedly reduced hypoxia action during the stroke.
Additionally, a separate research study(11) suggested that this potential of the peptide on the caspase 3 enzymes may extend to myocardial infarction. The action of suppressing the caspase 3 enzyme were also reported to be observed in skin cells. By reducing cellular apoptosis, the peptide may possibly stimulate cell proliferation, possibly leading to an increased regenerative process.(12)
Pinealon Peptide and Pineal Gland, Sleep Cycles
As the name suggests, Pinealon peptide has been suggested by researchers to act primarily on the pineal gland, which is considered by scientists to be the primary regulator of the sleep cycle. The pineal gland is located right at the center of the brain and is sensitive to light. Depending on the amount of light it is exposed to, it may produce melatonin hormone, which in increased levels may induce sleepiness. Sleep cycle disturbances are test subject specific but are typically considered to increase with age. Research (13) has suggested that when used in the state of insomnia or disturbed sleep cycle, Pinealon may possibly reset the pineal gland back to its optimal state, improve sleep, and possibly maintain blood pressure levels. Besides sleep regulation, pineal gland may also regulate cognitive function, bone calcification, and metabolism. All these functions are considered by scientists to decline due to the shrinkage of the pineal gland with the increasing age. Hence, by preserving the pineal gland, Pinealon peptide may possibly exhibit geroprotective potential.
Pinealon peptide is available for research and laboratory purposes only. Please review and adhere to our Terms and Conditions before ordering.
- Khavinson, V., Linkova, N., Kozhevnikova, E., & Trofimova, S. (2020). EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer's Disease. Molecules (Basel, Switzerland), 26(1), 159. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7795577/
- National Center for Biotechnology Information. PubChem Compound Summary for CID 10273502, Glu-Asp-Arg. https://pubchem.ncbi.nlm.nih.gov/compound/Glu-Asp-Arg
- Eroğlu, O., Karlıdağ, T., Kuloğlu, T., Keleş, E., Kaygusuz, İ., & Yalçın, Ş. (2018). The Protective Effect of Cortexin on Cisplatin-Induced Ototoxicity. The journal of international advanced otology, 14(1), 27–33. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6354512/
- Khavinson V, Ribakova Y, Kulebiakin K, Vladychenskaya E, Kozina L, Arutjunyan A, Boldyrev A. Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Rejuvenation Res. 2011 Oct;14(5):535-41. https://pubmed.ncbi.nlm.nih.gov/21978084/
- Meshchaninov VN, Tkachenko EL, Zharkov SV, Gavrilov IV, Katyreva Iue. EFFECT OF SYNTHETIC PEPTIDES ON AGING OF PATIENTS WITH CHRONIC POLYMORBIDITY AND ORGANIC BRAIN SYNDROME OF THE CENTRAL NERVOUS SYSTEM IN REMISSION. Adv Gerontol. 2015;28(1):62-7. Russian. PMID: 26390612. https://pubmed.ncbi.nlm.nih.gov/26390612/
- Khavinson VKh, Kuznik BI, Tarnovskaya SI, Lin'kova NS. Short Peptides and Telomere Length Regulator Hormone Irisin. Bull Exp Biol Med. 2016 Jan;160(3):347-9. doi: 10.1007/s10517-016-3167-y. Epub 2016 Jan 8. PMID: 26742748. https://pubmed.ncbi.nlm.nih.gov/26742748/
- Homocysteine. https://my.clevelandclinic.org/health/articles/21527-homocysteine
- Arutjunyan, A., Kozina, L., Stvolinskiy, S., Bulygina, Y., Mashkina, A., & Khavinson, V. (2012). Pinealon protects the rat offspring from prenatal hyperhomocysteinemia. International journal of clinical and experimental medicine, 5(2), 179–185. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3342713/
- Khavinson, V.K., Lin’kova, N.S., Tarnovskaya, S.I. et al. Short Peptides Stimulate Serotonin Expression in Cells of Brain Cortex. Bull Exp Biol Med 157, 77–80 (2014). https://link.springer.com/article/10.1007/s10517-014-2496-y#citeas
- Mendzheritskiĭ AM, Karantysh GV, Ryzhak GA, Dem'ianenko SV. [Regulation of content of cytokines in blood serum and of caspase-3 activity in brains of old rats in model of sharp hypoxic hypoxia with Cortexin and Pinealon]. Adv Gerontol. 2014;27(1):94-7. Russian. PMID: 25051764. https://pubmed.ncbi.nlm.nih.gov/25051764/
- Mariela Agosto, Michael Azrin, A Kanwar Singh, Allan S. Jaffe, Bruce T. Liang, T Serum Caspase-3 p17 Fragment Is Elevated in Patients With ST-Segment Elevation Myocardial Infarction, 2011, Journal of the American College of Cardiology, 220-221, V 57, https://www.jacc.org/doi/abs/10.1016/j.jacc.2010.08.628
- Voicekhovskaya MA, Chalisova NI, Kontsevaya EA, Ryzhak GA. Effect of bioregulatory tripeptides on the culture of skin cells from young and old rats. Bull Exp Biol Med. 2012 Jan;152(3):357-9. doi: 10.1007/s10517-012-1527-9. PMID: 22803085. https://pubmed.ncbi.nlm.nih.gov/22803085/