Pinealon

How does Pinealon work?

Pinealon's proposed mechanism is the defining feature of the Khavinson short-peptide model: rather than acting on a cell-surface receptor, the EDR tripeptide is reported to penetrate the cell and nuclear membranes and interact directly with DNA (and deoxyribooligonucleotides) to modulate gene expression. Downstream, cell-culture work describes antioxidant, anti-apoptotic, and proliferation effects in neurons. All of the mechanistic evidence below is preclinical.

1. Direct DNA / Gene-Expression Interaction [1]. EDR is proposed to bypass cell-surface receptors, penetrate the cell and nuclear membranes, and interact directly with DNA to modulate gene expression (Fedoreyeva et al. 2011, in HeLa cells and in vitro).
2. Oxidative-Stress Defense in Neurons [3]. In oxidatively stressed cortical neuron cultures, EDR reduced caspase-3 activation and reactive oxygen species, helped preserve mitochondrial membrane potential, and upregulated the antioxidant genes Sod2 and Cat.
3. Neural Cell-Cycle / Proliferation [4]. In neural progenitor cells, EDR modulated proliferation through changes in PCNA and p21 expression (Linkova et al. 2016).
4. Cell Viability via Free-Radical Suppression [2]. Cultured-cell work reported increased cell viability through suppression of free-radical levels and activation of proliferative processes (Khavinson et al. 2011).

What is Pinealon researched for?

Pinealon's research base is preclinical — in vitro neuronal cultures and rodent models of hypoxia and age-related cognitive decline — and comes predominantly from Khavinson-affiliated Russian laboratories. There are no human randomized controlled trials. The findings below should be read as early-stage, largely single-group preclinical signals, not clinical evidence.

1. Cognitive Aging Under Hypoxia [5]. In young and aged rats subjected to acute hypoxic hypoxia, treatment improved Morris-water-maze spatial learning and reduced brain caspase-3 activity (Mendzheritskiĭ et al. 2014).
2. Alzheimer's-Model Neuroprotection [7][8]. EDR restored neuronal spine density in Alzheimer's-model preparations (Kraskovskaya/Linkova 2017) and showed neuroprotection in an Alzheimer's-disease mouse model (Khavinson et al. 2021).
3. Proposed Epigenetic Mechanism in Alzheimer's [6]. A 2020 review synthesized a possible mechanism by which EDR regulates gene expression and protein synthesis in the pathogenesis of Alzheimer's disease (Khavinson et al. 2020).
4. Neuronal Viability and Proliferation [2]. Cell-culture work reported increased neuronal viability through free-radical suppression and activation of proliferative processes (Khavinson et al. 2011).

How is Pinealon dosed?

There is no validated research-dose consensus for Pinealon. It is supplied for research use only as a lyophilized powder. The original commercial Khavinson oral preparation is approximately 10 mg per capsule; injectable research use has no standardized, validated protocol.

Because no controlled human dosing studies exist, any injectable figure circulated for Pinealon is extrapolated rather than validated. The only manufacturer-defined dose is the ~10 mg oral capsule from the original Khavinson preparation. Researchers handling the lyophilized powder reconstitute it with bacteriostatic or sterile water (see storage below). Prof. Peptide deliberately does not provide an injectable mg schedule — publishing one would imply a validated protocol that does not exist.

What are the side effects of Pinealon?

Pinealon's human safety profile is not characterized. The available evidence is preclinical (cell culture and rodent), so there is no controlled human adverse-event data to summarize. This is a Research Use Only compound and is not intended for human consumption; nothing here should be read as human-use guidance. The honest summary is that human tolerability, interactions, and long-term safety are simply unknown.

How should Pinealon be stored?

1. Lyophilized (powder) form: store cold and desiccated, protected from light. Freeze at -20°C for long-term storage; 2–8°C is acceptable short-term.
2. Reconstitute with bacteriostatic or sterile water for injection. Add the water slowly down the inside wall of the vial and swirl gently — do not shake.
3. Reconstituted solution: refrigerate at 2–8°C and keep protected from light.
4. Protect from light at all times; store in original packaging.
5. Discard if the solution is cloudy, discolored, or contains particles.

What are the limitations of Pinealon research?

This is the most important section to read carefully. The entire Pinealon evidence base is preclinical — in vitro and rodent — and comes predominantly from Khavinson-affiliated Russian laboratories. There is no independent Western replication and no human randomized controlled trials.

Where to source Pinealon

Pinealon is not approved for human use and is sold by specialty research peptide vendors for laboratory use only. Quality varies across vendors — verify a Certificate of Analysis before purchase.

Pinealon FAQ

References

1. Fedoreyeva LI, Kireev II, Khavinson VKh, Vanyushin BF. Penetration of short fluorescence-labeled peptides into the nucleus in HeLa cells and in vitro specific interaction with DNA. Biochemistry (Moscow). 2011;76(11):1210-9. PMID 22117547. https://pubmed.ncbi.nlm.nih.gov/22117547/
2. Khavinson V, Ribakova Y, Kulebiakin K, et al. Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Rejuvenation Research. 2011. (Paywalled)
3. Khavinson VKh, et al. EDR peptide in cortical neuron cultures under oxidative stress (caspase-3, ROS, Sod2/Cat). 2012. PMID 23199282. https://pubmed.ncbi.nlm.nih.gov/23199282/
4. Linkova NS, et al. EDR peptide effects on PCNA/p21 in neural progenitor cells. 2016. PMID 27262825. https://pubmed.ncbi.nlm.nih.gov/27262825/
5. Mendzheritskiĭ AM, Karantysh GV, Ryzhak GA, Dem'ianenko SV. Cytokines and caspase-3 activity in old-rat brain under acute hypoxic hypoxia with Cortexin and Pinealon. Advances in Gerontology. 2014;27:94-97. (Paywalled)
6. Khavinson V, Linkova N, Kozhevnikova E, Trofimova S. EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation in the Pathogenesis of Alzheimer's Disease. Molecules. 2020. (Open Access)
7. Khavinson V, et al. Neuroprotective Effects of Tripeptides — Epigenetic Regulators in a Mouse Model of Alzheimer's Disease. Pharmaceuticals. 2021;14(6):515. (Open Access)
8. Kraskovskaya N, Kukanova E, Linkova N, et al. EDR peptide restores neuronal spine density in Alzheimer's-model preparations. Bulletin of Experimental Biology and Medicine. 2017. (Paywalled)

Published Studies