← All Compounds
Peptide — Khavinson Brain Tripeptide Bioregulator

Pinealon Preclinical

EDR tripeptide  |  Glu-Asp-Arg  |  Cortexin-derived short peptide  |  brain bioregulator
Molecular Weight
418.4 Da
Sequence
3 aa (Glu-Asp-Arg)
Half-life
Short plasma; tissue-penetrant
Route
Oral / SubQ / intranasal
FDA Status
Not approved
Origin
Khavinson (from Cortexin)
Related Drug
Cortexin (approved Russia)
Primary Claim
Neuroprotection + cognitive aging
Evidence
Khavinson group; limited independent replication
Cost & Access
Research-only
TL;DR

A 418-dalton Khavinson tripeptide that slips into cell nuclei. Zero Western Phase 2/3 trials.
What is it? A synthetic tripeptide Glu-Asp-Arg (EDR, 418 Da). A Khavinson short peptide isolated by fractionating Cortexin, the bovine cerebral cortex drug approved in Russia for stroke, TBI, epilepsy, and cognitive decline.
What does it do? At 418 Da, small enough to diffuse directly into cell nuclei. Proposed to modulate chromatin and neuroprotective gene transcription. Preclinical work reports reduced neuronal apoptosis, antioxidant activation, and better cognition in Alzheimer's and Huntington's mouse models.
Does the evidence hold up? Twenty years of Russian-framework clinical use as the "active short peptide" of Cortexin. Khavinson et al. Pharmaceuticals 2021 (Alzheimer's mouse model) is a modern anchor. No Western Phase 2/3 RCT. Independent replication still limited.
Who uses it? Russian neurology in post-stroke and post-TBI cognitive recovery. Longevity users pair it with Epitalon and Thymalin in the canonical Khavinson panel.
Bottom line? A small Khavinson tripeptide with a credible nuclear-penetration story. Still missing Western Phase 2/3.

What It Is

Pinealon is a synthetic tripeptide with the amino acid sequence Glu-Asp-Arg (EDR). It is one of the Khavinson "brain bioregulators" in the same family as Epithalon (AEDG, pineal/longevity) — developed by Vladimir Khavinson and colleagues at the St. Petersburg Institute of Bioregulation and Gerontology over the period 1990 to present. Specifically, Pinealon's EDR sequence was identified by fractionating Cortexin, a polypeptide neuroprotective drug derived from bovine cerebral cortex that has been clinically used in Russia and Eastern Europe for decades in the management of stroke, traumatic brain injury, cognitive decline, and epilepsy. Khavinson's group identified EDR as one of the shortest and most biologically active peptide sequences within Cortexin responsible for its neuroprotective phenotype.

What makes Pinealon unusual mechanistically is its small size — at 418 Da, it is small enough to cross cellular and nuclear membranes directly, which is uncommon for peptides (most require specific transport mechanisms or receptor binding). The proposed mechanism is that Pinealon translocates into the cell nucleus and modulates gene expression through direct interaction with nucleic acids and chromatin-associated proteins. This is the same framework Khavinson applies to Epithalon, Thymalin, and the other short peptide bioregulators — short peptides as "signal molecules" that modulate tissue-specific gene expression programs. The mechanistic hypothesis is unusual in mainstream molecular biology, but in-vitro support for nuclear translocation of fluorescence-labeled Pinealon has been published.

Pinealon's positioning in the Khavinson framework is as the "brain" bioregulator — the peptide whose tissue of origin (cerebral cortex via Cortexin) matches its proposed therapeutic targeting. Clinical use in Russia has centered on elderly cognitive decline, post-TBI cognitive recovery, stroke recovery, and general neuroprotection during aging. Dosing patterns follow the broader Khavinson framework: 10–20 day pulse courses repeated 1–2 times per year.

In the Kalios context, Pinealon sits in the same category as Epithalon and the other Khavinson peptides: substantial Russian clinical use over 20+ years, a mechanistically coherent but unusual molecular framework, and a significant evidence gap in Western-methodology replication. As of April 2026, there are no FDA-regulated Phase 3 trials of Pinealon. Community use is primarily by longevity-focused users stacking with Epithalon and NAD+, often in alternating courses.

Mechanism of Action

Pinealon's mechanism is tightly centered on the proposed gene-expression modulation framework, with downstream consequences in neuroprotection, cognition, and aging.

What the Research Shows

Pinealon's evidence base is concentrated in the Khavinson lab and modestly replicated in a handful of independent labs, consistent with the pattern of the other Khavinson peptides.

Honest Evidence Framing

Pinealon has a coherent Khavinson-framework preclinical evidence base and accumulated Russian clinical experience. It does not have Western Phase 2 or Phase 3 RCT validation. Independent laboratory replication of the gene-expression mechanism is limited. Safety experience is long and clean; efficacy evidence is concentrated in the originating research group with characteristic methodological limitations (publication in predominantly Russian-language journals, open-label designs, single-group authorship).

Human Data

Human evidence for Pinealon:

The pattern is very similar to Epithalon: extensive Russian use and an accumulated clinical experience, limited Western replication and no FDA-quality Phase 3 program. Users choosing Pinealon are implicitly accepting this evidence profile.

Dosing from the Literature

Dosing follows the broader Khavinson framework — short courses (10–20 days) repeated periodically.

ProtocolDoseFrequencyNotes
Oral (Khavinson framework)20 mgDaily, 10–20 day courseMost common oral dose in Russian clinical practice. Pinealon's small size supports oral absorption.
SubQ / IM (community)5–10 mgDaily SubQ, 10–20 day courseAlternative route; community preference.
Intranasal (community)5–10 mgDaily IN, 10–20 day courseSome users for direct CNS delivery; evidence limited.
Course interval6 months between courses1–2 courses per year is standard Khavinson framework.
Combined with EpithalonAlternating or concurrent coursesTypical longevity stack10-day Pinealon, gap, 10-day Epithalon, gap is one common pattern.
Dosing Disclaimer

Pinealon has no labeled human dose under any pharmaceutical regulatory system. The 20 mg oral dose reflects Russian clinical practice; community doses vary between 5–20 mg across different routes. There is no strong mechanistic basis for chronic daily dosing — the Khavinson framework explicitly favors pulse courses.

Reconstitution & Storage

Pinealon is supplied as lyophilized powder, typically 10 mg per vial. Oral use does not require reconstitution but may use dissolved solution for dosing precision.

Vial SizeBAC WaterConcentration5 mg Dose10 mg Dose
10 mg1 mL10 mg/mL50 units (0.5 mL)100 units (1.0 mL)
10 mg2 mL5 mg/mL100 units (1.0 mL)Entire vial
20 mg2 mL10 mg/mL50 units (0.5 mL)100 units (1.0 mL)
Oral powder (direct)None requiredMeasure by weight or capsule

→ Use the Kalios Peptide Calculator for exact dosing volumes

Supportive Nutrition & Lifestyle

Cognitive health and neuroprotection depend on multiple foundational inputs. Pinealon is a modulator on top of those inputs, not a substitute.

What to Expect — Timeline

Individual response varies. Pinealon's effects are typically subtle in the short term and clinically meaningful over repeat-course use.

Honest Framing

Pinealon's effects are typically subtle: slightly clearer thinking, mild cognitive sharpness, better sleep in some users. It is not a stimulant, not a racetam-level nootropic acute signal. Expectations calibrated to "clearer thinking and subtle cognitive support" match the actual experience better than "transformational cognitive enhancement." The Khavinson framework's durability over 40+ years of Russian clinical use supports a baseline of real mechanism, even where Western methodological validation remains thin.

Practical User Notes

Read This First

Pinealon is not FDA-approved. It is used in Russian clinical practice and community longevity protocols. The notes below are informational, not medical guidance.

Side Effects & Risks

Important

Pinealon's best safety evidence is Russian post-marketing, inherited from Cortexin. Independent Western replication is limited. Worth discussing with your doctor before any neurorecovery use.

Pinealon has one of the cleanest safety records in the Khavinson bioregulator family, consistent with 20+ years of Russian clinical use.

Bloodwork & Monitoring

Pinealon has minimal monitoring requirements. For cognitive endpoints, structured cognitive testing is more informative than lab markers.

Commonly Stacked With

Canonical Khavinson combination. Alternating 10-day courses of Pinealon (cognitive) and Epithalon (systemic longevity) is standard framework. Six-month intervals between courses.

Acute nootropic ACTH-derived peptide. Pinealon and Semax have different mechanisms; some users layer Semax for acute focus while using Pinealon for neuroprotection.

Russian anxiolytic tuftsin-derived peptide. Pinealon + Selank covers cognitive support and anxiolysis in community Russian-peptide protocols.

NAD+ precursors (NR / NMN)

Different mechanism (mitochondrial substrate). Complementary longevity stacking; no known interactions.

Omega-3 + B-complex + magnesium

Foundational cognitive-supportive supplements. Complement Pinealon's framework without specific overlap.

→ Check compound compatibility in the Stack Builder

Regulatory Status

Current Status — April 2026

Pinealon is not approved by the FDA, EMA, or any major Western regulator for any indication. Its parent molecule Cortexin is approved in Russia and several Eastern European and Asian countries; Pinealon as an isolated short-peptide product is used within the Khavinson bioregulator framework rather than as a separate approved drug.

Pinealon is not currently on the FDA Category 2 Bulk Drug Substances list. Compounding availability in US 503A/503B pharmacies is not established.

Pinealon is not specifically named on the WADA Prohibited List. Given its narrow neuroprotective framework, unlikely to become a major anti-doping target.

Pinealon is not DEA-scheduled. Community supply is through research-chemical vendors or Russian pharmacy import.

Cost & Access

Pinealon (EDR, Glu-Asp-Arg) is not approved for human use in the United States, the EU, or any major Western regulator. It is available through research suppliers for laboratory research purposes only. U.S. compounding pharmacies cannot legally compound Pinealon under current FDA bulk-substance rules — it has no FDA-approved reference product.

Research-chemical vendors supply lyophilized Pinealon at typical vial sizes of 10 mg or 20 mg. A typical community Khavinson protocol (5–10 mg/day SubQ for 10 consecutive days, repeated every 4–6 months) consumes 50–100 mg per course.

Parent molecule Cortexin (polypeptide complex of which Pinealon/EDR is one component) is an approved pharmaceutical in Russia and select Eastern European and Asian markets, used in Russian neurology and pediatric practice for cerebrovascular and cognitive indications. Cortexin import to the United States for personal use exists in a legal gray area; bulk import is prosecuted. Isolated Pinealon as a single-peptide product is not a commercial pharmaceutical anywhere, only a research preparation and community-protocol compound.

Pinealon is not currently among the peptides under HHS Secretary Robert F. Kennedy Jr.'s February 2026 Category 2 reclassification announcement. Public reporting on the reclassification list has not specifically named Pinealon. As a Russian-framework short peptide without a U.S. NDA sponsor, Pinealon is likely to remain in the research-only category for the foreseeable future.

Estimated availability as of April 2026. Actual costs vary by provider, location, and prescription status. Kalios does not sell compounds.

Related Compounds

People researching Pinealon often also look at these:

N-acetylated epithalon analogue with improved bioavailability and longer half-life.

Khavinson dipeptide (Lys-Glu). Immune/longevity-oriented short-peptide bioregulator.

Khavinson tetrapeptide (Ala-Glu-Asp-Pro). Cerebral cortex-oriented bioregulator.

Khavinson tetrapeptide (Lys-Glu-Asp-Ala). Liver-oriented short peptide bioregulator.

Khavinson tripeptide (Ala-Glu-Asp). Cartilage and joint-oriented short peptide bioregulator.

Next Steps

Key References

  1. Khavinson V, Ilina A, Kraskovskaya N, Linkova N, Kolchina N, Mikhailova N, Petukhov M. Neuroprotective Effects of Tripeptides-Epigenetic Regulators in Mouse Model of Alzheimer's Disease. Pharmaceuticals (Basel). 2021;14(6):515. PMID: 34071714.
  2. Khavinson VKh, Kuznik BI, Tarnovskaya SI, Lin'kova NS. EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer's Disease. Int J Mol Sci. 2021. PMC7795577.
  3. Khavinson VKh, Lin'kova NS, Kukanova EO. Neuroprotective Effect of EDR Peptide in Mouse Model of Huntington's Disease. J Neurol Neurosci. 2017. (Khavinson group Huntington's publication.)
  4. Khavinson VKh. Peptides and Ageing. Neuro Endocrinol Lett. 2002;23 Suppl 3:11-144. PMID: 12370707. (Comprehensive Khavinson peptide framework monograph.)
  5. Khavinson VKh, Morozov VG. Peptides of pineal gland and thymus prolong human life. Neuro Endocrinol Lett. 2003;24(3-4):233-240. PMID: 14523363.
  6. Anisimov VN, Khavinson VKh. Peptide bioregulation of aging: results and prospects. Biogerontology. 2010;11(2):139-149. PMID: 19633997.
  7. Khavinson VKh, Sibarov DA, Tsai PY, Adushkin BV, Ryzhak GA. Short peptides stimulate serotonin release and attenuate hyperexcitation in the hippocampus. Bull Exp Biol Med. 2017;163(4):539-541.
  8. Kolchina N, Khavinson V, Linkova N, Yakutseni P, Petukhov M, Morozova E, Ashapkin V. Systematic search for structural motifs of peptide binding to double-stranded DNA. Nucleic Acids Res. 2019;47(20):10553-10563. PMID: 31584079.
  9. Khavinson V, Popovich IG, Linkova NS, Mironova ES, Ilina AR. Peptide Regulation of Gene Expression: A Systematic Review. Molecules. 2021;26(22):7053. PMID: 34834146.
  10. Ashapkin VV, Linkova NS, Khavinson VK, Vanyushin BF. Epigenetic Mechanisms of Peptidergic Regulation of Gene Expression during Aging of Human Cells. Biochemistry (Mosc). 2015;80(3):310-322. PMID: 25761684.
  11. Khavinson VK, Popovich IG, Linkova NS, Mironova ES, Ilina AR. Peptide regulation of aging: methodology and evidence. Bull Exp Biol Med. 2022.
  12. Khavinson V, Diomede F, Mironova E, Linkova N, Trofimova S, Trubiani O, Caputi S, Sinjari B. AEDG Peptide (Epitalon) Stimulates Gene Expression and Protein Synthesis during Neurogenesis. Int J Mol Sci. 2020;21(2):609. PMID: 31963526.
  13. Klement GA, Hawrysh PJ, Khavinson V, Buck LT. Pinealon's effect on hypoxia tolerance in cultured rat pyramidal neurons. Cell Mol Neurobiol. 2018.
  14. Khavinson VK, Kuznik BI, Lin'kova NS. Cortexin and its mechanisms of action. Adv Gerontol. 2014;27(4):626-634.
  15. Russian Federation State Register of Medicines. Cortexin — parent drug of Pinealon's EDR sequence; approved for TBI, stroke, cognitive indications.
  16. Khavinson V, Linkova N, Diatlova A, Trofimova S. Peptide Regulation of Cell Differentiation, Proliferation, and Apoptosis. Adv Gerontol. 2020;10(2):98-106.
  17. Khavinson VKh, Kuznik BI, Trofimova SV, Lin'kova NS. Cortexin and its short peptides AEDG and EDR modulate gene expression of proteins in pathogenesis of Alzheimer's disease. Biomed Khim. 2020. (Parallel framework evidence for Khavinson short-peptide gene-expression paradigm.)
  18. Khavinson VKh, Malinin VV. Gerontological Aspects of Genome Peptide Regulation. Karger; Basel; 2005. (Monograph; framework reference.)

Last updated: April 2026  |  Profile authored by Kalios Peptides research team