Chemistry data
- Class
- synthetic tripeptide bioregulator
- Molecular weight
- 418.41 g/mol
- Sequence
- Glu-Asp-Arg
- Half-life
- short (minutes); biological effects persist beyond clearance
- Routes
- intraperitoneal · intranasal
- Studied doses
- intraperitoneal 10 μg/kg/day for 5 days
The brain's vulnerability to oxidative stress is a central puzzle in aging research. Pinealon (Glu-Asp-Arg) is a synthetic tripeptide—just three amino acids—developed by Vladimir Khavinson's group at the St. Petersburg Institute of Bioregulation and Gerontology. Research suggests it may suppress reactive oxygen species accumulation in neurons and modulate gene expression pathways involved in cellular survival PMID: 21978084 .
This mechanism positions pinealon differently from most research peptides. Rather than targeting a single receptor, it appears to interact directly with DNA, influencing transcription of genes associated with apoptosis and cellular maintenance. Preclinical studies in rat models indicate potential effects on cognitive function, neuronal resilience under oxidative stress, and markers of biological aging [PMID: 33396470, 26390612].
The evidence base is small and originates almost exclusively from one Russian research network. No completed human randomized controlled trials exist as of 2026. What follows is a research-relevant overview of what the preclinical data actually show.
Regulatory Status
- United States
- Research use only
- European Union
- Research use only
- United Kingdom
- Research use only
What is this compound?
Pinealon (Glu-Asp-Arg, or EDR) is a synthetic tripeptide with a molecular weight of approximately 418 daltons. It belongs to the class of peptide bioregulators—short amino acid chains proposed to interact directly with cellular DNA and influence gene expression. The tripeptide consists of L-glutamic acid, L-aspartic acid, and L-arginine, and was developed as part of a broader program of synthetic bioregulatory peptides at the St. Petersburg Institute of Bioregulation and Gerontology PMID: 21978084 .
The bioregulator concept distinguishes pinealon from conventional receptor-targeting peptides. Khavinson's research group hypothesized that very short peptides (2-4 amino acids) can enter cell nuclei and influence transcription by binding to promoter regions of specific genes. This proposed mechanism places pinealon in the same family as epitalon 
Epitalon tetrapeptide Pineal peptide studied for telomerase activation and longevity (Ala-Glu-Asp-Gly) and vesugen, though each targets different tissues and gene sets.
In research settings, pinealon has been administered via intraperitoneal injection in animal models. The compound's extremely small size suggests favorable bioavailability and potential for CNS penetration, though formal pharmacokinetic characterization in humans has not been conducted. All available data derive from preclinical studies and small-scale clinical observations in Russian populations.
How it works
Pinealon's proposed mechanism centers on direct gene expression modulation. Unlike peptides that bind surface receptors to trigger signaling cascades, pinealon is hypothesized to penetrate cell nuclei and interact with DNA promoter regions, influencing transcription of genes involved in cellular survival and maintenance PMID: 33396470 .
The most thoroughly documented effect is ROS suppression. In cell culture studies, pinealon demonstrated dose-dependent restriction of reactive oxygen species accumulation. When neurons were exposed to oxidative stress conditions, pinealon-treated cells showed significantly lower ROS levels and reduced necrosis rates compared to untreated controls. This antioxidant effect was observed at concentrations substantially lower than those required for comparable protection by compounds like carnosine PMID: 21978084 .
A second pathway involves apoptosis regulation. Research indicates pinealon modulates expression of caspase-3—a key executioner enzyme in programmed cell death—and the tumor suppressor protein p53. By downregulating caspase-3 activity, pinealon may reduce the rate of neuronal apoptosis under stress conditions. The p53 modulation suggests a more complex role in cell-cycle regulation that extends beyond simple antioxidant protection PMID: 33396470 .
Third, evidence points to mitochondrial function support. Studies examining cytochrome C oxidase—a critical enzyme in the mitochondrial electron transport chain—suggest pinealon may influence mitochondrial respiratory capacity. This connection to cellular energy production links pinealon to the broader category of mitochondrial-targeted research compounds PMID: 21978084 .
- Suppression of reactive oxygen species (ROS) accumulation in neurons
- Gene expression modulation via direct DNA interaction in brain and pineal tissue
- Regulation of caspase-3 and p53 to reduce neuronal apoptosis
- Modulation of cytochrome C oxidase activity in mitochondria
Research Findings
The most consistent preclinical finding for pinealon is neuroprotection under oxidative stress. In rat models of prenatal hyperhomocysteinemia—a condition that damages developing neurons through NMDA receptor overactivation and ROS accumulation—pinealon administration to pregnant dams protected offspring from cognitive deficits. Treated offspring showed improved spatial learning in Morris water maze tests and enhanced neuronal resistance to hydrogen peroxide-induced oxidative stress PMID: 21978084 .
Cognitive function preservation has been observed in additional rodent models. Pinealon maintained learning retention in rats with experimentally-induced diabetes, a condition known to impair hippocampal function through oxidative and inflammatory pathways. These findings align with the compound's proposed mechanism of gene expression modulation in brain tissue PMID: 21978084 .
Geroprotective effects represent a third research axis. A clinical observation study in elderly patients with organic brain syndrome reported that pinealon, combined with vesugen, improved markers of biological aging and CNS function. The study suggested pinealon exhibited anabolic and neuroprotective properties that may slow the rate of biological aging, though the non-randomized design and small sample size limit the strength of these conclusions PMID: 26390612 .
Cellular resilience extends beyond the nervous system. In vitro studies on skin fibroblasts from elderly donors showed that pinealon improved cell viability and proliferative capacity, suggesting broader tissue-protective effects PMID: 22803085 .
- neuroprotection preclinical
- cognitive-function preclinical
- anti-aging preclinical
- cellular-resilience preclinical
Dosage Context Explained
Published dosing data for pinealon are extremely limited. The most cited preclinical study employed 10 μg/kg/day administered intraperitoneally for 5 consecutive days in a rat model of prenatal hyperhomocysteinemia PMID: 21978084 . This dose was selected to evaluate neuroprotective effects during a specific developmental window.
In the clinical observation study involving elderly patients, pinealon was administered alongside vesugen, though specific dosing parameters were not consistently reported in the English-language abstract PMID: 26390612 . The Russian clinical literature references pinealon as a "cytogen" preparation—tissue-specific peptide bioregulators typically administered in short courses.
Intranasal administration has been discussed in the context of CNS-targeted delivery, leveraging the tripeptide's small molecular size for potential direct brain penetration via the olfactory route. However, standardized intranasal dosing protocols have not been published in peer-reviewed literature.
All dosage information should be treated as research-context reference points. No regulatory agency has established approved dosing guidelines for human use. Direct translation from rat intraperitoneal doses to any other species or route is unreliable.
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- Administration Routes
- intraperitoneal
- Range
- 10 μg/kg/day for 5 days
rat model of prenatal hyperhomocysteinemia
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Side Effects: Research Context
Pinealon's safety profile in available preclinical literature is notably sparse. The published studies do not report adverse effects at the doses tested, suggesting a favorable safety margin in animal models. However, this absence of reported toxicity should not be equated with demonstrated safety—it reflects the limited scope of conducted studies rather than comprehensive toxicological evaluation.
No formal toxicology studies, dose-escalation safety trials, or long-term carcinogenicity assessments have been published for pinealon. The compound's proposed mechanism of direct DNA interaction raises theoretical questions about off-target gene modulation, though no evidence of genotoxicity has been reported.
Theoretical contraindications include active malignancy, as any compound that modulates gene expression and cell survival pathways warrants caution in oncological contexts. The p53 modulation observed in mechanistic studies is particularly relevant, as p53 is a central tumor suppressor PMID: 33396470 .
The lack of human safety data means that any extrapolation from preclinical findings to human risk assessment remains speculative. Systematic pharmacovigilance data are unavailable.
- none documented in preclinical models
Frequently Asked Questions
Frequently Asked Questions
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Pinealon (Glu-Asp-Arg, or EDR) is a synthetic tripeptide with a molecular weight of approximately 418 daltons. It was developed by Vladimir Khavinson's group at the St. Petersburg Institute of Bioregulation and Gerontology as part of a program studying short peptide bioregulators. The tripeptide consists of L-glutamic acid, L-aspartic acid, and L-arginine, and is proposed to interact directly with cellular DNA to modulate gene expression [PMID: 21978084].
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Research suggests pinealon may suppress reactive oxygen species (ROS) accumulation in neurons, regulate caspase-3 and p53 expression to reduce apoptosis, and support mitochondrial function through cytochrome C oxidase modulation [PMID: 21978084, 33396470]. Its proposed mechanism of direct DNA interaction distinguishes it from conventional receptor-targeting peptides. These mechanisms are documented in preclinical studies and require further independent validation.
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Preclinical studies suggest neuroprotective effects in rat models of prenatal oxidative stress, cognitive function preservation in diabetic rodents, and geroprotective properties in elderly patients with organic brain syndrome [PMID: 21978084, 26390612]. Cell culture studies indicate improved fibroblast viability in cells from elderly donors [PMID: 22803085]. All findings are preclinical; no large-scale randomized clinical trials have been completed.
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No adverse effects have been reported at tested doses in preclinical studies, though systematic safety data are lacking. Theoretical concerns relate to pinealon's proposed direct DNA interaction and p53 modulation, warranting caution in individuals with active malignancy [PMID: 33396470]. Pinealon is classified as a research chemical only and is not approved for human consumption in the US, EU, or UK.
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Both are Khavinson-group peptide bioregulators with proposed gene expression modulation mechanisms, but they target different tissues and pathways. Epitalon (Ala-Glu-Asp-Gly) focuses on telomerase activation and melatonin regulation, while pinealon (Glu-Asp-Arg) targets ROS suppression and anti-apoptotic pathways in brain tissue. Epitalon has a larger evidence base including small human trials; pinealon's evidence is limited to preclinical models and clinical observations.