Compound reference
Pinealon
Also known as EDR, Glu-Asp-Arg
Pinealon (EDR, Glu-Asp-Arg) is a Khavinson "bioregulator" tripeptide marketed as a neuroprotective nootropic. Its antioxidant cell-culture data are concrete, and animal neuroprotection is reported — but the evidence is single-group, the epigenetic mechanism is unproven, and the human cognitive claims are uncontrolled.
- CAS
- 175175-23-2
- Formula
- C₁₅H₂₆N₆O₈
- Molar mass
- ≈418.4 g/mol
- Sequence
- Glu-Asp-Arg (EDR), tripeptide
Research peptide; not an approved drug. Evidence is preclinical and single-group.
Mode of action
Pinealon is the tripeptide glutamyl-aspartyl-arginine (Glu-Asp-Arg, abbreviated EDR), another of the "bioregulator" peptides from Vladimir Khavinson's St. Petersburg Institute of Bioregulation and Gerontology — the same program behind Epitalon and Cartalax. It was designed by analyzing the amino-acid composition of Cortexin, a brain-derived polypeptide preparation, and synthesizing a short defined sequence intended to carry the neuroactive signal.
Its mechanism splits into a concrete part and a speculative part. The concrete part is antioxidant and cytoprotective: in cultured neurons and other cells under oxidative stress, Pinealon dose-dependently restricts reactive-oxygen-species accumulation, reduces necrotic cell death, and shifts the timing of ERK1/2 signaling and the cell cycle. The speculative part is the group's general epigenetic model — that EDR penetrates the nucleus and binds histones or DNA in a sequence-specific way (with reported preferences for certain promoter regions) to regulate the expression of neuronal genes such as those governing calcium-channel function and apoptosis. As with the other Khavinson peptides, that DNA/histone-binding mechanism is advanced largely by one research network and has not been independently established.
Main intended effect
Neuroprotection and cognitive support — framed as antioxidant, anti-apoptotic protection of neurons and improvement of memory and attention.
Areas of interest
Pinealon is marketed as a neuroprotective nootropic, with research interest spanning cognitive aging and decline, Alzheimer's disease (mechanistic and model studies), and protection of the developing or stressed brain (prenatal hyperhomocysteinemia, hypoxia, diabetes-related models). It has also been studied in athletes for antioxidant and adaptation effects. It is sold as a research peptide for cognition and "brain longevity."
Evidence for intended effects
Pinealon has a more concrete anchor than Cartalax: its antioxidant, cell-protective activity in oxidatively stressed neurons and other cells is a real, repeatable in-vitro finding. Animal work extends this — Pinealon given to pregnant rats improved the cognition of offspring exposed to prenatal hyperhomocysteinemia and made their cerebellar neurons more stress-resistant, and the peptide has shown neuroprotection in hypoxia models. In an Alzheimer's mouse model, EDR helped preserve dendritic spines, and docking analyses link it to Alzheimer's-relevant gene promoters.
But the same limitations recur. Essentially all of this comes from one connected research tradition, with little independent replication. The human cognitive claims — improved memory, attention, and emotional state in older adults, and antioxidant gains in athletes — derive from uncontrolled or non-randomized reports in that same literature, not from rigorous independent trials. There is no Western regulatory approval and no modern randomized controlled trial. The antioxidant biology is plausible; the leap to a proven cognitive therapy is not supported.
| Strand | What exists | Tier |
|---|---|---|
| Antioxidant / cytoprotection | Dose-dependent ROS suppression in neurons (in vitro) | Concrete preclinical |
| Animal neuroprotection | Prenatal hyperhomocysteinemia, hypoxia, AD-mouse spine rescue | Preclinical (single tradition) |
| Mechanism | Proposed DNA/histone binding, gene regulation | Hypothesis (not independently established) |
| Human cognition | Uncontrolled reports in older adults / athletes | Weak / uncontrolled |
Studied amounts (literature dosing context)
The in-vitro studies used Pinealon at cell-culture concentrations; the animal studies used injected doses in rodents; and the group's human reports describe oral courses. None of these establish an approved or validated human dose. These are study figures from preclinical and uncontrolled work, and this page does not provide dosing guidance.
Safety and regulatory status
The Khavinson literature describes Pinealon, like its sibling peptides, as well tolerated and free of side effects — a claim that carries the same caveat as the efficacy data, since it comes from the same single network and largely uncontrolled settings rather than formal safety studies. Pinealon is not an approved drug in any jurisdiction; it is sold as a research peptide and nootropic. As with other gray-market peptides, products labeled "Pinealon" are of unverified identity and purity. It is best understood alongside Epitalon and Cartalax as part of the same bioregulator family, sharing both their proposed mechanism and their lack of independent, controlled human evidence.
Sources
Pinealon Increases Cell Viability by Suppression of Free Radical Levels and Activating Proliferative Processes
In vitro study (Khavinson, Ribakova and colleagues, Rejuvenation Research 2011) of the synthetic tripeptide Pinealon (Glu-Asp-Arg) in cerebellar granule cells, neutrophils, and PC12 pheochromocytoma cells under oxidative stress. Pinealon produced a dose-dependent reduction in reactive-oxygen-species accumulation, decreased necrotic cell death, delayed the time course of ERK1/2 activation, and modified the cell cycle. This is the most concrete in-vitro evidence for Pinealon's antioxidant and cytoprotective activity. The work is a cell-culture study from the originating research group; in-vivo and human relevance require separate evidence.
Pinealon protects the rat offspring from prenatal hyperhomocysteinemia
Animal study (Arutjunyan, Kozina and colleagues, International Journal of Clinical and Experimental Medicine 2012) testing the tripeptide Pinealon (Glu-Asp-Arg) in a rat model of prenatal hyperhomocysteinemia induced by maternal methionine loading. Offspring of treated dams showed improved spatial orientation and learning, and their cerebellar neurons were more resistant to oxidative stress, which the authors interpret as in-vivo confirmation of Pinealon's neuroprotective and antioxidant properties. The findings are from a single-group rodent model and have not been independently replicated or tested in humans.
EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer's Disease
Mechanistic review (Khavinson, Linkova, Kozhevnikova, Trofimova; Molecules 2021) proposing how the EDR peptide (Glu-Asp-Arg, Pinealon) — conceptually derived from the brain-peptide complex Cortexin — may exert neuroprotection relevant to Alzheimer's disease. The authors advance the group's hypothesis that EDR enters cells, binds histone proteins and/or nucleic acids, and thereby regulates gene expression and protein synthesis (for example through the MAPK/ERK pathway and antioxidant enzymes), reducing neuronal apoptosis. The model is mechanistically detailed but originates from a single research network, and the proposed DNA/histone-binding action is not independently established.
Neuroprotective Effects of Tripeptides—Epigenetic Regulators in Mouse Model of Alzheimer's Disease
Study (Khavinson and colleagues, Pharmaceuticals 2021; a correction was published in 2025) testing the tripeptides EDR (Pinealon) and KED in the 5xFAD transgenic mouse model of Alzheimer's disease, paired with molecular-docking analysis. The peptides prevented loss of dendritic spines and neuroplasticity impairment, and docking placed EDR binding sites in the promoter regions of genes implicated in Alzheimer's pathology, including CASP3, NES, GAP43, APOE, SOD2, PPARA, and PPARG. The work supports a neuroprotective, gene-regulatory model, but it comes from the originating research network and pairs an animal model with computational predictions rather than direct mechanistic proof in humans.
Peptide Regulation of Gene Expression: A Systematic Review
Systematic review (Khavinson, Popovich, Linkova, Mironova, and Ilina, Molecules 2021) from the St. Petersburg Institute of Bioregulation and Gerontology summarizing the group's body of work on short di-, tri-, and tetrapeptide "bioregulators," including AED (Cartalax) — which it associates with regulation of cartilage and skin-fibroblast function and neuronal-cell differentiation — and AEDG (Epitalon). The review advances the group's central hypothesis that such peptides penetrate cells, enter the nucleus, and bind DNA or histones to regulate gene expression. It is the most consolidated statement of the bioregulator program, but the underlying primary evidence is largely in vitro and originates from a single research network, and the proposed DNA-binding mechanism is not independently established.