Pinealon

Origin and structure

Pinealon is a chain of three amino acids, glutamic acid, aspartic acid and arginine, written Glu-Asp-Arg or EDR (C15H26N6O8, 418.40 g/mol, CAS 175175-23-2). It comes from the school of Vladimir Khavinson at the St Petersburg Institute of Bioregulation and Gerontology, which works on 'peptide bioregulators': short peptides of two to four amino acids that, in the group's view, each act on a particular tissue by regulating its genes.

Khavinson and colleagues filed a Russian patent application for the peptide on 30 May 2006, followed by an international application published in December 2007, presenting it as a new synthetic substance to stimulate the regeneration of nerve cells. The patent describes it as an acetate salt, a white, odourless powder, and already contains the toxicity tests, the animal experiments and a small clinical study. Later papers from the same group describe EDR as a component of Cortexin, a Russian neuroprotective drug extracted from the brain cortex of cattle. The name, which points to the pineal gland, therefore says little about where the peptide comes from or what it was developed for.

How it is thought to work

No receptor for Pinealon has been described. Khavinson's group proposes instead that short peptides enter cells and their nuclei, bind to DNA and histone proteins, and so switch particular genes on or off. The support comes mainly from the group's own experiments and computer modelling: labelled EDR entered cell nuclei, and docking studies predicted binding sites in the promoter regions of genes for the cell-death enzyme caspase-3, the antioxidant enzymes SOD2 and GPX1, the transcription factors PPARA and PPARG, and TPH1, the enzyme that makes serotonin. Such a mechanism would be unusual in pharmacology, and it rests largely on work from this one network of laboratories.

The effects measured in the laboratory are more conventional. In rat nerve cells and immune cells under oxidative stress, Pinealon limited the build-up of reactive oxygen species, reduced cell death and delayed activation of the ERK1/2 signalling pathway. In rats sensitive to oxygen shortage it raised the activity of the antioxidant enzymes SOD2 and glutathione peroxidase in the brain to the level of resistant animals, and in cultures of rat brain-cortex cells it increased the production of serotonin.

How Pinealon behaves in the body has not been measured: there are no published pharmacokinetic data in humans, so it is unknown whether a tripeptide swallowed as a capsule survives digestion or whether any of it reaches the brain. Russian studies have nevertheless given it by mouth as well as by injection.

Is Pinealon approved?

No. No medicine containing Pinealon is authorised by the EMA or the FDA. In the Netherlands it is not a registered medicine and may not be sold or promoted for human use; it is available only as research material, which is the basis our shop operates on.

Russian studies have also used Pinealon in capsule form: an occupational-health study in locomotive crews gave capsules of 100 micrograms. Use in such studies is not an approval as a medicine.

In the United States Pinealon is not approved for any use and has never been nominated for the list of bulk substances that pharmacies may compound with: it does not appear on the FDA's list of nominated substances in any of its three categories (version of 14 May 2026).

In sport Pinealon is not named on the WADA Prohibited List, but as a substance that no authority has approved for human therapeutic use it falls under category S0 and is prohibited at all times, in and out of competition. The Dopingautoriteit applies the same list in the Netherlands.

What the research shows

The literature is small and concentrated. Nearly every study comes from Khavinson's institute or Russian groups working with it, much of it published in Russian in the journal Advances in Gerontology (Uspekhi Gerontologii), and ClinicalTrials.gov lists no Pinealon trial. The main findings:

• Cells (Khavinson et al., Rejuvenation Res 2011): in rat cerebellar granule cells, neutrophils and PC12 cells exposed to oxidative stress, Pinealon limited reactive oxygen species and necrotic cell death in a dose-dependent way.
• Oxygen shortage and ageing in rats (Mendzheritsky group, 2013-2014, summarised in Khavinson's 2021 review): in rats of different ages exposed to acute hypoxia, Pinealon was compared with Cortexin. Its effects on the cell-death enzyme caspase-3 went in different directions across experiments, and in one study it improved maze learning in both young and old animals.
• Prenatal stress (Arutjunyan et al., Int J Clin Exp Med 2012): when pregnant rats on a methionine-loaded diet received Pinealon, their offspring learned spatial tasks better and their cerebellar neurons resisted oxidative stress better.
• Alzheimer's models (Khavinson et al., Pharmaceuticals 2021): in 5xFAD mice, two months of daily injections raised the density of dendritic spines in the hippocampus by 11% against saline, back to the level of normal mice (10 mice per group). The effect on long-term potentiation, a measure of synaptic plasticity, was a trend that did not reach statistical significance. A 2025 correction replaced two figures that had been identical; the authors say the conclusions are unaffected. In earlier cell cultures, EDR raised the number of mature 'mushroom' spines by up to 71% under amyloid toxicity.
• Independent mouse screen (Marín-Jerez et al., bioRxiv 2026, a preprint that has not been peer-reviewed): in an eight-week test of five candidate longevity treatments in groups of five male mice, Pinealon showed a non-significant trend towards better working memory and no detectable adverse effects. The authors work in Spain and Switzerland, outside the Russian network.
• Toxicity (developers' patent, 2007): according to the patent, single injections more than 5,000 times the proposed human dose in mice, and daily injections for 90 days in rats and six months in guinea pigs, caused no toxic effects. These data come only from the developers.
• Brain injury (same patent): 25 patients aged 31 to 60 with lasting consequences of a head injury were randomised to Pinealon injections or saline for 10 days. The treated groups did better on an attention test and had a higher EEG alpha index. The patent reports 'good results' in 59.4% of patients, a percentage that cannot come from 25 people, and its tables compare with 'commonly used medications' rather than saline. No adverse effects were recorded. The group's 2021 review describes the same test results as coming from oral use, although the patent gives injections, and it also mentions 72 brain-injury patients who received Pinealon by mouth alongside standard treatment, citing only an earlier Russian review.
• Workers and older adults (Advances in Gerontology, 2012 and 2015): Russian studies in locomotive crews and in middle-aged and older patients, the latter alongside the vascular peptide Vesugen (KED), reported better 'biological age' scores. The patient study, in 32 people aged 41 to 83 with organic brain syndrome (the abstract lists 18 men and 12 women), also found pro-oxidant activity and a fall in CD34+ blood stem cells.

Pinealon versus Epitalon and Cortexin

The name suggests the pineal gland, the small gland in the brain that makes melatonin, and Pinealon is often marketed for sleep. The research does not support that link. Khavinson's group places EDR in Cortexin, a brain-cortex extract, and studies it as a protector of nerve cells. When the group tested several of its peptides on cultured rat pineal tissue in 2011, Pinealon changed none of the markers measured, whereas Epitalon raised markers of both growth and secretion in the pineal cells. The nearest link to melatonin is that Pinealon raised serotonin, the molecule melatonin is made from, in cultures of brain-cortex cells. No study indexed in PubMed has measured melatonin after Pinealon.

Epitalon (Ala-Glu-Asp-Gly) is a different molecule: a tetrapeptide that the same school regards as its pineal peptide. The two are often sold side by side, and Russian studies have combined Pinealon with other Khavinson peptides, but evidence for one says nothing about the other. Cortexin, in turn, is a mixture of many peptides extracted from brain tissue; Pinealon is a single synthetic tripeptide, and results obtained with Cortexin cannot be transferred to it.

Frequently asked questions

Is Pinealon legal in the Netherlands?

Pinealon is not a registered medicine in the Netherlands or anywhere else in the EU, so it may not be sold or promoted for human use. It can be bought and sold as research material, which is the basis our shop works on.

Does Pinealon increase melatonin?

There is no evidence that it does. No study indexed in PubMed has measured melatonin after Pinealon. In cultured rat pineal tissue it changed none of the markers measured, and its developers describe it as a peptide for the brain cortex. The idea comes mostly from the name.

What is the difference between Pinealon and Epitalon?

Both come from Vladimir Khavinson's institute, but they are different molecules: Pinealon is the tripeptide Glu-Asp-Arg, linked to brain tissue, and Epitalon the tetrapeptide Ala-Glu-Asp-Gly, which the group regards as its pineal peptide. In the group's 2011 experiment on pineal tissue, Epitalon stimulated the pineal cells and Pinealon did not. Results for one cannot be applied to the other.

Has Pinealon been tested in humans?

Only in small Russian studies: a 25-patient brain-injury study described in a patent, and studies in workers and patients published in Russian. None appears on ClinicalTrials.gov, none has been repeated outside Russia, and the reports leave basic questions open, such as how many patients the published percentages refer to. They are not enough to show that Pinealon works or that it is safe.

Is Pinealon banned in sport?

Yes. It is not named on the WADA list, but as a substance without approval for human therapeutic use it falls under category S0, prohibited in and out of competition. The Dopingautoriteit applies the same list in the Netherlands.

Is Pinealon FDA-approved?

No. It has no FDA approval for any use, and it has never been nominated for the FDA's list of bulk substances that US pharmacies may compound with.

Storage and handling

Store according to product-label instructions and batch handling notes. Lyophilized research peptides are commonly kept dry, protected from light, and handled with clean laboratory technique.

References

Checked against these sources on 28 October 2026.

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