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Pinealon

Tier 3 · Reported use
Also known as EDR peptide · Glu-Asp-Arg

The strongest evidence present is Tier 1: small unblinded human observational studies from the Khavinson/St. Petersburg research network (e.g., 32-, 72-, 110-participant reports). However, sources uniformly note there are zero PubMed-indexed human RCTs, no registered clinical trials, and no independent Western replication — nearly all published work originates from a single interconnected research network. Mechanistic support is largely in-vitro, animal, and computational/theoretical. Some efficacy percentages come from a single low-tier marketing profile, and several commonly cited findings concern different peptides.

Half-life
Not recorded
Routes
Subcutaneous injection · Intramuscular injection · Oral / sublingual
Goals
cognitive · longevity
Cost / mg
Not recorded

How it works

Sources describe Pinealon as a synthetic three-amino-acid peptide (Glu-Asp-Arg, abbreviated EDR) from the Russian 'peptide bioregulator' school associated with Vladimir Khavinson. Vendor and review sources propose that its main proposed action is entering cells and interacting directly with DNA to influence which genes are switched on, particularly genes tied to neuronal function, antioxidant defense and apoptosis(vendor claim). In-vitro and animal reports describe it limiting reactive-oxygen-species buildup and reducing cell death under oxidative stress and low-oxygen conditions, though sources caution that many of these mechanisms are theoretical and that its blood-brain-barrier penetration and proposed pineal/melatonin and serotonin effects have not been confirmed by receptor-binding studies. Notably, sources disagree on whether it is antioxidant or pro-oxidant.

Overview

What Pinealon Is

Multiple vendor profiles describe Pinealon (aliases: EDR peptide, Glu-Asp-Arg) as a synthetic linear tripeptide with the sequence L-glutamyl-L-aspartyl-L-arginine, abbreviated EDR13. One profile notes that two of its three residues (glutamate and aspartate) carry negatively charged carboxylate side chains at physiological pH, while arginine carries a positively charged guanidinium group.

Sources list its molecular weight as approximately 418 Da (variously 418.40 or 418.41 g/mol), with molecular formula given as C15H25N5O8 or C15H26N6O8; one source instead cites ~404 or 461 Da. Profiles report that PubChem resolves 'pinealon' and 'Glu-Asp-Arg' to CID 10273502, that the US National Library of Medicine controlled vocabulary maps 'pinealon' to Glu-Asp-Arg, and that CAS number 175175-23-2 is assigned — though one lower-tier source instead lists CAS 409740-19-4.

Origin

Sources state Pinealon emerged from the Russian 'peptide bioregulator' school associated with Vladimir Khavinson and the St. Petersburg Institute of Bioregulation and Gerontology. One profile states it was isolated from Cortexin, a polypeptide neuroprotective complex derived from bovine and porcine brain tissue — a description that conflicts with profiles calling it a fully synthetic tripeptide. Profiles note that the closely named Lys-Glu-Asp (KED), sold as Vesugen, is a distinct compound.

Regulatory & Research Status

Sources characterize Pinealon as an investigational research chemical marketed as a brain/cortex-oriented bioregulator and, in Russia, as a 'Cytogen'-class supplement, while noting it is not an approved drug for any indication in any country. Sources uniformly state it is not FDA-approved for any human use (as of May 2026 per one source), has no regulatory classification as a bulk drug substance for U.S. compounding, is sold under research-use-only labeling, and as of April 2026 was not available through licensed U.S. providers.

One profile notes that most published research comes from a small interconnected network of authors, journals and institutions — appearing frequently in Advances in Gerontology, Bulletin of Experimental Biology and Medicine, Biochemistry (Moscow) and Rejuvenation Research with overlapping author lists. One profile reports a PubMed query returned 22 records total as of July 2026; another counts 15 published studies (8 human, 5 animal, 3 in-vitro, 2 reviews) with 0 registered clinical trials.

Reported Mechanisms

A review7 describes EDR as possessing neuroprotective properties, activating gene expression and synthesis of proteins that maintain neuronal function, and reducing apoptosis in vitro and in vivo; it reports EDR interferes with elimination of dendritic spines in neuronal cultures from mice modeling Alzheimer's and Huntington's diseases and promotes antioxidant-enzyme synthesis in rat cerebellum neuron cultures. A 2011 cellular study12 reported that fluorescein-labeled Pinealon penetrates the cytoplasm, nucleus and nucleolus of HeLa cells and interacts specifically with DNA, preferentially binding CNG- and CAG-containing sequences and recognizing cytosine methylation status; the authors concluded such interactions could epigenetically control gene activity. A computational study8 reported EDR can partly enter the DNA major groove near guanine N7/O6, aided by Mg ion screening of DNA phosphates.

In-vitro studies3,13 reported dose-dependent restriction of ROS accumulation in cerebellar granule cells, neutrophils and PC12 cells under oxidative stress, decreased necrotic cell death, a delayed ERK1/2 activation time course and cell-cycle modification, concluding direct interaction with the cell genome. Rat studies2 reported that Pinealon given to pregnant rats in a prenatal hyperhomocysteinemia model improved offspring spatial orientation and learning and reduced ROS and necrotic neurons. Another study11 reported increased neurogenesis under hypoxia, reduced neuroinflammation in old rats, and effects on brain caspase-3 and serum IL-6/TNF.

Several proposed mechanisms are explicitly theoretical: profiles propose Pinealon modulates pineal function and melatonin/circadian regulation and influences serotonin synthesis, while cautioning no receptor-binding study has confirmed pineal modulation; molecular docking suggesting EDR binds the tryptophan-5-hydroxylase promoter is noted as experimentally unvalidated.

Reported Human Findings

A study in 32 people aged 41-831 reported significant anabolic effects, improved CNS activity and slowed biological-age indicators, while noting Vesugen showed a more visible geroprophylactic effect. A study of 110 people9 reported a positive impact on biological-age indicators, with the most pronounced effect from combined Pinealon and Vezugen use, and characterized oligopeptide drugs including Pinealon as among the safest interventions studied. A 72-patient study in adults aged 30-74 dosed 0.2 mg twice daily for 20-30 days reported improved memory, reduced headache severity and enhanced emotional stability versus controls, with improvement in 59.4% of subjects with traumatic-brain-injury consequences. One profile explicitly notes that the 32- and 72-participant studies lacked double-blind, placebo-controlled designs. Separately, one profile reports Pineamin increased urinary 6-sulfatoxymelatonin excretion 1.9x in 55 elderly patients with diminished pineal function. One promotional profile claims 'clinical studies' showed 30% better memory retention, 50% improvement on attention tasks, 40% reduction in neurodegeneration markers and 35% lower MDA in 60 adults aged 45-65 — figures that appear only in that single marketing profile with no citation to a verifiable trial.

Studied and Marketed Uses

Sources describe Pinealon's studied and marketed uses as neuroprotection, cognitive enhancement, brain aging/memory, longevity, and circadian/sleep support, emphasizing these benefits are experimental and not proven in large human trials. The authors of the 32-person study1 described Pinealon in their report as a geroprotector, anabolic and neuroprotective (non-antioxidant type) agent and proposed it as a candidate for slowing aging in patients with organic brain syndrome.

What the research shows

90 findings extracted from the 16 sources cited below, strongest evidence first within each group. Every one links to the source it came from.

What human studies found

Based on 7 human study findings, 8 animal findings and 2 in vitro findings.

  • human studyPinealon has significant anabolic effects1

  • human studyPinealon improved the activity of the Central nervous system and other vital organs1

  • human studyPinealon slows the rate of aging by biological age indicators1

  • human studyVesugen demonstrated more visible geroprophylactic effect than Pinealon1

  • human studyPinealon caused decrease of markers CD34+ positive hematopoietic polypotent cells in blood with significant inhibition of hemopoiesis1

  • human studyEDR peptide improves memory issues in elderly patients7

  • human studyPinealon (Oligopeptide preparation containing glutamyl-asparagin-arginine complex) had positive impact on indicators of biological age9

  • animalPinealon (Glu-Asp-Arg) administration to pregnant rats loaded with methionine improved their offspring spatial orientation and learning ability2

Show 9 more findings
  • animalPinealon (Glu-Asp-Arg) improved offspring cognitive function in rats with experimental hyperhomocysteinemia caused by dietary methionine loading during pregnancy2

  • animalPinealon administration to pregnant rats loaded with methionine improved offspring spatial orientation and learning ability2

  • animalArginine-enriched peptides from seabuckthorn seed protein reverse learning and memory impairment in d-galactose-induced brain aging in mice6

  • animalOral administration of arginine-enriched peptides significantly reversed learning and memory impairment symptoms in Morris water maze and step-down tests6

  • animalEDR peptide normalizes behavioral responses in animal studies7

  • animalPeptides (3,6,10)a,b at 5micromol/kg reduced thrombus weights in rat model by 15-40%14

  • animalAspirin achieved comparable activity at dosage of ca. 110micromol/kg in rat anti-thrombotic model14

  • in vitroPinealon decreases necrotic cell death measured by the propidium iodide test3

  • in vitroGlu-Asp-Arg (EDR), Lys-Glu-Asp (KED), and Ala-Glu-Asp-Gly (AEDG) peptides have previously demonstrated neuroprotective effects in various models of Alzheimer's disease5

How it works

Based on 1 human study finding, 17 animal findings, 36 in vitro findings and 11 theoretical findings.

  • human studyPinealon showed prooxidant activity through chemiluminescence1

  • animalPinealon administration decreased reactive oxygen species accumulation in neurons isolated from the cerebellum of offspring developed under prenatal hyperhomocysteinemia2

  • animalPinealon administration decreased the number of necrotic cells in the population of neurons isolated from the cerebellum of offspring developed under prenatal hyperhomocysteinemia2

  • animalCerebellum neurons from pinealon-treated offspring became more resistant to oxidative stress2

  • animalPinealon made cerebellum neurons more resistant to oxidative stress in offspring of rats with prenatal hyperhomocysteinemia2

  • animalPinealon decreased reactive oxygen species accumulation in neurons isolated from cerebellum of offspring developed under prenatal hyperhomocysteinemia2

  • animalPinealon decreased the number of necrotic cells in cerebellar neuron populations from offspring under prenatal hyperhomocysteinemia2

  • animalArginine-enriched peptides increased activation of endothelial nitric oxide synthase and neuronal NO synthase in hippocampus6

Show 57 more findings
  • animalArginine-enriched peptides decreased inducible NO synthase in hippocampus6

  • animalArginine-enriched peptides normalized serum inflammatory cytokine levels (NF-κB, TNF-α, IL-6)6

  • animalArginine-enriched peptides suppressed the Arg-inducible nitric oxide pathway6

  • animalEDR peptide reduces the intensity of apoptosis in in vitro and in vivo studies7

  • animalPinealon (Glu-Asp-Arg) increases neurogenesis in brain conditions of hypoxia11

  • animalPinealon decreases neuroinflammatory reactions to a reference level under sharp hypoxic hypoxia in old rats11

  • animalPinealon affects caspase-3 activity in the brain under sharp hypoxic hypoxia11

  • animalPinealon affects interleukin-6 levels in blood serum under sharp hypoxic hypoxia in old rats11

  • animalPinealon affects tumor necrosis factor in blood serum under sharp hypoxic hypoxia in old rats11

  • animalAnti-thrombotic activity of nano-particles [(3,6,10)a,b]-Cu(II) increased by 100-fold over corresponding peptides14

  • in vitroPinealon has neuroprotective properties confirmed in vitro2

  • in vitroPinealon has neuroprotective properties confirmed in previous in vitro experiments2

  • in vitroThe synthetic tripeptide pinealon (Glu-Asp-Arg) demonstrates dose-dependent restriction of reactive oxygen species (ROS) accumulation in cerebellar granule cells, neutrophils, and pheochromocytoma (PC12) cells3

  • in vitroPinealon restricts ROS accumulation induced by oxidative stress stimulated by receptor-dependent or -independent processes3

  • in vitroThe protective effect of pinealon is accompanied with a delayed time course of ERK 1/2 activation and modification of the cell cycle3

  • in vitroRestriction of ROS accumulation and cell mortality is saturated at lower concentrations, whereas cell cycle modulation continues at higher concentrations of pinealon3

  • in vitroPinealon is able to interact directly with the cell genome3

  • in vitroAll peptides promote the arborization of the dendritic tree, increasing both the number of primary processes and the total length of dendrites5

  • in vitroTripeptides have no effect on the activity of mitochondria and lysosomes and the level of p16 protein in induced neurons5

  • in vitroEDR peptide reduces oxidative DNA damage in induced neurons derived from elderly donor fibroblasts5

  • in vitroShort peptides partially protect induced neurons from age-related changes and stimulate dendritogenesis in neurons5

  • in vitroEDR peptide (Glu-Asp-Arg) possesses neuroprotective properties7

  • in vitroEDR peptide activates gene expression and synthesis of proteins involved in maintaining neuronal functional activity7

  • in vitroEDR peptide interferes with the elimination of dendritic spines in neuronal cultures from mice with Alzheimer's and Huntington's diseases7

  • in vitroEDR peptide promotes activation of antioxidant enzyme synthesis in culture of cerebellum neurons in rats7

  • in vitroEDR (Glu-Asp-Arg) can partly penetrate into the major groove of DNA8

  • in vitroEDR affects the base atoms, mainly the N7 and O6 of guanine8

  • in vitroMg ions can promote DNA-EDR interaction due to their effective screening of the negatively charged phosphate groups of DNA8

  • in vitroThe action of Mg ions in promoting DNA-EDR interaction remains in salted solution8

  • in vitroPinealon (Glu-Asp-Arg) shows marked fluorescence in cytoplasm, nucleus, and nucleolus in HeLa cells after incubation with fluorescein isothiocyanate-labeled peptide12

  • in vitroShort biologically active peptides like pinealon are able to penetrate into an animal cell and its nucleus and may interact with various components of cytoplasm and nucleus including DNA and RNA12

  • in vitroPinealon differently affects the fluorescence of 5,6-carboxyfluorescein-labeled deoxyribooligonucleotides and DNA-ethidium bromide complexes compared to other peptides12

  • in vitroPinealon shows specific interaction with nucleic acid structures and discriminates between different nucleotide sequences and recognizes cytosine methylation status12

  • in vitroPinealon preferentially binds with deoxyribooligonucleotides containing CNG sequence (CNG sites are targets for cytosine DNA methylation in eukaryotes)12

  • in vitroPinealon preferentially binds with CAG-containing sequences12

  • in vitroSite-specific interactions of pinealon with DNA can control epigenetically cell genetic functions and play a role in regulation of gene activity12

  • in vitroPinealon demonstrates dose-dependent restriction of reactive oxygen species (ROS) accumulation in cerebellar granule cells, neutrophils, and pheochromocytoma (PC12) cells13

  • in vitroPinealon's ROS-restricting effect occurs in oxidative stress induced by receptor-dependent or -independent processes13

  • in vitroPinealon decreases necrotic cell death measured by propidium iodide test13

  • in vitroPinealon's protective effect is accompanied with delayed time course of ERK 1/2 activation13

  • in vitroPinealon causes modification of the cell cycle13

  • in vitroPinealon is able to interact directly with the cell genome13

  • in vitroCu(II)-peptide complexes assembled into stable nano-particles surrounded by negative charges in normal saline14

  • in vitroCu(II)-peptide complexes had zeta potential ranging from -4.102 to -9.825mV14

  • in vitroCu(II)-peptide complexes had diameters ranging from 212.1+/-4.0 to 632.4+/-36.7nm in normal saline14

  • in vitroTEM analysis showed compounds remained as nano-globes in solid state with diameters ranging from 15 to 20nm14

  • theoreticalPinealon targets circadian and mitochondrial regulators4

  • theoreticalTherapeutic peptides modulate molecular signaling networks central to cellular medicine4

  • theoreticalPeptides act on key pathways such as PI3K/Akt, mTOR, MAPK, TGF-β, and AMPK to exert influence over tissue regeneration, inflammation resolution, and neuromuscular recovery4

  • theoreticalEDR peptide is assumed to enter cells and bind to histone proteins and/or ribonucleic acids7

  • theoreticalEDR peptide can change the activity of the MAPK/ERK signaling pathway7

  • theoreticalEDR peptide affects synthesis of proapoptotic proteins (caspase-3, p53)7

  • theoreticalEDR peptide affects proteins of the antioxidant system (SOD2, GPX1)7

  • theoreticalEDR peptide affects transcription factors PPARA, PPARG, serotonin, calmodulin7

  • theoreticalPeptide Lys-Glu is an immunomodulatory peptide that modulates life span by modulating irisin gene expression10

  • theoreticalPeptide Glu-Asp-Arg is a neuroprotective peptide that modulates life span by modulating irisin gene expression10

  • theoreticalPeptides Lys-Glu, Glu-Asp-Arg, and Ala-Glu-Asp-Gly play a role in epigenetic regulation of irisin content10

Dosing

Based on 1 animal finding and 2 in vitro findings.

  • animalCu(II)-peptide complexes [(3,6,10)a,b]-Cu(II) required dosage of 0.05micromol/kg for anti-thrombotic activity14

  • in vitroRestriction of ROS accumulation and cell mortality is saturated at lower concentrations of pinealon13

  • in vitroCell cycle modulation by pinealon continues at higher concentrations13

Safety and side effects

Based on 2 human study findings.

  • human studyPinealon did not affect the degree of chromatin condensation and is safe on nuclear genetic level1

  • human studyOligopeptide drugs (including Pinealon) were among the most safe interventions regarding influence on biochemical and immunological parameters and clinical condition of patients9

What people use it for

Based on 1 human study finding and 1 expert opinion finding.

  • human studyCombined use of Pinealon and Vezugen (two Oligopeptide complexes) showed the most pronounced positive impact on indicators of biological age9

  • expert opinionPinealon is recommended for use as a geroprotector anabolic neuroprotective no antioxidant type for reducing the rate of aging in patients with organic brain syndrome1

Other findings

Based on 1 in vitro finding.

  • in vitroPinealon (Glu-Asp-Arg) is a synthetic tripeptide13

Points of contention

Where the evidence is unsettled, thin, or says less than the popular claim — worth knowing before you draw conclusions.

Limited evidence

Evidence base is almost entirely preclinical and comes from one research network

Multiple sources state Pinealon has zero PubMed-indexed human RCTs and no Western clinical trials, with essentially all published research originating from Khavinson's group and affiliated institutions and not independently replicated. Human data are limited to small unblinded observational reports (e.g., 32, 55, 72, 110 participants).

Contested

Sources disagree on whether Pinealon is antioxidant or pro-oxidant

Several in vitro and animal reports describe Pinealon restricting ROS and upregulating antioxidant enzymes (SOD2, GPX1), yet a tier-1 human study and a tier-3 profile report detected pro-oxidant/prooxidant activity by chemiluminescence, and the tier-1 study classifies it as a 'no antioxidant type' agent.

Contested

Blood-brain barrier penetration is unproven and molecular weight figures conflict

Vendor profiles claim membrane and BBB penetration, but tier-3 profiles state no study has demonstrated how the tripeptide crosses the BBB in pharmacologically relevant quantities, noting the BBB typically excludes molecules above 400-500 Da. Reported molecular weights also vary (~404, 418.40/418.41, and 461 Da) and molecular formulas differ (C15H25N5O8 vs C15H26N6O8), as do CAS numbers (175175-23-2 vs 409740-19-4).

Single source

Percentage efficacy figures come from one low-tier marketing profile

Claims of 30% memory retention increase, 50% task improvement, 40% neurodegeneration-marker reduction and 35% MDA decrease in 60 adults appear only in a single tier-3 marketing profile (Pinealon Peptide | Brain & Memory Support) with anecdotal grounding and no citation to a verifiable trial.

Other

Some cited sources concern different peptides, not Pinealon

Effect of seabuckthorn seed protein and its arginine-enriched peptides on combating memory impairment in mice. studies arginine-enriched seabuckthorn peptides and Synthesis, nano-scale assembly, and in vivo anti-thrombotic activity of novel short peptides containing L-Arg and L-Asp or L-Glu. studies Cu(II)-peptide nanoparticle anti-thrombotics; neither is about Pinealon (Glu-Asp-Arg) specifically, so their findings should not be attributed to Pinealon. Also, the telomerase-induction finding sometimes associated with this school is an Epithalon result never replicated for Pinealon.

Other

Conflicting descriptions of origin and mechanism target

Some profiles describe Pinealon as isolated from Cortexin (brain-tissue complex) and as pineal-derived, while others describe it as a fully synthetic tripeptide targeting cortical/pineal tissue; claims of direct pineal/melatonin and serotonin modulation are labeled theoretical and unconfirmed by receptor-binding studies.

Using it with other compounds

  • SemaxComplementary

    No documented conflict

    Both support neuroprotection and neurogenesis but by completely different mechanisms — Semax via BDNF/TrkB neurotrophin signaling and Pinealon via proposed direct gene/DNA regulation and antioxidant enzyme upregulation. Different upstream targets converging on neuronal survival make this a plausibly complementary neuroprotective pairing.

    Tier 4Theoretical — not established

    Shares neurogenesis

  • VilonSame mechanism

    Worth caution

    Vilon is another ultra-short Khavinson bioregulator that, like Pinealon, is proposed to act without a membrane receptor by binding gene-promoter DNA and remodeling chromatin. They target different systems on paper (Vilon skews immune/geroprotective, Pinealon neuroprotective), but the entire underlying 'peptide binds DNA to reactivate genes' mechanism is shared and rests on modeling/in-vitro claims. Understand that combining them does not give you two independent, well-validated tools — it gives you two peptides resting on the same unproven premise.

    Tier 4Theoretical — not established
  • EpithalonSame mechanism

    Worth caution

    Both are short Khavinson-school 'peptide bioregulators' proposed to act by binding DNA/histones and switching gene expression rather than a membrane receptor, and both are pitched as neuroprotective/neurogenic with effects on circadian and melatonin biology. Because they share the same class and proposed mechanism, running them together is largely redundant rather than additive — pick one for your goal rather than stacking two overlapping bioregulators.

    Tier 4Theoretical — not established
    What the research doesn't establish
    Although both are short peptides proposed to bind DNA or histones, that shared hypothesis does not establish they act through the same downstream pathways. Epithalon's documented mechanism centers on telomerase/hTERT and senescence markers (p16/p21), whereas Pinealon acts via MAPK/ERK, caspase-3/p53 apoptotic signaling, and antioxidant enzymes; their circadian, melatonin, and neurogenic effects are not shown to converge.

    Shares neurogenesis

  • CerebrolysinComplementary

    No documented conflict

    Pinealon is a short bioregulator peptide reported to reduce neuronal oxidative stress and apoptosis and support dendritic/neuroplastic changes, overlapping with Cerebrolysin's neurogenic and neuroprotective goal via a different (proposed gene-regulatory) mechanism. Combination is anecdotal.

    Tier 4Theoretical — not established

    Shares neurogenesis

  • P21Complementary

    Worth caution

    Both report enhanced dendritic arborization, synaptic plasticity and neurogenesis. P21 drives BDNF/TrkB and PI3K/Akt–GSK-3β signaling, while Pinealon is proposed to reach similar endpoints via gene-expression/ERK modulation. The distinct mechanisms pointing at the same plasticity outcome make them complementary in principle, with only preclinical/anecdotal support for combining.

    Tier 4Theoretical — not established

    Shares neurogenesis

Safety and side effects

Safety Overview

Some profiles report no serious adverse effects documented at standard doses and only rare local injection-site reactions in the Russian clinical literature — but this reassurance is contradicted by the single strongest human study (the tier-1 polymorbidity report; see 'Contested Oxidative Effects' below), which found a decrease in CD34+ hematopoietic polypotent cells in blood with significant inhibition of hemopoiesis (blood-cell formation). Profiles otherwise state the safety profile is entirely unknown — with no Phase I data, uncharacterized long-term repeated-cycle safety, and theoretical risks of endocrine disruption via pineal modulation and immune reactions from peptide immunogenicity. One profile states Pinealon has not been studied in any formal pharmacokinetic drug-drug interaction trial in humans.

Contested Oxidative Effects

Sources disagree on whether Pinealon is antioxidant or pro-oxidant. Several in-vitro and animal reports describe it restricting ROS and upregulating antioxidant enzymes (SOD2, GPX1)2,3, yet a tier-1 human study1 reported it showed pro-oxidant activity by chemiluminescence and caused a decrease of CD34+ hematopoietic polypotent cells in blood with significant inhibition of hemopoiesis — while noting it did not affect chromatin condensation and was considered safe at the nuclear genetic level, and classifying it as a 'no antioxidant type' agent. One additional profile likewise states some pro-oxidant activity has been detected, warranting monitoring.

Key Uncertainties

  • Blood-brain-barrier penetration is unproven. Vendor profiles assert high water solubility, selective pineal uptake and transit across lipid bilayers including nuclear membranes, but tier-3 profiles caution no study has demonstrated how the tripeptide crosses the BBB in pharmacologically relevant quantities, noting the BBB typically excludes molecules above 400-500 Da(vendor claim) — a range in which Pinealon's conflicting reported weights (~404, 418, 461 Da) fall.
  • Evidence is nearly all preclinical and single-network. Multiple sources note zero PubMed-indexed human RCTs and no Western trials; human data are limited to small unblinded observational reports (32, 55, 72, 110 participants) from Khavinson's group and affiliates, not independently replicated.
  • Efficacy percentages are from one marketing source. The 30%/50%/40%/35% figures appear only in a single tier-3 promotional profile with no verifiable citation.
  • Some cited findings concern different peptides. Sources caution that certain literature (arginine-enriched seabuckthorn peptides; Cu(II)-peptide nanoparticles) and the telomerase-induction result associated with this school (an Epithalon finding) should not be attributed to Pinealon.

Not FDA-approved for any human use; sold under research-use-only labeling.

Reconstitution and handling

Dosing

No dose has been established for this compound. No regulatory label exists for Pinealon — sources uniformly state it is not FDA-approved for any human use and is sold under research-use-only labeling. One profile explicitly notes no published human dose-ranging or pharmacokinetic study of Pinealon exists. The figures below are what sources report, not guidance.

  • One low-tier vendor profile lists biohacker/research dosing as 100-300 mcg subcutaneously daily for 10-20 days, repeated 2-3 times per year.
  • Another profile cites 200 mcg per day in 10-to-20-day courses, described as equivalent to about 3 units on an insulin syringe.
  • One low-tier vendor profile lists indication-specific doses of 100-300 mcg per injection: 200 mcg neuroprotection, 300 mcg cognitive enhancement, 100 mcg circadian support, 250 mcg anti-aging, 200 mcg neuroendocrine, 200 mcg synaptic plasticity (all from one low-tier vendor profile) — dosed 10-20 days on, repeated every 3-6 months, subcutaneous as primary route.
  • One low-tier vendor profile describes a subcutaneous protocol at 1.0-2.0 mg/day (ranges given as 5-10 mg), 10-20 day cycles (up to 28 days extended) with 2-3 months off, and a sample titration of 1.0 mg days 1-5, 1.5 mg days 6-14, 2.0 mg days 15-20; the same profile lists 20 mg/day for the oral route.
  • One low-tier vendor profile describes Russian clinical dosing for post-stroke and age-related cognitive decline as 0.5-2 mg intramuscularly for 10-14 days per neurologist, and Russian retail sublingual/oral dosing as drops or capsules 3-4x/day for 30 days, 3x/year.
  • Human observational reports used, for example, 0.2 mg twice daily for 20-30 days (72-patient study) and a cited 5 mg daily protocol; an animal study cited a 100 ng/kg optimal dose for spatial learning.

Routes reported across sources include subcutaneous injection (described as the more common research route), intramuscular injection, and oral/sublingual (the route used in most published Russian-language clinical reports).

Reconstitution & Preparation

These are container calculations reported by profiles, not dose recommendations:

  • One profile notes the common research vial size is 20 mg lyophilized powder. Its protocol reconstitutes a 20 mg vial with 3.0 mL bacteriostatic water, yielding 6.67 mg/mL, so 1 unit (0.01 mL) on a U-100 insulin syringe ≈ 66.7 mcg; example draws given as 15 units (0.15 mL) for 1.0 mg, 22.5 units (0.225 mL) for 1.5 mg, and 30 units (0.30 mL) for 2.0 mg.
  • Another profile states a 10 mg vial reconstituted with 2 mL bacteriostatic water yields 5 mg/mL (5,000 mcg/mL), with 0.04 mL ≈ 4 units on a U-100 syringe.

Storage

One profile states lyophilized stock is stable at −20 °C for years (per another source up to 24 months), cites HPLC purity ≥98%, and advises that reconstituted peptide be refrigerated at 2-8 °C and discarded at 28 days.

The reported doses differ by up to two orders of magnitude — this is not a formatting quirk. The microgram figures (roughly 100–300 mcg/day) and the milligram figures (1–2 mg/day subcutaneously, ranges to 5–10 mg, and 20 mg/day orally) come from different low-tier vendor sources and are not reconciled anywhere in the published literature. Because no human dose-ranging or pharmacokinetic study of Pinealon exists, there is no evidence base for choosing between them. Someone following a milligram-level protocol would be taking roughly 10–100 times what the microgram sources describe, so the higher figures warrant particular caution.

Sources

Ordered by evidence quality — the strongest first.

  1. Constitutive activity in gonadotropin receptors.(opens in a new tab)
    Tier 4PubMed · pubmed.ncbi.nlm.nih.gov · 2014

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