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The Peptide Effect
preclinicalNeuroprotection & Sleep

Pinealon

Also known as: EDR, Glu-Asp-Arg, Pinealon bioregulator, Khavinson pineal peptide

Pinealon is a synthetic tripeptide bioregulator (Glu-Asp-Arg) developed by Professor Vladimir Khavinson at the Saint Petersburg Institute of Bioregulation and Gerontology. It belongs to the Khavinson bioregulator peptide family — a class of ultra-short peptides theorized to bind specific DNA sequences and regulate gene expression in target tissues. Pinealon specifically targets the pineal gland and central nervous system, with reported neuroprotective, sleep-modulating, and antioxidant properties. It represents the Russian bioregulatory medicine tradition, which is largely distinct from Western pharmaceutical research.

Key Facts

Mechanism
Pinealon is proposed to act through the Khavinson bioregulation model, in which short peptides (2–4 amino acids) bind complementary DNA sequences in gene promoter regions, modulating transcription in tissue-specific ways. Pinealon (Glu-Asp-Arg) is theorized to interact with DNA regulatory elements in pinealocytes (pineal gland cells) and cortical neurons. In vitro, it has demonstrated the ability to penetrate cell membranes and localize to the nucleus. Its proposed downstream effects include: normalization of melatonin synthesis via pineal gland gene regulation, neuroprotective activity through upregulation of anti-apoptotic proteins (Bcl-2) and downregulation of pro-apoptotic proteins (Bax, caspase-3), and antioxidant effects via enhanced superoxide dismutase activity. The bioregulator model remains controversial in Western science, as the mechanism by which a tripeptide would achieve sequence-specific DNA binding is not fully elucidated.
Research Status
preclinical
Half-Life
Very short (minutes — typical of tripeptides, though effects may persist through gene expression changes)
Molecular Formula
C₁₅H₂₅N₅O₈
Primary Use
Neuroprotection & Sleep

Benefits

  • Neuroprotective effects demonstrated in cell culture — reduces neuronal apoptosis under oxidative stress by modulating Bcl-2/Bax ratiopreliminary
  • May normalize pineal gland function and melatonin synthesis, particularly in age-related pineal calcificationpreliminary
  • Improved sleep quality and circadian rhythm regulation reported by users, potentially through restored melatonin secretion patternsanecdotal
  • Antioxidant properties in CNS tissue — enhanced superoxide dismutase and glutathione peroxidase activity in preclinical studiespreliminary
  • May support cognitive function in elderly individuals through neuroprotective and pineal-normalizing mechanismsanecdotal

Dosage Protocols

RouteDosage RangeFrequencyNotes
Oral / sublingual10–20 mgOnce daily, typically before bedStandard Khavinson bioregulator protocol. Sublingual administration may improve bioavailability for this tripeptide. Taken 20–30 minutes before sleep.
Intranasal spray100–300 mcgOnce daily before bedSome suppliers offer intranasal formulations. May provide faster onset and more direct CNS access. Dosing not standardized.
Oral / sublingual (cycling protocol)10–20 mgDaily for 10–30 day cycles, 2–4 cycles per yearTraditional Khavinson cycling approach. Bioregulators are typically used in defined courses rather than continuously, with effects said to persist for months after each cycle.

Medical disclaimer

Dosage information is provided for educational reference only. Always follow your prescriber's instructions and consult a qualified healthcare provider before starting any peptide protocol.

Side Effects

  • Generally well tolerated in available studies — no significant adverse effects reported in published literaturerare
  • Mild drowsiness — occasional reports, likely related to melatonin pathway modulationcommon
  • Vivid dreams or changes in dream patterns — reported anecdotally by some userscommon
  • Headache — infrequently reported during initial dosingrare
  • Unknown long-term effects — the bioregulator model of gene expression modulation has not been validated in long-term human studiesserious

Frequently Asked Questions

What are Khavinson bioregulator peptides and how are they different from other peptides?
Khavinson bioregulator peptides are a class of ultra-short synthetic peptides (2–4 amino acids) developed by Professor Vladimir Khavinson in Russia over several decades. Unlike typical therapeutic peptides that bind cell-surface receptors, bioregulators are theorized to penetrate cells, enter the nucleus, and bind specific DNA sequences to regulate gene expression in a tissue-specific manner. Each bioregulator targets a specific organ: Pinealon for the pineal gland, Cortagen for the cerebral cortex, Epithalon for the pineal/telomerase system, Thymalin for the thymus, etc. This approach is widely used in Russian medicine but has limited acceptance in Western science due to the unconventional mechanism of action and the majority of research being published in Russian-language journals.
How does Pinealon compare to melatonin supplements?
Pinealon and melatonin work at fundamentally different levels. Melatonin supplements directly provide the hormone — essentially hormone replacement. Pinealon, if the bioregulator model is accurate, works upstream by normalizing the pineal gland's own melatonin production through gene expression modulation. The theoretical advantage is that Pinealon restores natural, physiological melatonin secretion patterns rather than overriding them with exogenous hormone. The disadvantage is that the evidence base for Pinealon is dramatically thinner than for melatonin, which has extensive clinical trial data. They are not interchangeable — melatonin is a proven sleep aid, while Pinealon remains an experimental research compound.
Is the Russian peptide bioregulator research credible?
This is a nuanced question. Professor Khavinson and his institute have published hundreds of papers, and the research has been influential enough to result in approved medications in Russia (e.g., Thymalin, Epithalamin). Several papers have appeared in indexed, peer-reviewed journals. However, the research has significant limitations by Western standards: most studies are small, many lack rigorous controls, independent replication by non-Russian labs is limited, and the proposed mechanism (tripeptides binding specific DNA sequences) challenges established molecular biology. The science should be evaluated with interest but also healthy skepticism. The compounds may work through mechanisms other than those proposed.
Can tripeptides like Pinealon survive digestion and be orally bioavailable?
This is a valid concern. Larger peptides are typically degraded by gastrointestinal enzymes and have poor oral bioavailability. However, tripeptides (3 amino acids) and dipeptides have demonstrated significantly better intestinal absorption than larger peptides. The intestinal epithelium has specific peptide transporters (PepT1/SLC15A1) that actively transport di- and tripeptides across the gut wall. Studies have shown that certain tripeptides can reach systemic circulation intact after oral administration. Sublingual administration may further improve bioavailability by avoiding first-pass metabolism. Whether Pinealon specifically achieves therapeutically relevant concentrations after oral dosing has not been definitively established.
What is the recommended cycling protocol for Pinealon?
The traditional Khavinson bioregulator protocol involves taking Pinealon daily for 10–30 days, then discontinuing for 3–6 months before the next cycle. Typically 2–4 cycles per year are recommended. The rationale is that bioregulators are thought to trigger lasting gene expression changes that persist well beyond the administration period — essentially "resetting" the target tissue's function. Continuous daily use is generally not recommended in the Khavinson model. Some practitioners combine Pinealon cycles with Epithalon cycles, targeting both pineal function and telomere maintenance. There is no clinical trial data validating any specific cycling protocol.

References

  1. 1
    Peptide regulation of gene expression and protein synthesis in bronchial epithelium(2010)PubMed ↗
  2. 2
    Short peptides stimulate cell regeneration and regulate gene expression(2012)PubMed ↗
  3. 3
    Neuroprotective effect of EDR peptide in models of oxidative stress in vitro(2017)PubMed ↗
  4. 4
    Peptide bioregulators: a new class of geroprotectors (review)(2018)PubMed ↗

Last updated: 2026-02-14