Pinealon

Technical data

CAS

175175-23-2

Molecular formula

C15H26N6O8

Molecular weight

418.41 g/mol

Identity and composition

Pinealon is a short synthetic tripeptide with sequence Glu-Asp-Arg (EDR) studied in preclinical research as an agent of neuronal cytoprotection against oxidative stress. It belongs to the family of short bioregulator peptides and is investigated mainly in cell and animal models, not in humans.

As for its chemical identity, Pinealon corresponds to the sequence H-Glu-Asp-Arg-OH (L-glutamyl-L-aspartyl-L-arginine). Its molecular formula es C15H26N6O8 and its molecular weight is approximately 418.4 g/mol. It is also known as EDR peptide, Glu-Asp-Arg y L-glutamyl-L-aspartyl-L-arginine. In the databases consulted, a single CAS number was not confirmed (the catalogs show conflicting values), so that datum is omitted.

Product for research use.

Mechanism of action

The mechanism of action of Pinealon described in the literature is mostly proposed or experimental, derived from in vitro and in vivo models, and has not been confirmed in controlled clinical trials.

In cellular models, the peptide has been observed to reduce dose-dependent the accumulation of reactive oxygen species (ROS) induced by oxidative stress in cerebellar granule cells, neutrophils and PC12 cells, and that it decreases necrotic cell death (PMID 21978084).

It has been proposed that the peptide penetrates the cell and binds to histones and/or RNA, modulating gene expression. Among the described pathways is the signaling MAPK/ERK (delayed activation of ERK1/2 under oxidative stress), the increase in antioxidant enzymes (SOD2, GPX1), the reduction of pro-apoptotic proteins (caspase-3, p53) and the modulation of transcription factors PPARA/PPARG (PMID 33396470).

These mechanisms should be interpreted as experimental working hypotheses, not as demonstrated effects in people.

Pharmacokinetics

No verifiable human pharmacokinetic data were found for Pinealon. There are no documented values for half-life, bioavailability, or distribution in the sources reviewed.

In animal studies, administration has been used intraperitoneal, but the formal pharmacokinetic parameters are not characterized in the literature consulted. Consequently, any estimate of the temporal profile or of systemic exposure in humans would be speculative and is deliberately omitted.

Scientific evidence

The available evidence on Pinealon is preclinical, preliminary and limited. It is dominated by Russian research groups (Khavinson school, Institute of Bioregulation and Gerontology of St. Petersburg) and requires independent replication.

In preclinical studies, neuronal cytoprotection against oxidative stress has been investigated: a dose-dependent reduction of ROS and of necrotic cell death was observed in neuronal cells (PMID 21978084), and mechanisms of gene-expression regulation have been proposed in the context of models related to Alzheimer's disease (PMID 33396470). An in vivo study reported that Pinealon administered intraperitoneally was associated with better spatial learning and greater neuronal survival in the offspring of rats exposed to prenatal hyperhomocysteinemia (PMID 22567179).

No Western randomized clinical trials or registrations on ClinicalTrials.gov were found, and the compound does not have FDA or EMA approval. All of these findings should be interpreted as exploratory.

Research applications

Pinealon is offered exclusively for research use. Product for research use.

It may be of interest for research in:

• In vitro models of oxidative stress and ROS accumulation in neuronal cells.
• Preclinical studies of cytoprotection and cell viability.
• Exploratory research on short peptides and regulation of gene expression.
• Animal models of neuroprotection related to brain aging.

Not applicable for:

• clinical use, clinical use, diagnosis, or treatment.
• Therapeutic veterinary use.
• Any application that presupposes demonstrated efficacy or safety in people, since there are no controlled clinical trials supporting it.

Research protocols

The reported dosing protocols come from only from preclinical studies and should not be extrapolated to humans.

In an in vivo study in rats, administration was used intraperitoneal at 10 µg/kg/day (PMID 22567179). Cellular studies describe dose-dependent effects on the reduction of ROS, but the sources reviewed do not document a standardized dosing scheme or handling parameters applicable outside the experimental context.

There are no validated protocols for clinical use. Any experimental design must be defined in accordance with the study objectives and the corresponding laboratory practices.

Reconstitution

As a general laboratory guide for lyophilized peptides: reconstitution is usually performed with bacteriostatic water (sterile water with approximately 0.9% benzyl alcohol), which allows multiple withdrawals while maintaining relative sterility.

Standard technique recommendations:

• Add the diluent, letting it run slowly down the wall of the vial, without injecting it directly onto the powder.
• Do not shake vigorously; gently swirl or rotate the vial until fully dissolved.
• For studies without preservatives, sterile water for injection or saline solution may be used, according to the requirements of the protocol.

These indications are for general laboratory handling and do not constitute instructions for use in people.

Stability and storage

Standard handling recommendations for research peptides:

• Lyophilized (powder): store frozen, protected from light and moisture. In dry form, short peptides usually remain stable for prolonged periods.
• Reconstituted (in solution): keep refrigerated and use within a short term; for more prolonged storage, freezing in aliquots is usually preferred.
• Avoid the repeated freeze-thaw cycles, which can degrade the peptide; divide into single-use aliquots.

These ranges are a general laboratory guide; the specific conditions depend on the formulation and the investigator's protocol.

Safety profile

The safety profile of Pinealon in humans is unknown. No formal toxicological studies or peer-reviewed human safety data were identified in regulatory sources.

The reviewed preclinical studies do not report manifest toxicity at the doses used, but the absence of controlled clinical trials prevents characterizing the safety profile, interactions or contraindications in people. No documented contraindications are available due to the lack of clinical studies.

The compound is not approved as a drug by the FDA or the EMA. It must be handled only under laboratory conditions and with the standard precautions applicable to research reagents. Product for research use.

Comparative context

Pinealon is part of the family of short bioregulator peptides associated with the Khavinson school. It shares with other members the conceptual framework of gene expression regulation through short peptides and an evidence base that is mostly Russian and preclinical.

Some qualitative comparisons within its class:

• Epitalon (Epithalon, Ala-Glu-Asp-Gly): is studied mainly in relation to telomerase and pineal regulation. Pinealon, by contrast, is investigated above all for its neuronal cytoprotection against ROS.
• Vesugen and Cortagen: share the same approach of short bioregulator peptides.

The distinguishing feature of Pinealon compared to these analogues is its experimental focus on the protection of neuronal cells against oxidative stress, rather than on longevity pathways or endocrine regulation.

History and development

Pinealon is a synthetic tripeptide of sequence Glu-Asp-Arg (EDR) which, according to the literature, was originally derived from the neuroprotective preparation Cortexin (PMID 33396470).

Its development falls within the research line of the short bioregulator peptides driven by the Khavinson school of the Institute of Bioregulation and Gerontology in Saint Petersburg. This current studies how peptides of few amino acids could modulate gene expression and exert cytoprotective effects.

To date, the characterization of Pinealon comes essentially from preclinical studies by this group; no Western clinical development programs or regulatory registrations were found that have advanced toward its approval as a medication.

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Scientific references (6)

Peer-reviewed literature on Pinealon, with its PubMed identifier when available:

• Role of Mono- and Divalent Ions in Peptide Glu-Asp-Arg-DNA Interaction (Silanteva IA et al. · The journal of physical chemistry. B · 2019) PMID 30762356.
• Pinealon protects the rat offspring from prenatal hyperhomocysteinemia (Arutjunyan A et al. · International journal of clinical and experimental medicine · 2012) PMID 22567179.
• Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes (Khavinson V et al. · Rejuvenation research · 2011) PMID 21978084.
• [EFFECT OF SYNTHETIC PEPTIDES ON AGING OF PATIENTS WITH CHRONIC POLYMORBIDITY AND ORGANIC BRAIN SYNDROME OF THE CENTRAL NERVOUS SYSTEM IN REMISSION]. (Meshchaninov VN, et al. · Adv Gerontol · 2015) PMID 26390612.
• Neuroprotective Effects of Tripeptides-Epigenetic Regulators in Mouse Model of Alzheimer's Disease. (Khavinson V, et al. · Pharmaceuticals (Basel) · 2021) PMID 34071923.
• Short Peptides Protect Fibroblast-Derived Induced Neurons from Age-Related Changes. (Kraskovskaya N, et al. · Int J Mol Sci · 2024) PMID 39518916.

Guides and articles about Pinealon

Lecturas del blog de EXOMA que la editorial asoció a este compuesto:

• Khavinson Bioregulators: Complete Guide to Cytomax Peptides

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