Pinealon (Glu-Asp-Arg) - Pineal Gland-Derived Neuroprotective Peptide

Pinealon for Research: Complete Scientific Overview

Pinealon is a synthetic tripeptide with the amino acid sequence Glu-Asp-Arg (Glutamic Acid-Aspartic Acid-Arginine), derived from the pineal gland. As part of a family of short-chain pineal peptides, Pinealon has been investigated for its neuroprotective, cerebroprotective, and geroprotective properties. Research suggests that Pinealon may influence gene expression related to circadian rhythm regulation, neuronal survival, synaptic plasticity, and oxidative stress resistance, making it a valuable tool for studying pineal gland function and age-related neurological decline. The pineal gland, known as the "third eye," is the primary site of melatonin synthesis and plays a central role in circadian biology, making Pinealon particularly relevant for chronobiology and neuroendocrinology research.

Mechanism of Action

Pinealon exerts its biological effects through multiple well-characterized mechanisms that collectively promote neuronal health and resilience:

• Gene Expression Modulation: Regulates expression of genes involved in neuronal survival, synaptic function, and oxidative stress response, including upregulation of BCL-2 (anti-apoptotic), BDNF (neurotrophic factor), SOD (superoxide dismutase), and GPx (glutathione peroxidase).
• Neuroprotection: Protects neurons from oxidative stress, excitotoxicity, and apoptosis through modulation of survival signaling pathways including PI3K/AKT and MAPK/ERK cascades.
• Cerebroprotection: Reduces ischemic damage and improves neurological outcomes in cerebral ischemia research models via preservation of the blood-brain barrier and reduction of infarct volume.
• Circadian Rhythm Regulation: May influence pineal gland function and melatonin synthesis pathways, affecting circadian entrainment and sleep-wake cycle regulation through modulation of clock gene expression.
• Anti-inflammatory Effects: Reduces neuroinflammation through modulation of microglial activation and downregulation of pro-inflammatory cytokines (IL-1β, TNF-α, IL-6) while promoting anti-inflammatory mediators.
• Mitochondrial Protection: Preserves mitochondrial membrane potential, reduces reactive oxygen species (ROS) production, and maintains ATP synthesis in neuronal cells under metabolic stress.
• Synaptic Plasticity Enhancement: Promotes dendritic spine density and synaptic protein expression, contributing to improved neuronal connectivity and cognitive function.

Key Research Applications

• Neuroprotection & Cerebral Ischemia: Investigating Pinealon's protective effects in stroke, middle cerebral artery occlusion (MCAO), and global ischemia models, including infarct volume reduction and functional recovery assessment.
• Pineal Gland Function & Circadian Rhythms: Studying the role of pineal peptides in melatonin synthesis, clock gene expression, and circadian entrainment in both in vitro and in vivo models.
• Anti-Aging & Geroprotective Research: Evaluating Pinealon's effects on age-related cognitive decline, oxidative stress accumulation, and cellular senescence in aging animal models.
• Neurodegenerative Disease Models: Investigating therapeutic potential in Alzheimer's disease (amyloid-beta toxicity, tau pathology), Parkinson's disease (dopaminergic neuron protection), and Huntington's disease models.
• Oxidative Stress & Mitochondrial Function: Studying Pinealon's antioxidant properties and mitochondrial protective effects in neuronal cell cultures and isolated mitochondria preparations.
• Cognitive Enhancement & Memory: Evaluating effects on learning, memory consolidation, and synaptic plasticity using behavioral paradigms (Morris water maze, novel object recognition, fear conditioning).
• Sleep & Chronobiology: Investigating Pinealon's influence on sleep architecture, circadian phase shifting, and melatonin rhythms in diurnal and nocturnal animal models.
• Neuroinflammation: Studying microglial activation, astrocyte reactivity, and inflammatory cytokine profiles in models of neuroinflammatory disease.

Comparison: Pinealon vs Related Pineal Peptides

• Pinealon (Glu-Asp-Arg - EDR): Tripeptide; primary focus on neuroprotection, cerebroprotection, anti-aging; influences gene expression related to neuronal survival and oxidative stress.
• Epithalon (Ala-Glu-Asp-Gly - AEDG): Tetrapeptide; telomerase activation, anti-aging, circadian regulation, immune modulation.
• Melatonin: Pineal hormone; circadian regulation, potent antioxidant, sleep promotion, chronobiotic effects.

Chemical Information & Handling

CAS Number: Refer to COA
Molecular Formula: C15H27N7O8
Molecular Weight: 433.4 g/mol
Sequence (3-Letter): Glu-Asp-Arg
Sequence (1-Letter): EDR
Purity: >99% (HPLC)
Form: Lyophilized powder
Solubility: Soluble in water, saline, PBS, and DMSO (excellent aqueous solubility due to charged residues)
Storage: -20°C (lyophilized), 4°C (reconstituted). Stable for 24 months when stored at -20°C.
Reconstitution: Reconstitute with sterile bacteriostatic water or sterile saline. Gently swirl until fully dissolved. Do not vortex. Aliquot to avoid freeze-thaw cycles.

Each vial contains exactly the indicated net peptide weight. For long-term storage, keep lyophilized powder at -20°C away from light and moisture. Reconstituted solutions should be used within 14-30 days when stored at 4°C.

Quality Assurance

PeptideVanta's Pinealon undergoes rigorous quality control including HPLC purity analysis (>99%), ESI-mass spectrometry for molecular weight confirmation (expected 433.4 Da), endotoxin testing (<0.5 EU/mg), sterility testing, and residual solvent analysis. Each batch is accompanied by a Certificate of Analysis (COA) with complete testing results. The peptide is synthesized using solid-phase peptide synthesis (SPPS) with Fmoc chemistry, followed by HPLC purification and lyophilization under sterile conditions.