Pinealon

Typical use cases

Dosing guidelines

Titration

No formal titration scheme; protocols are typically described as fixed-dose short courses of ~10-20 days rather than titrated

Reconstitution

For lyophilized injectable powder, commonly reconstituted with bacteriostatic water (e.g., a 20 mg vial with ~3 mL for ~6.67 mg/mL, or a 10 mg vial with ~1 mL for ~10 mg/mL). Swirl gently, do not shake. N/A for oral capsule form.

Injection sites

Subcutaneous injection (commonly abdomen) when used as injectable; also available as an oral capsule

Storage & handling

Store lyophilized powder refrigerated (2-8°C); reconstituted solution kept refrigerated and typically used within ~30 days. Protect from light and freezing.

Side effects

• Headache Mild · Uncommon
• Vivid dreams or mild insomnia (especially if taken late in the day) Mild · Uncommon
• Transient fatigue or drowsiness Mild · Uncommon
• Mild anxiety or restlessness Mild · Rare
• Dizziness Mild · Rare
• Injection-site irritation or redness (injectable form) Mild · Uncommon

Research summary

Pinealon is a short synthetic tripeptide (Glu-Asp-Arg, "EDR") from the Russian "bioregulator" peptide class developed by Vladimir Khavinson's group at the St. Petersburg Institute of Bioregulation and Gerontology, and is classified within the geroprotector category. The evidence base is overwhelmingly preclinical: in vitro and in vivo studies report that Pinealon produces dose-dependent suppression of reactive oxygen species in cerebellar granule cells, neutrophils and PC12 cells, reduces necrotic cell death, and is associated with lower caspase-3 and p53 and increased antioxidant enzyme activity such as SOD2 and GPx1 (Khavinson et al., Rejuvenation Research 2011). Because of its very small size it is hypothesized to enter cells and act epigenetically by interacting with promoter/DNA regions and histones rather than through surface receptors, influencing pathways including MAPK/ERK, PPARA/PPARG and serotonin synthesis (Molecules 2020 review on EDR and Alzheimer's pathogenesis). In a 5xFAD transgenic-mouse Alzheimer's model, EDR was reported to help prevent dendritic-spine loss and support neuroplasticity (Pharmaceuticals 2021). Human data are limited to small, mostly Russian observational and clinical-practice reports (e.g., oral use in older patients and in traumatic-brain-injury sequelae) describing improved memory, attention and reduced headache, with no completed Western randomized controlled trials and no regulatory approval as a drug. Key limitations are the absence of rigorous double-blind human trials, small sample sizes, potential publication bias within a single research lineage, and unestablished long-term safety. Findings should be regarded as exploratory and educational, not as validated clinical evidence.

Key references

• https://pubmed.ncbi.nlm.nih.gov/21978084/
• https://pmc.ncbi.nlm.nih.gov/articles/PMC7795577/
• https://pmc.ncbi.nlm.nih.gov/articles/PMC8227791/
• https://pubchem.ncbi.nlm.nih.gov/compound/18220191

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