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Pinealon: The Blood-Brain Barrier-Crossing Peptide
Pinealon: The Blood-Brain Barrier-Crossing Peptide
Last updated June 2026 · Clean Reference Format
Summary
Pinealon is a tripeptide — Glu-Asp-Arg (EDR), ~404 Da — isolated from pineal gland extracts by Khavinson’s research group. Its most distinctive property is documented blood-brain barrier permeability, confirmed through fluorescence-tagged tracking studies. It acts as a neuronal protective agent (improved survival under oxidative stress, reduced apoptosis) and circadian modulator (restoration of circadian-regulated parameters in aged animal models). It is among the smallest peptides demonstrated to directly access the central nervous system.
Mechanism
Pinealon crosses the blood-brain barrier (demonstrated via fluorescence-labeled tracking) → accumulates in CNS tissue → modulates gene expression in neurons (consistent with Khavinson’s bioregulation theory) → supports neuronal survival pathways under stress conditions → modulates circadian clock components in pineal-connected neuronal circuits. The arginine residue may contribute to BBB transit via adsorptive transcytosis and to neuronal protection via nitric oxide signaling precursor activity.
Key Data
- BBB permeability confirmed: fluorescence-tagged Pinealon detected in CNS tissue after peripheral administration.
- Neuronal cell culture: improved survival under oxidative stress and reduced apoptotic markers with Pinealon treatment.
- Aged animal models: partial restoration of circadian-regulated parameters (sleep-wake cycling, hormonal patterns).
- One of the smallest peptides (~404 Da, 3 amino acids) demonstrated to cross the BBB and produce measurable CNS effects.
Pinealon vs. Epithalon
| Parameter | Pinealon | Epithalon |
|---|---|---|
| Sequence | Glu-Asp-Arg (EDR) | Ala-Glu-Asp-Gly (AEDG) |
| Length | 3 aa (tripeptide) | 4 aa (tetrapeptide) |
| MW | ~404 Da | ~390 Da |
| BBB Crossing | Yes (documented) | Not specifically demonstrated |
| Primary Focus | Neuronal protection, circadian | Telomerase activation |
| Origin | Pineal gland | Pineal gland |
Access Pinealon for Research
≥99% purity · HPLC/MS verified · Available for qualified research applications.
All content for research and educational purposes only. Pinealon is not approved for human consumption. Choice Peptide Labs supplies peptides for in vitro research only. Comply with all applicable regulations.
