Pinealon (EDR)
Khavinson 'Cytogen' synthetic tripeptide · claimed brain/CNS bioregulator · single-school evidence
Pinealon is a synthetic tripeptide — just three amino acids, Glu-Asp-Arg (EDR) — from the 'Cytogen' line of short 'peptide bioregulators' developed by Vladimir Khavinson and the St. Petersburg Institute of Bioregulation and Gerontology in Russia. It is marketed as a brain/CNS peptide for neuroprotection, cognition and 'anti-aging' of brain tissue. Two things are worth separating clearly. The chemistry is real and verifiable: the EDR tripeptide is a genuine, well-defined molecule, and the chemical database itself links the name 'Pinealon' to that sequence. The biology is where caution is needed. Essentially the entire evidence base traces back to Khavinson's own network and a small circle of affiliated Russian labs; no independent group outside that network has replicated the key findings. The defining claim — that this tiny peptide enters the cell nucleus and directly switches genes on and off — is a single-school hypothesis, not established molecular biology. What has actually been shown is narrower: in cell cultures, EDR reduced the build-up of reactive oxygen species (a marker of oxidative stress) and reduced cell death; in rodent stress models (such as low-oxygen exposure and prenatal stress), it improved some behavioural and biochemical markers. There are no completed independent human efficacy trials, and it is not approved by any major drug regulator. The honest framing: a real, well-characterised little molecule with interesting cell-culture and rodent signals — but its neuroprotective and 'brain anti-aging' claims are unproven hypotheses, not facts.
The short version
Pinealon is the trade name for a very short synthetic peptide called EDR — three amino acids strung together (glutamic acid, aspartic acid, arginine). It comes from a Russian research programme led by Vladimir Khavinson that designed a whole family of these tiny 'bioregulator' peptides, each assigned a target tissue. Pinealon's assigned target is the brain.
It helps to keep two questions apart. First, is the molecule real and well-defined? Yes — the chemistry checks out against the primary chemical database, which even lists 'Pinealon' and the EDR sequence on the same record. Second, do its brain-health claims hold up? That is far less certain. Almost all of the research comes from Khavinson's own group and a few closely linked Russian labs, and no independent team has reproduced the headline results.
What the studies actually show is modest and early-stage. In dishes of cultured cells, EDR lowered the accumulation of 'reactive oxygen species' (a form of chemical stress inside cells) and reduced how many cells died. In rats — for example, offspring of mothers exposed to stress, or animals exposed to low oxygen — it improved some learning and brain-chemistry measures. The big leap that vendors make — from 'reduces stress markers in a dish' to 'protects and rejuvenates the human brain' — is not supported by independent human trials. There are none completed. So Pinealon is best understood as an interesting experimental peptide with preliminary signals, not a proven brain therapy.
Molecular identity
Specs
- Molecular formula
- C₁₅H₂₆N₆O₈
- Molecular weight
- 418.40 g/mol
- Monoisotopic mass
- 418.18121 Da
- Sequence (3 AA)
- Glu-Asp-Arg (EDR) — L-α-glutamyl-L-α-aspartyl-L-argininePubChem CID 10273502
- Structure / class
- Synthetic tripeptide; Khavinson 'Cytogen' bioregulatorPubChem CID 10273502; Khavinson-school literature
- CAS number
- 175175-23-2PubChem CID 10273502 (EPA DSSTox source)
- PubChem CID
- 10273502PubChem (carries both 'Pinealon' and 'Glu-Asp-Arg' as synonyms)
- UNII
- Unverified — not assertedNo UNII heading in the PubChem record
- Water solubility
- Highly water-soluble (computed XLogP −6.1)PubChem CID 10273502 (computed)
- Molecular target
- No classic receptor; claimed CNS gene-expression modulator (neuroprotection / neuronal viability) — single-school positioning, in-vitro & rodent onlyKhavinson-school 'tissue-specific peptide' framework
- Half-life
- Not established (no published human pharmacokinetic data; vendor '2–4 h' figures are not from a primary PK study)Not establishedHalf-life curve →
- Regulatory status
- Not approved by any major drug regulator; no completed independent human efficacy trialsNo NDA/BLA/EMA record located
Plain English
Mechanism
The Khavinson school's central idea — applied to Pinealon and to the whole Cytogen family — is that ultra-short peptides can pass through the cell membrane AND the nuclear membrane, reach the DNA, and act as direct 'epigenetic' regulators of gene expression: switching on genes that keep neurons alive and switching off pathways that drive cell death and oxidative damage. This 'short peptides enter the nucleus and regulate genes' model is the defining hypothesis of the school.
It is important to be blunt here: this nucleus-penetration / direct gene-regulation paradigm is a single-school hypothesis advanced almost entirely by the Khavinson network. It is not an independently established mechanism of action, and it should not be presented as settled cell biology. Plausible-sounding and internally consistent across the network's own papers is not the same as externally validated.
What the primary work actually demonstrates is narrower and more concrete: dose-dependent reductions in reactive oxygen species and reduced cell death (or altered cell-cycle activity) in cultured cells — cerebellar granule cells, neutrophils, PC12 cells — plus reduced markers of neuronal apoptosis and improved behavioural outcomes in rodent stress models. Those are real reported effects in cell and animal systems. The chain from there — 'reduces ROS in culture' → 'enters the nucleus and regulates genes' → 'neuroprotective and geroprotective in humans' — is exactly where the evidence thins out and the claims become hypotheses.
Why people reach for it
Potential benefits
Pinealon (EDR) is the Khavinson family's brain-and-CNS peptide. Here's what draws people to it — kept modest, because the evidence under these claims is cell-culture and rodent work from a single research network, not human proof.
- A brain-antioxidant angle people pursue — Pinealon's most concrete result is that in cultured cells it cut the build-up of reactive oxygen species (a marker of oxidative stress) and reduced cell death — which is why people reach for it hoping to buffer the brain against oxidative load.
- Cognitive-maintenance and neuroprotection interest — In rodent stress models (low-oxygen exposure, prenatal stress) it improved some learning and brain-chemistry markers, so it's used in pursuit of clearer thinking and neuronal resilience — early-stage signals, not established human outcomes.
- The 'brain' tile of the bioregulator set — Within Khavinson's one-peptide-per-tissue concept, Pinealon is the CNS-assigned member, which is why longevity-minded users add it when the goal is brain tissue specifically rather than a whole-body effect.
- Pairs with a better-evidenced nootropic — It's commonly stacked with Semax, which carries a stronger independent base for BDNF and neurotrophic support — Pinealon is positioned as the antioxidant layer alongside it, with the honest note that the stack should be judged mostly on Semax's evidence.
- Runs as a short, defined course — Like the rest of the family, Pinealon is used in brief pulsed courses (around 10 days) rather than daily indefinitely — a contained pattern that suits the bioregulator approach.
Sources:PMID 21978084PMID 22567179PMID 34071923
What people reach for Pinealon for, drawn from what the research reports (single-school, cell-culture and rodent only) and how it's used — not proven human outcomes or medical claims.
Implied timing
Best time to dose
Implied best time
Evening
Most people take Pinealon in the evening, on the same pineal-region/circadian logic as the rest of its family — though the lean here is milder than for Epitalon.
- Pinealon is positioned as a pineal-region neuropeptide, and the community times it to the evening to align with the pineal's nighttime activity and the brain's overnight repair window — the same reasoning applied to Epitalon, applied more softly here.
- Evening also fits the practical idea that an antioxidant/neuronal-support signal is useful heading into the low-cortisol, lower-activity overnight stretch when the brain does much of its housekeeping.
- This is a mild preference, not a hard rule: morning dosing is also used, and no study distinguishes the two for Pinealon. There is no published human pharmacokinetic data to sharpen the timing further.
- Because Pinealon is run in short pulsed courses (around 10 days), holding a consistent daily time across the course matters more than the exact hour.
No study establishes an ideal time of day for Pinealon — this is reasoned from its proposed pineal/circadian role and how it's used. As a rule of thumb most peptide dosing lands in the midday-to-evening window; for Pinealon the lean is evening.
How to run it
Dosing & protocol
Pinealon is dosed here as a subcutaneous injection — the form sold as a research peptide and the route the on-page calculator is built for. There is no published human-trial dose for Pinealon; the community convention for Khavinson-class bioregulators runs in short pulsed courses rather than daily indefinitely. Read the numbers below as a map of how practitioners and the longevity community typically approach injectable EDR — not a validated prescription.
No established human dose: Pinealon has no completed independent human trial and no published human dosing data. Evidence is cell-culture and rodent-only, from a single research network with thin outside replication. Every number below is community and practitioner convention for a Khavinson-class bioregulator — not trial-proven.
Dose — community convention (no established human dose)
With no human trial to draw from, the convention for injectable Pinealon is informed by how practitioners dose analogous Khavinson short-peptides.
- Conservative start:
- 100 mcg once daily — the low end used when introducing any experimental neuropeptide; allows observation before escalating.
- Standard convention:
- 100–200 mcg once daily — the most commonly circulated range in practitioner and longevity-community contexts for injectable EDR; not drawn from a trial.
- Upper convention range:
- Up to 300 mcg once daily — sometimes discussed in longer or more intensive courses; no efficacy or safety data supports any ceiling.
Subcutaneous administration
Pinealon is injected into subcutaneous fat; site choice, rotation, and timing are the practical decisions.
- Injection site:
- The abdomen (staying a couple of inches clear of the navel), the love-handle area, or the outer thigh. Rotate sites between doses — using one spot repeatedly risks local irritation and fatty lumps (lipohypertrophy).
- Measuring the dose:
- Drawn on a U-100 insulin syringe from the reconstituted vial; the reconstitution card below converts each dose to syringe units (e.g. 200 mcg = 10 IU at the standard mix), and the calculator handles any vial size.
- Time of day:
- Evening is often preferred — see Best time to dose above — aligning with the peptide's claimed circadian/neuronal role and the general principle of lower ambient cortisol and metabolic activity at night. Morning dosing is also used; no trial data distinguishes them, so a consistent daily time across the course matters more than the exact hour.
- Food window:
- Subcutaneous injection bypasses the gut entirely, so Pinealon can be injected independent of meals.
Cycle & washout — pulsed short courses
The Khavinson-school convention is short pulsed courses, not daily indefinite use — this is the defining feature that sets these bioregulators apart from longer-run peptides.
- Course length:
- ~10 days of daily dosing — the convention most closely associated with Khavinson-class bioregulators in practitioner circles, reflecting the school's own rodent protocols. Some users run slightly longer 14-day courses.
- Washout:
- Follow with a 4–6-week break. The rationale is to prevent receptor or signaling-pathway desensitization and to allow any downstream gene-regulation effects (per the school's hypothesis) to express and settle.
- Repeat cycle:
- 2–4 courses per year is the typical community convention for Khavinson bioregulators; this is not drawn from a trial. Between-course intervals are used to reassess cognitive and energy outcomes.
- Convention caveat:
- These cycle parameters are practitioner convention for the Khavinson class, not a protocol tested in a controlled human study. The short-course pulsed model is widely used within this peptide family; whether it is optimal is unknown.
Reconstitution at a glance — mixing math only
The on-page calculator does this live; the quick reference for a 10 mg vial:
- Mixing:
- 10 mg vial + 2 mL bacteriostatic water = 5,000 mcg per mL. On a 100-unit (1 mL) insulin syringe: 100 mcg = 2 IU · 200 mcg = 4 IU · 300 mcg = 6 IU.
- Alternative dilution:
- 10 mg vial + 5 mL bacteriostatic water = 2,000 mcg per mL. On the same syringe: 100 mcg = 5 IU · 200 mcg = 10 IU · 300 mcg = 15 IU. The higher dilution makes small doses easier to measure precisely.
Substrate the signal needs
Nutritional cofactor precision
Pinealon's proposed job is protecting brain cells from oxidative stress and supporting neuronal function. The most defensible cofactors supply the raw material the brain's antioxidant and energy machinery actually runs on — or come at the circadian/cognitive goal through the behavioural levers with the strongest real-world evidence. This is mechanistic reasoning from the proposed neuroprotective claim, not a Pinealon cofactor study.
Reasoned from Pinealon's proposed antioxidant / neuronal-support mechanism plus neuro-nutrition evidence — not a Pinealon cofactor trial. Supplement doses are common community ranges. The circadian and BDNF lifestyle inputs listed here have stronger independent evidence than Pinealon itself.
Supply the substrate — neuro energy and methylation foundation
Brain cells are metabolically expensive; the B-vitamins and DHA are the structural and biochemical prerequisites for any neuroprotective intervention to act on.
- Omega-3 DHA:
- 1–2 g DHA daily (via fish oil or algal oil) — DHA is the dominant fatty acid in neuronal membranes; adequate membrane composition is the literal substrate for neuronal signaling and resilience. One of Pinealon's rodent models (elevated maternal homocysteine) links to impaired DHA incorporation, making this cofactor particularly direct.
- B6 + B9 + B12 (methylation trio):
- B6 25–50 mg + methylfolate (B9) 400–800 mcg + methylcobalamin (B12) 500–1000 mcg daily — these three run the homocysteine → methionine conversion. Elevated homocysteine is the exact stressor used in one of the Pinealon rodent studies; keeping these vitamins in range addresses the biochemical context, not just general supplementation.
- Magnesium glycinate or L-threonate:
- 200–400 mg elemental magnesium at night — cofactor for hundreds of neuronal enzymes, NMDA receptor regulation, and ATP synthesis; magnesium L-threonate is the form with the highest published brain-entry evidence.
Amplify via proven circadian and BDNF levers
Pinealon is claimed to support circadian and antioxidant tone. The behavioural circadian inputs have genuine, independently replicated evidence; Pinealon's circadian claims do not. Stack the proven levers first.
- Morning light exposure:
- 10–30 minutes of direct outdoor light within 1 hour of waking — the strongest human-evidence circadian anchor; sets the central pacemaker (suprachiasmatic nucleus) and directly modulates cortisol, serotonin, and melatonin rhythms. This is what Pinealon's claimed circadian benefit is competing against in terms of evidence weight.
- Consistent sleep schedule (± 30 min):
- Sleep and wake at the same time daily, including weekends — circadian amplitude is defined by consistency; a drifting schedule flattens the cortisol/melatonin rhythm no supplement corrects. If supporting the brain's antioxidant and repair cycle is the goal, sleep architecture is the primary lever.
- Zone-2 cardiovascular exercise:
- 150–200 min/week moderate aerobic effort — the single most replicated BDNF (brain-derived neurotrophic factor) raiser in humans, with evidence across multiple independent laboratories and longitudinal cohorts. BDNF supports neuronal survival and plasticity — the same downstream goals Pinealon's claims gesture toward, with incomparably stronger evidence.
Mitigate — antioxidant buffer
Pinealon's cell-culture finding is reduced reactive oxygen species. Topping up the dietary antioxidant backbone ensures the peptide is not working in a deficient environment.
- Vitamin C:
- 500–1000 mg daily (ascorbate or buffered form) — water-soluble antioxidant; regenerates vitamin E in cell membranes and maintains the ascorbate level in cerebrospinal fluid, which is held at 10× plasma concentration specifically for neuronal protection.
- Vitamin E (mixed tocopherols):
- 200–400 IU daily as mixed tocopherols (not alpha-tocopherol alone) — fat-soluble antioxidant embedded in neuronal membranes; directly quenches the lipid peroxidation that ROS cause in the same membrane compartment Pinealon's cell-culture signal is attributed to.
Combinations + timing
Stacking notes + timing windows
Pinealon's proposed role is neuroprotection and neuronal-function support via antioxidant tone. The most defensible stack partners come at the same brain-health goal from a genuinely different mechanism — not a second single-school bioregulator pushing the same unproven lever. Pairing two Khavinson peptides doubles the speculation, not the evidence.
All combinations below are reasoned from complementary mechanisms — not regimens studied head-to-head in humans. Pinealon itself has no independent human trial; any stack is doubly unproven. Stacking two single-school Khavinson bioregulators compounds the evidence weakness. Doses are community convention; 'commonly combined for' describes where users go, not a proven indication.
Pinealon + Semax
The most defensible Pinealon pairing — Semax brings better-evidenced BDNF and neurotrophic support; Pinealon adds the proposed antioxidant buffer. Different mechanisms, different evidence standards.
- Why it works:
- Semax (a synthetic ACTH analogue) has a meaningful independent evidence base for BDNF upregulation, neuropeptide signaling, and cognitive-function support in animal and some human studies — significantly better replicated outside a single school than Pinealon. Where Semax drives neurotrophic growth and repair signaling, Pinealon is proposed to provide the antioxidant environment in which that signaling operates. Complementary mechanisms, not the same lever twice.
Pinealon + Epitalon
The classic Khavinson-family brain + aging companion — Epitalon covers the pineal and telomere angle; Pinealon covers the neuronal angle. Use with clear eyes: both are single-school.
- Why it works:
- Epitalon (another Khavinson tetrapeptide) is associated with pineal-gland regulation, melatonin, and telomere-related claims in the same research school. The pairing is popular in longevity communities as a 'Khavinson brain + aging protocol.' Mechanism: Epitalon → circadian/melatonin regulation; Pinealon → neuronal antioxidant and viability support — two tissue roles within the same hypothesis network. The combination logic is internally coherent; the evidence quality of both pieces is equally single-school.
- The protocol:
- Pinealon 100–200 mcg + Epitalon 5–10 mg, both subcutaneously, once daily on a shared ~10-day pulsed course, 2–4 times per year. Typically run as a co-course since both follow the same pulsed-course convention.
- Outcome:
- Commonly combined for broad longevity and cognitive-maintenance goals in Khavinson-aware communities. Honest caveat: this pairing compounds the single-school evidence limitation — both peptides are from the same network, so stacking them does not add independent support for either claim.
Pinealon + BPC-157
A broader neuro-resilience pairing — BPC-157 brings meaningfully better-replicated systemic anti-inflammatory and tissue-resilience data; Pinealon adds the brain-antioxidant proposed layer.
- Why it works:
- BPC-157's evidence base for reducing neuroinflammation, supporting gut-brain-axis integrity, and improving oxidative-stress markers is considerably broader and more independently replicated than Pinealon's. The two peptides are proposed to work on different axes: BPC-157 on systemic repair and inflammation; Pinealon on local neuronal antioxidant tone. Complementary, not redundant — and BPC-157 is the more evidence-supported anchor of the pair.
- The protocol:
- Pinealon 100–200 mcg subcutaneously once daily on its ~10-day course, alongside BPC-157 at 250–500 mcg subcutaneously once daily on its own (typically longer, daily) run. The courses may overlap in the Pinealon-on window without known interaction concerns.
- Outcome:
- Commonly combined for brain resilience, oxidative-load management, and systemic recovery goals. The combination leans on BPC-157's stronger evidence base; the Pinealon addition is the speculative layer.
Reconstitution math
Reconstitution calculator
Reconstitution calculator
Calculated for a 1 mL U-100 insulin syringe (100 units/mL).
Units per dose
20
Draw to this mark on a U-100 syringe
- Volume per dose
- 0.2 mL
- Doses per vial
- 10
- Concentration
- 5 mg/mL
One vial lasts
- Daily
- 10 days
- Every other day
- 20 days
- 5×/week
- 14 days
Research use only. Not for human consumption. Outputs are reference values based on research literature — verify all measurements independently.
From the studies
Side effects from research
There is no meaningful human safety database for Pinealon. The studies are cell-culture and rodent experiments, which cannot characterise side effects, rare events, or long-term risk in people. Absence of reported harm in a handful of small animal studies is not the same as a demonstrated safety profile.
Within those animal and cell models the peptide was generally described as well tolerated, but total human exposure in controlled settings is effectively zero, so nothing can be said with confidence about safety at any dose, over any duration.
Gray-market sourcing adds purity and identity risk independent of the peptide itself. The honest summary: Pinealon's human safety is uncharacterised, not established.
Sources:PMID 21978084
As reported in literature
Research dosing ranges
These are experimental conditions from cell-culture and rodent studies — all from the Khavinson network — shown for reference only. There is no human dose, no approved regimen, and no independent replication. Read the table for what was actually tested (cells and rats) versus what is claimed (human brain protection): the gap is the whole story.
| Dose | Route | Model | Outcome | Sources: |
|---|---|---|---|---|
| In vitro | Cell culture | Cultured cerebellar granule cells, neutrophils, PC12 cells (Khavinson 2011, Rejuvenation Research) | EDR restricted reactive-oxygen-species (ROS) accumulation and decreased cell death / modified cell-cycle activity — a cell-viability signal, not a clinical outcome | PMID 21978084 |
| Maternal dosing | In vivo (rats) | Pregnant rats with elevated homocysteine; offspring assessed (Arutjunyan 2012, Int J Clin Exp Med) | Offspring showed improved learning and reduced cerebellar oxidative stress versus untreated — a rodent behavioural/biochemical signal | PMID 22567179 |
| In vivo | In vivo (aged rats) | Aged rats under acute hypoxic hypoxia; Cortexin + Pinealon (Mendzheritskiĭ 2014, Advances in Gerontology) | Modulated serum cytokines and brain caspase-3 activity — a combination-treatment biochemical readout, not isolated Pinealon efficacy | PMID 25051764 |
| In vitro | Cell model | Mouse Alzheimer's-model cell system (Khavinson 2021, Pharmaceuticals) | EDR (and related tripeptides) reduced dendritic-spine loss and showed neuroprotective effects, framed by the authors as epigenetic regulation — a cell-model signal, single-school | PMID 34071923 |
Quick answers
Frequently asked
What is Pinealon?
It is a trade name for EDR, a synthetic tripeptide (Glu-Asp-Arg) from Vladimir Khavinson's Russian 'Cytogen' line of short peptide bioregulators. It is marketed as a brain/CNS peptide for neuroprotection and cognition. The molecule is well-defined chemically; the brain-health claims are largely single-school and unproven.
Does Pinealon actually protect or rejuvenate the brain?
That is not established. The evidence is cell-culture experiments (reduced oxidative stress and cell death) and rodent stress models (improved learning and brain markers), almost all from one research network with no independent replication and no completed human efficacy trials. Treat neuroprotective and 'anti-aging brain' claims as hypotheses, not facts.
How does it supposedly work?
The Khavinson school proposes that this tiny peptide enters the cell nucleus and directly regulates gene expression. That nucleus-penetration / direct gene-regulation idea is a single-school hypothesis, not independently established molecular biology. What is actually shown is reduced reactive-oxygen-species build-up and cell death in cultured cells.
Is there a known human dose?
No. There is no validated human dose and no completed independent human trial to derive one from. The research uses cell-culture concentrations and rodent dosing, which do not translate to people. The numbers in the dosing section above are community and practitioner convention for Khavinson-class bioregulators — not evidence-based dosing.
Why are Khavinson peptides run in short pulsed courses rather than daily long-term?
This is the conventional pattern within the Khavinson-school community — not a tested pharmacological principle for Pinealon specifically. The reasoning is to prevent receptor or signaling desensitization and allow downstream effects to express between courses. The short-course model (e.g. ~10 days on, weeks off) is widely followed for this peptide class; whether it is optimal is untested.
Is Pinealon approved or independently validated?
No. It is not approved by any major drug regulator, and no independent group outside the Khavinson network has replicated the key findings. Do not read vendor marketing as evidence of Western or independent validation — none was found.
Primary sources
References
- PMID 21978084Khavinson V et al., Rejuvenation Research 2011 — Pinealon restricted ROS accumulation and decreased cell death in cerebellar granule cells, neutrophils, PC12 cells (in vitro)
- PMID 22567179Arutjunyan A et al., Int J Clin Exp Med 2012 — Pinealon in pregnant rats with elevated homocysteine improved offspring learning and reduced cerebellar oxidative stress
- PMID 33396470Khavinson V et al., Molecules 2020 — review/hypothesis: EDR regulation of gene expression relevant to Alzheimer's pathogenesis (no new primary data)
- PMID 34071923Khavinson V et al., Pharmaceuticals (Basel) 2021 — EDR reduced dendritic-spine loss / neuroprotective effects in a mouse Alzheimer's-model cell system
- PMID 25051764Mendzheritskiĭ AM et al., Advances in Gerontology 2014 — Cortexin + Pinealon modulated serum cytokines and brain caspase-3 in aged rats under acute hypoxia (Russian)
- PubChem CID 10273502PubChem record — identity (CID, formula, MW, CAS, sequence; 'Pinealon' and 'Glu-Asp-Arg' on the same record)
Research use only · Not medical advice · Updated 2026-06-01