Pinealon

Glu-Asp-Arg (EDR), pinealone, "brain bioregulator" tripeptide

Immune & bioregulators

Awaiting medical reviewEN ES DE FR PT ZH+ Follow for updates

Summary

Class: Synthetic tripeptide (3 amino acids: Glu-Asp-Arg), designed by the Khavinson group as a brain/pineal-targeted bioregulator
Mechanism: Proposed to enter neurons and alter gene expression (e.g. of proteins involved in cell division and ageing), reduce oxidative stress and protect neurons from hypoxia and excitotoxicity; mechanism is from cell culture and molecular modelling
Routes studied: Intraperitoneal and intranasal (rodents); cell culture; community subcutaneous, intranasal and oral
Dose range reported: Animal: roughly 0.1–1 mg/kg in rodent neuroprotection studies †. Community: 1–10 mg/day subcutaneous or intranasal for 10–20 day courses; oral capsule products at a few mg. No human dose from any trial
Half-life: Not characterised; expected to be minutes in plasma as an unprotected tripeptide. The group claims small peptides can cross cell membranes and the blood–brain barrier; evidence is from in-vitro and tracer models
Storage: Lyophilised: refrigerate, protect from light. Reconstituted: refrigerate; community practice is use within ~4 weeks
Regulatory status: Not approved as a medicine anywhere. Sold as an oral "bioregulator" supplement in Russia and online. See region table

Doses are as reported in studies or by the community — never recommendations.

1What it is

Pinealon is a three-amino-acid synthetic peptide (glutamate-aspartate-arginine) from the same St Petersburg research programme that produced thymalin and Epitalon. Despite the name, it is positioned as a brain and nervous-system bioregulator rather than specifically a pineal one — the group's naming follows the tissue the parent extract came from or the intended target. Its parent extract is Cortexin, a cattle-brain polypeptide preparation registered as a medicine in Russia for stroke, encephalopathy and cognitive impairment.

Pinealon has far less published material than Epitalon. What exists is mostly rodent and cell-culture work from the Khavinson group — neuroprotection against hypoxia and oxidative stress, effects on cell cycle proteins in cultured neurons, and behavioural effects in aged or prenatally stressed rats — plus Russian-language clinical reports that usually concern Cortexin rather than the tripeptide. There are no controlled human trials of pinealon.

2How it's thought to work

Gene expression. in the bioregulator model, pinealon enters the nucleus and binds specific DNA sequences, changing expression of genes involved in neuron survival and differentiation. Molecular-docking studies support a plausible binding geometry; direct in-vivo proof is lacking.

Antioxidant / anti-apoptotic. reduces reactive oxygen species and markers of programmed cell death in cultured neurons and in rat brain exposed to hypoxia (Khavinson 2011; Arutjunyan 2012).

Cell-cycle regulation. reported to alter levels of proteins such as p53 and caspase-3 in neuronal cultures, interpreted as protecting cells from stress-induced death.

Irisin / metabolic signalling. more recent cell work reports pinealon raised expression of irisin-related and neurotrophic markers in cultured cells; early and unreplicated.

Melatonin and circadian effects. suggested by analogy with Epitalon; little direct data.

Proposed: a tripeptide directed at brain tissue, reported to protect neurons from oxygen deprivation in rodent models. Human data are absent.Schematic — not to scale

3What the research shows

Graded C/D

Neuroprotection against hypoxia and oxidative stress (rodent, cell)

Rat models of prenatal hyperhomocysteinemia and hypoxia reported that pinealon reduced oxidative damage in brain tissue and improved later cognitive performance in offspring (Arutjunyan 2012; Khavinson 2011). Cultured cortical neurons were protected from hypoxia-induced death. [1][2]

Cognitive and behavioural effects in aged animals

Aged rats given pinealon performed better on learning and memory tasks in small studies from the originating group.

Graded —/B (extract only)

Human cognition, stroke recovery, "brain ageing"

No controlled human trials of pinealon. Russian clinical reports of improved cognition and recovery after stroke concern Cortexin, the brain extract, and are mostly open-label. Community use of pinealon for memory, focus or neuroprotection rests on the rodent data and anecdote.

Lifespan

No lifespan studies of pinealon itself are published in English-language indexed journals. Lifespan claims attached to it online are borrowed from Epitalon and Epithalamin.

Graded C/D

Retina and sensory systems

Related short peptides from the same programme (e.g. the retina-targeted peptide used in Khavinson's retinitis pigmentosa work) have rodent and cell data; pinealon-specific retinal studies are limited to cell culture.

Any independent replication

None identified. Every published study of pinealon involves the originating group or its collaborators.

4Reported side effects and interactions

Literature-reported

no human safety data. Rodent studies report no toxicity at the doses used, which were short-term.

Community-reported

generally described as uneventful; some report improved sleep or a calm focus, others no effect. Injection-site irritation, mild headache and, with intranasal use, nasal irritation are the complaints that appear.

Theoretical. a peptide that genuinely changed neuronal gene expression or cell-cycle proteins would warrant caution in anyone with a history of brain tumour or seizures; there is no data either way. Immunogenicity of a 3-residue peptide is expected to be very low.

Interactions. none documented.

Markers researchers commonly monitor

No compound-specific markers are established. Protocols that include pinealon generally record:

Marker	Why it's watched
Baseline CBC and CMP	general safety monitoring.
Homocysteine	the rodent model in which pinealon showed protection involved hyperhomocysteinemia; also a general vascular-brain risk marker.
Validated cognitive tests (e.g. MoCA, digit span, reaction time)	because any claimed effect is cognitive and there is no biochemical readout.
Sleep quality and melatonin rhythm	if a pineal effect is expected, by analogy with Epitalon.
Oxidative stress markers (e.g. 8-OHdG, malondialdehyde)	research-only, corresponding to the proposed mechanism.

Free for everyone. Safety information is never behind a paywall.

5Reconstitution and handling

Commonly supplied in 10 mg or 20 mg vials; also as intranasal sprays and oral capsules. with , swirl gently, protect from light.

Open in calculator, pre-loaded →

6Commonly studied alongside

Epitalon (both pineal/brain bioregulators; combined in community "course" protocols), Cortexin (the parent extract), Semax and Selank (other Russian neuropeptides; no combined trials), thymalin and other organ-specific bioregulators.

Informational cross-links. Not stack recommendations.

7Regulatory status by region

Region	Status (checked —)
United States	Not FDA-approved. Not specifically named on the 2023 Category 2 compounding list †; unapproved drug if marketed for human use
European Union	Not authorised as a medicine; oral products sold online are not approved supplements with authorised health claims
United Kingdom	Not licensed
Australia	Not approved
South Africa	Not registered
Russia / CIS	Not a registered medicine; sold as a dietary supplement ("peptide bioregulator"). The related extract Cortexin is a registered medicine †
Sport	Not specifically named by WADA; as a non-approved substance it falls under S0 †

8Open questions

Does a tripeptide given by injection or nasal spray reach the brain intact in meaningful amounts?
Is there any human data at all beyond anecdote? Currently no.
Can any of the rodent neuroprotection findings be reproduced by an independent laboratory?

9References

1Khavinson VKh et al. (2011). Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Bull Exp Biol Med [verify exact title]. PubMed · DOI
2Arutjunyan A et al. (2012). Pinealon protects the rat offspring from prenatal hyperhomocysteinemia. Int J Clin Exp Med [verify journal]. PubMed
3Khavinson VKh, Linkova NS, Tarnovskaya SI (2016). Short peptides regulate gene expression. Bull Exp Biol Med. PubMed · DOI
4Anisimov VN, Khavinson VKh (2010). Peptide bioregulation of aging: results and prospects. Biogerontology. PubMed · DOI
5Khavinson VKh et al. (2020). Peptide regulation of gene expression: a systematic review. Molecules [verify exact title]. PubMed · DOI

† Being confirmed by our reviewers against current sources.

10Community

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Self-reported side effects Phase 2

Not enough data yet. 0 of the 50 members needed have logged this compound for 4+ weeks. We don't show anything below 50, so no one can be identified.

11Page history

25 Oct 2026Profile published — awaiting medical review

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