Pinealon
Also known as: Glu-Asp-Arg
A short tripeptide bioregulator studied in Russian gerontology research for neuroprotective and anti-ageing effects on the central nervous system.
Pinealon is a Khavinson tripeptide (Glu-Asp-Arg) studied for pineal-directed neuroprotection and gerontoprotective effects in Russian clinical cohorts.
Evidence tier: B — clinical evidence (trials or approved use in some jurisdictions)
- Category
- Neuroprotection
- Half-life
- Short plasma half-life; epigenetic effects extend beyond exposure
- Formula
- C₁₅H₂₆N₆O₈
- Weight
- 418.4 g/mol
- Sequence
- Glu-Asp-Arg
Section 1
Overview
Pinealon is a short synthetic tripeptide developed within Vladimir Khavinson's bioregulator peptide programme at the St. Petersburg Institute of Bioregulation and Gerontology. The Khavinson school's central hypothesis is that short peptides of two to four amino acids can act as direct gene-expression regulators, binding to specific DNA motifs and modulating transcription of age-related target genes.
Pinealon is positioned in this framework as a neuroprotective and anti-ageing peptide, derived conceptually from peptide extracts of the pineal gland and synthesised in a defined three-amino-acid sequence.
Published research focuses on neuroprotection against oxidative stress, hypoxia, and excitotoxic damage in cell-culture and animal models, with measurable effects on antioxidant enzyme expression and stress-response gene activation.
Section 2
Discovery & History
- Developed in the 1990s–2000s at the St. Petersburg Institute of Bioregulation and Gerontology under the direction of Vladimir Khavinson, as part of the institute's programme to derive defined synthetic short peptides from complex bioregulator extracts of endocrine and neural tissues.
- Part of a family of related short bioregulator peptides including Epitalon (Ala-Glu-Asp-Gly, pineal), Vesugen (Lys-Glu-Asp, vascular), Cortagen (Ala-Glu-Asp-Pro, brain-cortex), Livagen (chromatin), Thymalin (immune), and Cerluten (pulmonary).
- Used in Russian clinical and research practice as a neuroprotective bioregulator; not approved as a medicine in Western jurisdictions, with all publicly-available data originating from Russian-language or Russian-collaborating international peer-reviewed sources.
- International peer-reviewed publications from the Khavinson group describe both phenotypic neuroprotective effects and proposed epigenetic transcription-modulation mechanisms — the latter remain a distinctive theoretical framework that has not been fully independently replicated outside the originating school.
- The peptide has been tested in Russian gerontology cohorts and forms part of the periodic (typically twice-yearly, 10-day-course) bioregulator protocols that characterise the Khavinson practice framework.
Section 3
Mechanism of Action
- 1Proposed direct binding to specific DNA promoter regions — the central Khavinson-school mechanism — modulating transcription of antioxidant, stress-response, and DNA-repair genes; the interaction has been described biophysically by the originating group but has attracted continuing debate outside Russia.
- 2Upregulation of endogenous antioxidant enzyme expression (superoxide dismutase, catalase, glutathione peroxidase) in neuronal cell culture under oxidative challenge, providing the biochemical footprint of the transcriptional effect.
- 3Reduction of reactive oxygen species (ROS) accumulation and lipid peroxidation markers in cellular and animal models of hypoxia, ischaemia-reperfusion, and glutamate excitotoxicity.
- 4Modulation of telomerase activity in some in vitro models, consistent with the broader Khavinson 'gerontoprotective' framework in which short peptides are hypothesised to interact with telomere-associated protein complexes.
- 5Inhibition of glutamate-induced excitotoxicity in neuronal preparations — measurable preservation of neuronal viability under NMDA-receptor-driven excitotoxic insult at pharmacologically-plausible concentrations.
- 6Anti-apoptotic effects via reduced caspase-3 activation in stressed neuronal cultures, plausibly downstream of the antioxidant transcriptional response.
- 7Cerebrovascular effects — reported improvements in cerebral perfusion parameters in animal hypoxia models, part of the peptide's positioning as a neuroprotective bioregulator.
Section 4
Researched Benefits
Findings reported in the published preclinical and clinical literature. Effects in research contexts do not constitute claims of therapeutic benefit in humans.
- 1Protection of cultured neurons against oxidative stress and glutamate excitotoxicity — the flagship in-vitro finding across multiple independent Khavinson-collaborated studies.
- 2Reduction of behavioural deficits and improved learning performance in animal models of cerebral hypoxia and ischaemia-reperfusion injury.
- 3Upregulation of endogenous antioxidant defences in cell-culture and in vivo tissue-analysis work.
- 4Potential gerontoprotective effects in the Khavinson-school framework — the broader programme includes multi-decade cohort work in Russian gerontology populations reporting reductions in age-related morbidity.
- 5Used as a research tool in models of neurodegenerative ageing and mitochondrial dysfunction, alongside Epitalon and the other Khavinson short peptides.
- 6Reported cognitive-preservation effects in aged-animal cohorts, plausibly downstream of the neuroprotective mechanism rather than a direct pro-cognitive effect.
- 7Well-tolerated in the reported clinical experience, with adverse-event rates comparable to placebo in the human protocols documented in Russian sources.
Section 5
Theoretical Dosing & Protocols
| Route | Dosage | Frequency | Duration |
|---|---|---|---|
| Intranasal / parenteral (research) | Microgram-range doses in animal protocols | Cyclical (typically 10–20 day courses) in research practice | Short courses repeated periodically |
Note: No standardised human dosing in peer-reviewed Western literature.
Section 6
Administration Routes
- Intranasal — the primary research route and the reference administration modality in Russian clinical practice; exploits nose-to-brain delivery in the same fashion as Semax and Selank.
- Subcutaneous and intramuscular routes are used in some animal studies and in Russian clinical protocols where dose-response control is prioritised.
- Oral administration is generally not used — the short tripeptide is susceptible to gastrointestinal proteolysis and undergoes near-complete first-pass metabolism.
- Intraventricular administration has been used in mechanistic animal research to bypass blood-brain-barrier questions, though this is a research-only route.
Section 7
Safety Profile
Commonly reported
- · Minimal published acute toxicity in animal studies at pharmacologically relevant doses — the Khavinson-school peptides in general display unusually clean acute-toxicity profiles.
- · Mild local irritation possible with intranasal administration; transient and self-limiting.
- · Occasional mild headache during initial dosing, resolving within days of continued administration.
- · Well-tolerated in the reported Russian clinical experience across paediatric, adult, and elderly populations.
Rare / theoretical
- · Long-term safety data outside the Khavinson group is sparse — chronic-use safety beyond the standard 10-day-course-per-6-months protocol is not well-characterised.
- · Mechanism (direct DNA binding by short peptides) remains debated in Western pharmacology; regulatory-scale safety evaluation would require replication of the mechanistic claims independently.
- · Theoretical interaction with epigenetic-modifier drugs given the proposed transcriptional-modulation mechanism — no documented clinical events but a prudent research-context consideration.
- · No documented hypersensitivity reactions in the published cohort work, but the low sample-size context of the peptide's clinical history is a caveat.
Contraindications
- · Not licensed for human use in the UK, EU (centralised), or US — supply for human consumption is prohibited under the Human Medicines Regulations 2012.
- · Pregnancy and lactation — no controlled human data.
- · Concurrent use with mechanism-relevant experimental agents in research contexts should be evaluated for potential interaction, particularly other bioregulator peptides at the epigenetic-transcriptional level.
Section 8
UK & EU Regulatory Context
United Kingdom
Not a licensed medicine in the United Kingdom. Research chemical only.
European Union
Not approved by the EMA. Used in research and traditional clinical practice in the Russian Federation.
Section 9
Clinical Studies Summary
Pinealon and oxidative neuroprotection
Neuronal cell-culture work in primary rat cortical and hippocampal neurons demonstrating markedly reduced oxidative damage, preserved mitochondrial membrane potential, and higher cell viability under hydrogen peroxide and glutamate excitotoxic challenge in Pinealon-pretreated cultures, with correlated increases in the expression of superoxide dismutase and catalase.
Read studyPinealon in models of cerebral hypoxia
In-vivo rodent model of acute normobaric hypoxia with intranasal Pinealon pretreatment; the treated group showed improved behavioural performance on maze and rota-rod tests and reduced histological damage in the hippocampus and cortex versus vehicle-treated controls.
Read studyPinealon epigenetic mechanism characterisation
Molecular-biology study characterising the proposed direct-DNA-binding mechanism of Pinealon via ChIP-seq and gel-shift approaches, identifying preferential association with promoter regions of specific antioxidant and stress-response genes and providing the mechanistic scaffold for the observed neuroprotective effect.
Section 10
Frequently Asked Questions
Section 10a
Practical Research Guidance
Cycle guidance
Reconstitution & storage
UK sourcing notes
Section 11
Sourcing for Laboratory Research
Sourcing Pinealon for laboratory research
Researchers in the United Kingdom and elsewhere typically obtain Pinealon from specialist research-chemical suppliers. Purity, third-party testing, and supplier transparency are the principal differentiators worth evaluating before placing an order. The two suppliers below are commonly referenced in UK research contexts.
Reminder: research peptides are sold strictly for in vitro and preclinical laboratory purposes. Importation or supply for human consumption is not permitted under UK medicines legislation.