Pinealon
Khavinson tripeptide investigated for neuroprotection and cognitive ageing.
- Sequence: Glu-Asp-Arg (EDR)
- Member of the St Petersburg cytomedine peptide family
- Studied in hypoxia, oxidative stress and cognitive-decline models
- Reported reduction of neuronal apoptosis under stress conditions
- Sequence
- H-Glu-Asp-Arg-OH
- Molecular weight
- 418.4 g/mol
- Half-life
- Short circulating half-life; gene-regulatory activity persists hours longer per Khavinson group reports.
Overview
Pinealon is a synthetic tripeptide composed of L-glutamic acid, L-aspartic acid and L-arginine (sequence shorthand EDR). It is a member of the Khavinson family of short bioregulatory peptides developed at the St Petersburg Institute of Bioregulation and Gerontology, sharing the family's theoretical framework: short peptide sequences derived from tissue extracts that act as gene-regulatory signals selective for the tissue of origin.
Whereas Epitalon (AEDG) was derived from the pineal polypeptide epithalamin and is studied for telomere and pineal-axis effects, Pinealon has been positioned in the Khavinson programme as a more directly neurotropic short peptide — investigated principally for neuronal survival under stress, antioxidant gene expression and cognitive preservation in aged rodents.
International independent research on Pinealon is more limited than on Epitalon, and most published work comes from the same St Petersburg research group. This page summarises what is in the literature, the proposed mechanisms, the available safety information and the UK regulatory framing.
Mechanism of action
The principal proposed mechanism is the same gene-regulatory model applied across the Khavinson short-peptide family. According to Khavinson and colleagues, EDR enters cells and reaches the nucleus, where it binds short DNA sequence motifs in promoter regions and modulates transcription. In Pinealon's case, the target gene profile is reported to favour antioxidant-defence and antiapoptotic genes in neuronal lineages.
In in vitro models of hypoxic and oxidative stress, Pinealon reduces reactive oxygen species accumulation and preserves mitochondrial membrane potential in cultured neurons. The peptide reduces caspase-3 activation and DNA fragmentation under conditions that produce substantial apoptosis in vehicle-treated controls.
In rodent models, intranasal and subcutaneous administration produce measurable effects on hippocampal antioxidant enzyme expression (SOD1, catalase) and on behavioural measures of learning and memory in aged animals. Effects are typically modest but reproducible within the published series.
The gene-regulatory model — short peptides reaching the nucleus and binding DNA directly — remains the most actively debated aspect of Pinealon's pharmacology. Independent replication of the proposed binding motifs in chromatin immunoprecipitation experiments has not been reported outside the original group.
Research history
Pinealon was developed in the 1990s as part of the broader Khavinson cytomedine programme and has been subject to in-house preclinical investigation since. Published work has appeared in Russian-language gerontology journals (Bulletin of Experimental Biology and Medicine, Advances in Gerontology) and in international journals on neuroscience and ageing.
Outside the St Petersburg group, Pinealon is comparatively under-studied. There are no large-scale phase II or III clinical trials registered with the MHRA, EMA or FDA. Interest from the wider longevity research community has grown alongside the broader Khavinson short-peptide programme, but independent reproduction work remains limited.
Summarised studies
Effect of Pinealon on free-radical accumulation in cortical neurons
Khavinson VKh, Lin'kova NS, Tarnovskaya SI, Umnov RS
EDR pre-treatment reduced ROS accumulation by 35–50% and preserved mitochondrial membrane potential under oxidative challenge.
Neuroprotective effect of Pinealon in a rat hypoxia model
Arutjunyan AV, Kozina LS, Stvolinskii SL, et al.
Subcutaneous Pinealon reduced post-hypoxic neuronal apoptosis in hippocampus; partial preservation of behavioural performance on Morris water maze.
Short peptides as gene regulators: AEDG and EDR binding to DNA promoter motifs
Fedoreyeva LI, Smirnova TA, Kireev II, et al.
EDR exhibits sequence-selective binding to specific DNA motifs in promoter regions of neural-development and antioxidant genes.
Pinealon and cognitive preservation in aged rodents
Kozina LS, Arutjunyan AV, Khavinson VKh
Improvement in spatial-memory performance in aged rats receiving Pinealon courses vs. age-matched vehicle controls.
Safety profile
Available rodent toxicology of Pinealon, conducted predominantly within the Khavinson research programme, has not produced acute or sub-chronic toxicity signals at doses substantially above the pharmacological range. No mutagenic or tumour-promoting effects have been reported.
Human safety information is limited and consists primarily of open-label observational data from elderly cohorts. The absence of large-scale placebo-controlled human safety studies means that subtle effects cannot be excluded.
Standard considerations for parenteral peptide handling apply: contamination, injection-site reactions and immunogenicity from non-sterile material are practical risks if research-grade peptide is mishandled.
UK regulatory status
Pinealon is not a licensed medicine in the United Kingdom. It is not held on the MHRA register and no marketing authorisation has been granted for human therapeutic use.
Supply in the UK is limited to research-grade material labelled for laboratory and preclinical use only. Researchers should follow institutional SOPs for unlicensed investigational compounds.
Frequently asked questions
What is Pinealon?
Pinealon is a synthetic tripeptide (Glu-Asp-Arg, EDR) developed at the St Petersburg Institute of Bioregulation and Gerontology as part of the Khavinson short-peptide family. It is studied for neuroprotective and cognitive-preservation effects in animal models.
How does Pinealon differ from Epitalon?
Both are short Khavinson peptides, but Epitalon (AEDG, a tetrapeptide) is principally studied for telomerase and pineal-axis effects, while Pinealon (EDR, a tripeptide) is positioned as a more directly neurotropic peptide focused on neuronal survival and cognitive function.
Is Pinealon a nootropic?
It is sometimes described as one based on its effects on cognitive performance in aged rodents, but it has not been characterised as a classical nootropic in human clinical trials. The 'nootropic' framing is informal and not regulator-recognised.
Has Pinealon been tested in humans?
Open-label observational studies in Russian-language gerontology journals report tolerability and modest improvements in cognitive performance, but no phase II or III randomised controlled trials have been registered with major regulators.
Is Pinealon legal in the UK?
Pinealon is not a licensed medicine in the UK and is supplied only as a research-grade peptide for laboratory and preclinical use.
How is Pinealon usually administered in research protocols?
Published rodent protocols use subcutaneous or intranasal administration in pulsed courses; cell-culture work uses low-nanomolar concentrations in growth medium.
Related peptides
Adjacent compounds in the longevity research literature with overlapping mechanisms or shared research history.
A synthetic tetrapeptide (Ala-Glu-Asp-Gly) derived from the pineal polypeptide epithalamin, studied for its effects on telomerase activity, circadian regulation, and lifespan extension in animal models.
A 24-amino-acid mitochondrially-derived peptide encoded within the 16S rRNA gene, studied for cytoprotective, metabolic and neuroprotective signalling that declines with age.
A 28-amino-acid synthetic equivalent of an N-acetylated peptide fragment originally isolated from thymic tissue, studied for immune-modulatory activity and increasingly examined in the context of immunosenescence and longevity.
References
- Arutjunyan AV et al., Bull Exp Biol Med 2012 — hypoxia model
- St Petersburg Institute of Bioregulation and Gerontology
See also our editorial coverage at PeptideAuthority.co.uk for related research dossiers.