Pinealon 20mg

Compound Name: Pinealon

Synonyms: Glu-Asp-Arg tripeptide, Epithalamin Short Peptide

CAS Number: 175175-23-2

Molecular Formula: C₁₅H₂₆N₆O₈

Molecular Weight: ~418.40 g/mol

Structure: Synthetic tripeptide

Peptide Sequence: H-Glu-Asp-Arg-OH

Chemical Structure:

Source: PubChem

Mechanism of Action: Pinealon acts by suppressing the accumulation of reactive oxygen species (ROS) in various cell types, leading to reduced oxidative stress and necrotic cell death. It modulates intracellular signaling pathways such as ERK1/2 and the cell cycle, supports antioxidant enzyme activity, and stabilizes cellular membranes. Pinealon also normalizes neurochemical imbalances in models of metabolic and hypoxic stress, influences NMDA receptor subunit gene expression, and restores normal neurotransmitter rhythms, collectively promoting neuroprotection and metabolic resilience^1,2,4.

Biological Activity: Pinealon exhibits pronounced antioxidant, neuroprotective, and geroprotective activities. It restricts ROS accumulation and cell loss under stress, supports cell proliferation, improves cognitive function in aged and diabetic animal models, and restores diurnal rhythms of neurotransmitters in the brain, especially norepinephrine^1-4. It also enhances learning and memory by modulating NMDA receptor subunit expression and bolsters the antioxidant defense system^2,3.

Storage: Store at –20°C in a dry, dark environment.

Drug Categories: Neuroprotective Peptides, Antioxidants, Cognitive Enhancers, Geroprotectors

Additional Notes: Non-toxic in studied animal models; investigational compound.

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

Pinealon is a synthetic tripeptide comprising glutamic acid, aspartic acid, and arginine, designed with structural motifs derived from natural brain peptides. Recognized for its potent neuroprotective and antioxidant properties, Pinealon effectively restricts the accumulation of harmful reactive oxygen species in neural and non-neural cells under conditions of metabolic or hypoxic stress¹. Experimental research demonstrates its capacity to reduce cell death, delay activation of stress-related signaling pathways, and promote cell cycle progression, thereby increasing cell viability and supporting regeneration^1,4.

Pinealon’s therapeutic profile has been validated in multiple animal models, showing a positive impact on cognitive functions such as learning and memory, even in aged, diabetic, or stressed subjects^2,3. By correcting neurochemical imbalances and restoring healthy rhythms of norepinephrine and oxidative stress markers, Pinealon demonstrates wide-ranging benefits in brain health, adaptation to stress, and overall cell resilience^3,4. These effects may involve interaction with key receptor systems, including NMDA receptor gene regulation, and enhancement of endogenous antioxidant enzyme activity².

Research Highlights

• Neuroprotective Effects: Demonstrated to protect neurons from oxidative and excitotoxic damage by suppressing reactive oxygen species (ROS) accumulation, stabilizing cellular membranes, delaying ERK1/2 stress signaling, and preventing necrotic cell death; shown to preserve neuronal viability and function in models of hypoxia, hyperhomocysteinemia, and diabetes^1-4.
• Cognitive Enhancement and Learning Support: Improves spatial learning, navigation performance, and memory retention in young, aged, and metabolically impaired animal models; benefits correlate with modulation of NMDA receptor subunit gene expression, normalization of Grin2a/Grin2b ratios, and improved synaptic plasticity^2,3.
• Antioxidant and Anti-Stress Adaptation: Potently restricts intracellular and extracellular ROS production, elevates antioxidant enzyme activity (superoxide dismutase, glutathione peroxidase), and mitigates prooxidant stress responses; supports adaptation to acute hypoxic exposure and metabolic challenges by bolstering endogenous defense mechanisms^1,3.
• Regulation of Neuroendocrine Rhythms: Restores diurnal dynamics of norepinephrine in the medial preoptic area of the hypothalamus impaired by hyperhomocysteinemia; contributes to normalized gonadotropin-releasing hormone (GnRH) regulation and supports reproductive function in female rats under metabolic stress⁴.
• Geroprotective Properties: Enhances learning and resilience in aged animal models under cognitive stress, potentially linked to modulation of the caspase‑3 system in brain structures; supports brain metabolic homeostasis and reduces the negative impact of age- related oxidative imbalance³.

Mechanism of Action

Reactive Oxygen Species (ROS) Suppression and Antioxidant Effects

• Reduces intracellular and extracellular ROS accumulation in neurons and neutrophils via dose-dependent mechanisms¹.
• Enhances the activity of key antioxidant enzymes (superoxide dismutase, glutathione peroxidase) under stress conditions¹.
• Prevents ROS-induced cell death and necrosis, supporting cell viability and neuroprotection¹.

ERK1/2 Modulation and Cell Cycle Regulation

• Delays and suppresses ERK1/2 phosphorylation, interfering with oxidative and stress signaling cascades¹.
• Promotes redistribution of cells through G1, S, and G2 phases, fostering proliferative activity even under stress¹.

NMDA Receptor Subunit Regulation

• Modulates gene expression of NMDA receptor subunits (Grin1, Grin2a, Grin2b, Grin2d) in the hippocampus².
• Normalizes Grin2a/Grin2b ratio, which is linked to improved cognitive function and learning in diabetic animal models².

Circadian and Neurotransmitter Regulation

• Restores diurnal dynamics and proper rhythmicity of neurotransmitters (e.g., norepinephrine) in hypothalamic areas involved in reproduction and cognition⁴.
• Supports neuroendocrine homeostasis under conditions of metabolic and oxidative stress⁴.

Pharmacokinetic Profile

• Route of Administration: Subcutaneous injection (SC)
• Dosing Frequency: Once daily
• Half-life: 6-8 hours

Formulation & Handling

• Supplied as lyophilized powder or sterile solution for laboratory use
• Typical storage at –20°C, protected from light and moisture

Selected Clinical Trial Activity

Pinealon is a research-grade compound that has been studied in laboratory settings but has not undergone full clinical development. It is not approved for therapeutic use in humans, and no large-scale clinical trials have been conducted to evaluate its safety or efficacy as a medication. Pinealon is supplied strictly for laboratory research and investigational purposes only.

References

¹Khavinson, V. et al. Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Rejuvenation Res. 14, 535–541 (2011).

²Karantysh, G. V. et al. Effect of Pinealon on learning and expression of NMDA receptor subunit genes in the hippocampus of rats with experimental diabetes. Neurochem. J. 14, 314–320 (2020).

³Mendzheritskii, A. M. et al. Effect of peptide geroprotectors on navigation learning in rats of different ages and caspase-3 systems in their brain structures. Adv. Gerontol. 4, 37–45 (2014).

⁴Korenevskii, A. V. et al. Pinealon corrects hyperhomocysteinemia-induced disturbances of the diurnal dynamics of hypothalamic norepinephrine content in female rats. Neurochem. J. 8, 205–207 (2014).