Pinealon

Important: Pinealon is not approved by the FDA for human use. This page is intended for research and educational purposes only and does not constitute medical advice or an endorsement to purchase for personal use.

Pinealon is a synthetic tripeptide (composed of three amino acids: Glutamic acid, Aspartic acid, and Arginine, or Glu-Asp-Arg) known as a bioregulator, often used for neuroprotective and nootropic purposes. It is designed to act on the central nervous system, supporting brain health, cognitive function, and mental clarity.

Key Benefits

• Supports cognitive function by helping maintain memory, focus, and mental clarity.
• Promotes healthy brain aging through its potential neuroprotective effects.
• May help protect neurons from oxidative stress and age-related cellular damage.
• Supports cellular health by influencing gene expression involved in cell repair and function.
• May improve sleep quality and overall well-being by supporting healthy nervous system function.
• Supports healthy aging processes through its effects on cellular regulation and tissue maintenance.

FDA-Approved Uses

⚠️ NOT FDA APPROVED FOR ANY HUMAN INDICATION ⚠️

Pinealon has no FDA-approved use in the United States or any major Western regulatory jurisdiction.

Regulatory status (as of May 2026):
– Not on the FDA 503A Bulks List (Category 1) — no confirmed legal 503A compounding pathway as of May 2026
– No PCAC review scheduled specifically for Pinealon as of May 2026
– Available in Western markets as a ‘lab-use’ / research compound only
– Russia: Used clinically within Khavinson’s bioregulator peptide framework

⚠️ NAME CLARIFICATION: Despite being called ‘Pinealon,’ this peptide was NOT derived from the pineal gland. The name reflects its proposed neurological and circadian-rhythm-supporting effects, not its origin. It is a brain-specific bioregulator developed by the same Khavinson group that created Epitalon and Thymalin.

Conditions studied in research (Russian literature — NOT FDA-reviewed):

• Cognitive enhancement and neuroprotection — primary research focus
• Sleep quality improvement / circadian rhythm support
• Alzheimer’s disease and neurodegeneration prevention (preclinical)
• Age-related retinal degeneration (eye drop protocols in Russian research)
• Antioxidant brain aging prevention
• Traumatic brain injury recovery support (animal models)
• 7General anti-aging / longevity (neuroepigenetic mechanism)

WADA status: NOT on WADA Prohibited List — advantage for athletes

Trade Names in the USA and Manufacturers

No FDA-approved trade name or manufacturer in USA.

Also known as:
– EDR peptide (single-letter amino acid abbreviations: Glu-Asp-Arg)
– Pineal peptide bioregulator

Discovery and development:

• Developed by Prof. Vladimir Khavinson at the St. Petersburg Institute of Bioregulation and Gerontology, Russia
• Part of the same Khavinson bioregulator family as Epitalon (AEDG), Thymalin, and Vilon
• Specifically designed as a brain-targeted bioregulator (retina and cerebral cortex tropism)
• Primary research institution: St. Petersburg Institute of Bioregulation and Gerontology

US availability (as of May 2026):

• Grey-market research peptide vendors: Available as lyophilized powder and oral capsules (‘research use only’)
• No licensed 503A compounding pharmacy pathway currently authorized
• Some US telehealth longevity clinics include Pinealon in nootropic peptide stacks

Key combination use:
– Pinealon (morning, cognitive) + Epitalon (bedtime, circadian/telomere) is a common community pairing
– Also combined with Semax for cognitive synergy (complementary mechanisms)

Molecular identity:
– Synthetic tripeptide (3 amino acids): Glu-Asp-Arg (EDR)
– MW: ~418.4 Daltons — extremely small; enables BBB penetration
– BBB penetration: Via PEPT2 transporter (proton-coupled oligopeptide transporter 2) — documented transport mechanism
– Chemical formula: C₁₄H₂₅N₅O₈

Dosage

⚠️ No FDA-approved dosing. All protocols from Russian clinical research and community use.

KEY PRINCIPLE: Cyclical use — NOT daily continuous. Consistent with Khavinson bioregulator family protocols.

Oral / sublingual (accessible route due to small MW):
Standard oral dose: 20 mg/day
Cycle duration: 20–30 consecutive days
Frequency per year: 2–3 cycles
Sublingual: 5–6 drops held under tongue 30–60 sec, 3–4x daily
[Sublingual likely offers better absorption than swallowed capsules]

Subcutaneous injection (most direct route):
Dose: 5–10 mg SC once daily
Cycle: 10–20 consecutive days
Frequency per year: 2–3 cycles
Note: Some sources cite 100–300 mcg SC as injectable dose; 1 mg cited by others
[Discrepancy in community dosing reflects absence of established human pharmacokinetic studies]

Eye drop formulation (Russian research; niche use):
Used in some Khavinson retinal degeneration studies
Not a standard community protocol

Reconstitution (injectable):
Lyophilized powder; reconstitute with Bacteriostatic Water
Store lyophilized at -18°C or below
Reconstituted: refrigerate; use within 14–21 days
Very stable vs. larger peptides due to extremely small size (~418 Da)

Pricing

No FDA-approved commercial pricing.

Research peptide vendors and supplement capsules (unregulated):
Oral capsules (20 mg): ~20–20–50 per cycle supply (30 capsules)
Injectable vials: ~30–30–80 per vial
Cost per cycle: ~40–40–100
Annual cost (2–3 cycles): ~80–80–300

Pinealon is among the most affordable longevity peptides due to:

• Extremely small MW (3 amino acids; simple synthesis)
• Low doses required
• Cyclical (not daily) use protocol
• Oral bioavailability (no needle required)

Note: Some US telehealth clinics offer Pinealon as part of broader nootropic peptide protocols at 100–100–300/month bundled with other compounds.

Tips

• Despite being called ‘Pinealon,’ this peptide does NOT originate from the pineal gland and does NOT directly affect melatonin production the way Epitalon does. Pinealon’s mechanism is primarily antioxidant neuroprotection and chromatin-level gene expression normalization.
• Pinealon is not a stimulant and not a sedative. Its effects are gradual and cumulative — working at gene expression level. Do not expect an acute cognitive ‘hit’ similar to Semax or racetams. Benefits are structural and emerge over weeks of cyclical use.
• The combination of Pinealon (morning) + Epitalon (bedtime) is a popular pairing targeting complementary aging mechanisms: brain-specific antioxidant protection (Pinealon) and systemic circadian/telomere regulation (Epitalon).

Side Effects

Very favorable safety profile based on available data — reflects Khavinson bioregulator class as a whole:

Commonly reported (mild and transient):

• Injection site reactions: Mild redness, swelling, slight discomfort at injection site (most common with injectable form)
• Headache: Mild; occasional; early in protocol
• Nausea: Mild; uncommon; more frequent with oral high-dose administration
• General well-tolerance: Community and Russian research reports consistently note minimal adverse effects

Not typically associated with:
– Stimulant-like effects (insomnia, anxiety, elevated heart rate) — Pinealon is not a stimulant
– Sedation or drowsiness — not a sedative
– Hormonal disruption — no effects on GH, IGF-1, cortisol, or reproductive hormones reported

⚠️ Theoretical concern — caspase-3 anti-apoptotic mechanism:

• Pinealon reduces caspase-3 expression (anti-apoptotic effect in healthy neurons under oxidative stress)
• However, caspase-3 also plays a role in eliminating damaged or pre-cancerous cells
• In active malignancy: reducing caspase-3 could theoretically protect cancer cells from apoptosis
• This mechanism-based concern is flagged but not confirmed in human studies

2025 systematic review note (applies to Khavinson bioregulator class):
‘Information regarding critical issues about this peptide’s safety is missing’ — comprehensive human safety characterization has not been completed

⚠️ Long-term safety: Absent from published literature. All safety data from short-term Russian clinical studies.

Contraindications

No formal FDA contraindications (no approved label).

Based on mechanism and Khavinson bioregulator class:

Strong caution / avoid:
– Active malignancy: Caspase-3 anti-apoptotic mechanism may protect cancer cells from programmed death — avoid until human oncology safety data exists
– Pregnancy and breastfeeding: No safety data; not recommended

Use with caution:
– Children and adolescents: Gene expression modulation in developing brain is unpredictable; not recommended
– Patients with active seizure disorders: Neuroprotective effects on neuronal excitability not characterized in epilepsy context
– Known hypersensitivity to Pinealon or components

No evidence of interactions with common medications, hormones, or metabolic pathways documented in available literature.

Pharmacology

Pinealon (Glu-Asp-Arg; EDR) is a synthetic tripeptide (3 amino acids) and member of Prof. Khavinson’s ‘bioregulator peptide’ family, developed at the St. Petersburg Institute of Bioregulation and Gerontology, Russia.

Molecular details:
– Sequence: Glu-Asp-Arg (glutamic acid – aspartic acid – arginine)
– MW: ~418.4 Daltons — among the smallest bioactive peptides; smaller than even Epitalon (390 Da) is slightly smaller; Pinealon at 418 Da is still exceptionally small
– Chemical formula: C₁₄H₂₅N₅O₈
– Tissue tropism: Brain and retina — specifically targeted to cerebral cortex and retinal neuronal populations

Blood-brain barrier penetration:
– Documented transport via PEPT2 (proton-coupled oligopeptide transporter 2) — a carrier expressed on brain endothelial cells and choroid plexus
– Small MW enables passive diffusion in addition to PEPT2-mediated active transport
– This gives Pinealon genuine CNS access — a significant advantage over larger peptides that cannot cross the BBB

Oral bioavailability:
– Small size enables resistance to gastrointestinal peptide degradation to a degree not seen in larger peptides
– Oral and sublingual administration viable (contrast with most peptides >1 kDa requiring injection)

Class: Bioregulator peptide — acts on chromatin and gene expression rather than traditional receptor-ligand pharmacology

Mechanism of action

Pinealon’s mechanism operates through several interconnected neuroprotective pathways:

1. Chromatin Remodeling / Epigenetic Gene Expression Normalization (primary mechanism per Khavinson bioregulator theory):
Pinealon (EDR) interacts directly with chromatin — binding to specific gene promoter/regulatory regions in neuronal cells.
→ Normalizes age-associated dysregulation in gene expression in brain and retinal tissue
→ ‘Resets’ epigenetic drifts associated with cellular aging
→ Acts as an epigenetic regulator restoring transcriptional patterns toward younger, healthier states
This is the foundational mechanism proposed for the entire Khavinson bioregulator class

2. Antioxidant Gene Upregulation:
→ Upregulates superoxide dismutase (SOD) and catalase expression in neuronal cells
→ Directly scavenges reactive oxygen species (ROS)
→ Reduces oxidative DNA damage — antimutagenic neuroprotection
Reference: Khavinson et al. (2011, Rejuvenation Research): ‘Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes’

3. Anti-Apoptotic Effects (caspase-3 suppression):
Pinealon reduces caspase-3 expression in neurons facing oxidative stress
→ Prevents premature neuronal death from ROS-induced apoptosis
⚠️ Dual-edge: caspase-3 also eliminates pre-cancerous cells — reason for active malignancy contraindication

4. Circadian Rhythm Support:
Supports the neuronal populations and gene expression patterns governing the sleep-wake regulatory system
→ Improves sleep ARCHITECTURE (deep sleep quality) from biological infrastructure level
→ Does NOT directly cause sedation; works on regulatory mechanisms underlying sleep quality

5. Neuroprotection in Retinal Tissue:
Specific tropism for retinal neuronal cells
→ Reduces retinal cell death from oxidative stress and age-related degeneration
→ Basis for eye drop formulations in Russian retinal disease studies

Result Claims from Different Companies

Prof. Khavinson / St. Petersburg Institute of Bioregulation and Gerontology (primary research group):

In vitro / cell studies:
– Khavinson et al. (2011, Rejuvenation Research): Pinealon demonstrated statistically significant increases in cell viability, reduction in free radical levels, and activation of proliferative processes in neuronal cell cultures
– Demonstrated epigenetic regulation: Pinealon binds to specific DNA promoter sequences in neuronal genes associated with anti-aging and neuroprotection

Animal studies:
– Neuroprotective effects confirmed in oxidative stress models
– Retinal protection in age-related retinal degeneration models
– Cognitive maintenance in aging animal cohorts

Neuroepigenetics review (Ilina et al., 2022, IJMS):
– ‘Neuroepigenetic mechanisms of action of ultrashort peptides in Alzheimer’s disease’
– Pinealon and related tripeptides proposed as epigenetic regulators targeting Alzheimer’s-related gene expression

Community/clinical reports (2025–2026):
– Consistently reported: Improved sleep quality (specifically deep sleep depth, not sedation), gradual cognitive clarity over cycles, neuroprotective ‘maintenance’ effect rather than acute enhancement
– PeptideDeck 2026: ‘Not a nootropic — no acute sharpness. Works at gene expression level; effects gradual, cumulative, and structural’

⚠️ KEY LIMITATIONS:

• Majority of studies from ONE research group (Khavinson, St. Petersburg)
• No large-scale independent Western RCTs
• No FDA-reviewed clinical trial evidence
• Human safety not comprehensively characterized
• Optimal human dosing not established by pharmacokinetic studies

Disclaimer

This content about “Pinealon
(EDR Peptide / Glu-Asp-Arg)
Khavinson Bioregulator — Brain-Specific

⚠️ NOT FDA APPROVED
⚠️ NOT from the pineal gland (despite the name)
WADA: Not prohibited” is for informational and educational purposes only, is not medical advice, does not replace consultation with a licensed healthcare professional, and affiliate links may result in compensation at no additional cost to you.