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Pinealon

Also known as EDR peptide, glutamyl-aspartyl-arginine

Tripeptide from the Russian bioregulator programme, neuroprotective claims without independent evidence.

preclinical Neuro & cognition research chemical

At a glance

Category
Neuro & cognition
Status
research chemical
Route
subcutaneous and intramuscular in research; oral or sublingual in the capsule form of the bioregulator line
Half-life
No published pharmacokinetics. A tripeptide with free termini and no protective modification; survival in plasma presumably a matter of minutes. All circulating figures are unsourced.
Onset
No validated onset time; there are no controlled human data on the time course of any effect
Molecular weight
418.4 g/mol 1
Sequence
Glu-Asp-Arg

As far as can be established, synthetic pinealon is not a registered medicine anywhere. Endoluten and the Cytomax capsule line are registered in Russia as a food supplement (BAD), a notification regime without any efficacy assessment - which is something other than approval as a medicine. PeptideX has not been able to open the Russian register from outside Russia to confirm this, so the registration should be read as an unverified claim rather than an established fact. No EMA or FDA approval; outside Russia traded exclusively as a 'research chemical'. A search of ClinicalTrials.gov returns no registered study of pinealon at all 12.

Doping status: Not listed by name; as a non-approved substance it falls under S0 and therefore counts as prohibited at all times

Checked against the WADA 2026 Prohibited List. For a specific product and country, Global DRO is the lookup athletes are expected to use — the List names substances, not brand names.

Mechanism of action

Pinealon is the tripeptide member of the same pineal series as Epitalon, from the same institute and the same researcher (Khavinson, St Petersburg Institute of Bioregulation and Gerontology). It stands to Endoluten roughly as Epitalon stands to Epithalamine: a synthetic single peptide presented as the active fraction of a crude organ extract.

The proposed mechanism is the same as for Epitalon: EDR is said to enter neuronal nuclei, bind to promoter DNA and direct the expression of genes for antioxidant defence, DNA repair, apoptosis regulation and serotonergic signalling.

The same criticism applies with even greater force. A tripeptide has even less capacity for sequence-specific DNA recognition than a tetrapeptide. That EDR, with an arginine residue, carries a roughly neutral net charge is sometimes put forward as a reason why DNA interaction would be more plausible than with Epitalon, but weak electrostatic association is not yet regulatory binding. The one physical-chemistry study of the interaction reports that EDR can partly enter the DNA major groove and contact guanine, and that magnesium ions promote the association by screening the phosphate charge 11 - which describes a salt-dependent, non-specific approach to the double helix rather than a promoter-selective regulatory contact. No independent structural biology confirms a regulatory binding mode. This is a hypothesis, not a mechanism.

Passage across the blood-brain barrier is attributed to the peptide transporter PEPT2. PEPT2 genuinely exists and transports di- and tripeptides, so the claim is not absurd, but it has been found only in secondary sources and not in a primary transport study for EDR. With oral administration of an unprotected tripeptide, bioavailability is moreover an obvious objection, which the programme answers with the assumption of intact absorption - not with independent evidence.

The positioning differs from Epitalon: Pinealon is not presented as a telomerase activator but as a neuroprotective agent. The specific cancer concern around Epitalon therefore does not apply, but Pinealon thereby also lacks the one independently replicated cell-biological finding that Epitalon does have.

What the research shows

Pinealon's evidence base is considerably weaker than that of Epitalon, which is already weak in itself. There is no human study with the synthetic peptide, no independent Western replication of any finding whatsoever, and all the animal research comes from the Khavinson group or affiliated Russian laboratories. There is no basis at all for stating that Pinealon improves cognition, protects neurons or slows brain ageing in humans.

Research in humans

No clinical study with synthetic Pinealon reporting cognitive or other outcomes was found, and ClinicalTrials.gov holds no registered trial of it 12. The claims that relate to humans rest on extrapolation from the literature on Endoluten and Epithalamine - different substances, namely crude bovine extracts - and from rat research.

Animal and lab research

The specific findings, and what the primary papers actually report: dose-dependent restriction of reactive oxygen species accumulation and reduced necrotic cell death in rat cerebellar granule cells, neutrophils and PC12 cells, with activation of proliferative processes 6 - note that this is cerebellar and PC12 material in culture, not cortical neurons, and the paper reports no measurement of mitochondrial membrane potential; protection of rat offspring against prenatal hyperhomocysteinaemia, with better spatial orientation and learning and fewer necrotic cerebellar neurons after maternal dosing 7; dose-dependent preservation of a learned Morris-maze skill and altered hippocampal NMDA receptor subunit expression in rats after streptozotocin-induced diabetes, best at 100 ng/kg 8; stimulation of serotonin expression in ageing rat brain cortex cell cultures 9; and improved survival with altered behaviour and brain caspase-3 activity in old rats after carotid artery occlusion, in a study that gave Pinealon and Cortexin as separate arms 10. Claims of preserved mitochondrial membrane integrity under hypoxia circulate widely but could not be traced to any primary publication and have been removed.

Caveats. Structural problems in that work: small sample sizes; extreme ischaemia and hypoxia models that do not model normal cognitive ageing; frequent co-administration with Cortexin, which makes the contribution of EDR itself impossible to attribute; outcome measures chosen after the fact; no protocol registration; no blinding described. Publication takes place in Russian-affiliated journals with limited external scrutiny, and a large part of the work is in Russian and therefore hard to assess independently.

What it is used for

  • Presented as a neuroprotective agent and as a remedy for cognition and brain ageing - claims the evidence does not support
  • Studied in animal research in cerebral ischaemia 10, prenatal hyperhomocysteinaemia 7 and streptozotocin-induced diabetes 8
  • Self-administered in the grey market in courses, without a validated indication or dose

Dosing

Dose
In rodent studies microgram doses, usually intraperitoneally or intranasally over short courses; exact values per kilogram differ between studies. The capsule form (Endoluten) is used as 1-2 capsules per day. In user protocols 1-10 mg per day subcutaneously circulates, and in some protocols 100-200 mcg per day.
Frequency
In user protocols once daily
Route
subcutaneous in user protocols
Duration
In user protocols courses of 10-20 days, 2-4 times per year
  • There is no validated dose: no dose-finding research, no maximum tolerated dose, no human pharmacokinetics and no dose-response curve. The nearest thing to a dose-response study is the rat diabetes experiment, which compared 50, 100 and 200 ng/kg and found 100 ng/kg best 8 - nanograms per kilogram, in rats, which is several orders of magnitude below anything in the circulating human protocols.
  • The common figures are an artefact of the vial size, not a research finding.
  • Doses are described here solely because they circulate, not because they are supported.

These figures describe what the literature and published protocols report. They are not advice and not a dosing instruction.

Protocols

Bioregulator course (grey market)

user protocol — not validated

Source: user protocols and vendor material

This is not a validated schedule. It is a pattern that circulates among users and sellers, reproduced because it is what people actually follow — not because it has been tested. No trial established these doses, this interval or this duration, and nobody is checking what is in the vial. Treat every number below as an assertion, not a finding.

Days 1-10, some protocols to 201-10 mg per day by subcutaneous injection; some protocols instead give 100-200 mcg per day
Repeattwo to four times a year

The hundredfold spread between the two circulating figures is itself the point: no dose-finding work exists to choose between them, and the milligram figures track the vial size. The Russian capsule product in the same line is taken orally at 1-2 capsules per day and is a different preparation, not a swallowed version of this schedule.

Schedules are reproduced as their source states them. Units, IU and milligrams explains why the figures are not interchangeable between products.

Reconstitution

Vial sizes
10 mg, 20 mg (lyophilised powder); alongside capsules as part of the Endoluten line, a different product based on bovine extract
Solvent
bacteriostatic water (0.9% benzyl alcohol); sterile water only if used within the same session
Storage
Powder at 2-8 °C for the short term or -20 °C long term, protected from light. Reconstituted at 2-8 °C and, according to suppliers, to be used within about 2-4 weeks; with ordinary sterile water, the same day. Avoid repeated freezing and thawing.

Worked example

10 mg vial + 2 ml bacteriostatic water = 5 mg/ml. 1 mg then corresponds to 0.2 ml, that is 20 units on a U100 insulin syringe.

Let the water run slowly down the wall, swirl and do not shake; do not use if cloudy. These handling instructions come from suppliers and are not pharmacopoeia specifications. Grey market products are regularly mislabelled, underdosed or contaminated; certificates of analysis drawn up by sellers themselves cannot be independently verified.

Work it out for Pinealon

Safety

Side effects

  • Not systematically documented, because no systematic safety research exists. The absence of a side effect profile reflects a lack of research, not demonstrated safety
  • Reported at user level, uncontrolled: injection site reactions, headache and changes in sleep

Do not use if

  • Pregnancy and breastfeeding - no data; notably, the animal literature specifically dosed pregnant rats and measured effects in their offspring 7, which is a reason for caution and not for reassurance
  • Children and adolescents - no data
  • Hypersensitivity to the peptide or to benzyl alcohol in the diluent
  • Unlike Epitalon, the claimed mechanism does not imply a specific oncological contraindication - but 'no known mechanistic risk' is not the same as 'studied and found safe'

Interactions

Not studied. Theoretically, caution with serotonergic agents given the reported stimulation of serotonin expression in cortical cell cultures 9, and with other centrally acting agents; this is reasoning from a cell-culture finding, not an observed interaction.

Sources