MEDICAL DISCLAIMER: Educational research guidelines only. Lyophilized peptides are investigational chemical compounds and are NOT approved for human consumption, diagnosis, or therapy. Consult a licensed physician before any research application.
Pinealon Dosage Chart, Schedule & Reconstitution Protocol
Quickstart Highlights
Pinealon is a Khavinson-class synthetic tripeptide with the sequence Glu-Asp-Arg (EDR), designed at the Saint Petersburg Institute of Bioregulation and Gerontology as a short peptide bioregulator of the pineal-cerebrum axis. Like other short Khavinson cytogens, Pinealon is hypothesized to translocate across the plasma and nuclear membranes and bind regulatory regions of double-stranded DNA, modulating tissue-specific gene transcription in pinealocytes and cortical neurons (PMID: 22617397). Anisimov, Khavinson, and colleagues have reported that Pinealon protects neurons against oxidative and hypoxic stress, normalizes circadian gene expression, and extends median lifespan in animal models when given in repeated pulsed courses across the second half of life (PMID: 23425559). Researchers study it for sleep-wake regulation, cognitive resilience under stress, and geroprotection, often paired with Epitalon in pineal-targeted longevity protocols.
Reconstitute: Add 3 mL bacteriostatic water → 6.67 mg/mL concentration.
Easy measuring: At 6.67 mg/mL, 1 unit = 0.01 mL = 0.0667 mg (67 mcg) on a U-100 insulin syringe.
Storage: Lyophilized frozen; reconstituted refrigerated; avoid repeated freeze–thaw.
Half-life: Plasma clearance is minutes; downstream effects on neuronal gene expression and oxidative stress markers are reported to persist days to weeks per ten-day pulsed course.
Route: Subcutaneous injection in most research protocols; intramuscular and intranasal routes also appear in Russian sources targeting CNS endpoints.
Status: Khavinson-licensed research peptide bioregulator; not FDA, EMA, or MHRA approved. Human evidence base is restricted to Russian observational and translational studies.
Quick Protocol Navigation
Reconstitution Instruction & Mixing Step-by-Step
Lyophilized powder must be reconstituted carefully. Agitating peptide chains can shear disulfide bonds and render the peptide biologically inert.
Draw 3.0 mL bacteriostatic water with a sterile syringe.
Inject slowly down the vial wall; avoid foaming.
Gently swirl/roll until dissolved (do not shake).
Inject slowly; wait a few seconds before withdrawing the needle.
Do not aspirate for subcutaneous injections; inject slowly and steadily[17].
Interactive Pinealon Syringe Calculator
Currently visualizing the 20 mg vial reconstituted with 3 mL bacteriostatic water. Adjust the target dose to dynamically render syringe units.
Reconstitution Calculation: 20mg dry powder in 3mL water yields 6.67 mg/mL. To evaluate a 250mcg dose, pull to 3.8 units (4 syringe ticks).
U-100 Syringe Representation
3.8 Units (4 Ticks)
Educational reference visual. Assumes standard U-100 insulin syringe where 1.0 mL volume = 100 units.
Titration & Dose Escalation Schedules
| Days | Daily Dose | Units (per injection) (mL) |
|---|---|---|
| Days 1–5 | 1.0 mg (1,000 mcg) | 15 units (0.15 mL) |
| Days 6–14 | 1.5 mg (1,500 mcg) | 22.5 units (0.225 mL) |
| Days 15–20 | 2.0 mg (2,000 mcg) | 30 units (0.30 mL) |
Administration guidelines: Refer to guidelines | 3 mL Reconstitution
Research Supplies Quantity Planner
Scientific mathematical planning of syringes, bacteriostatic water and dry vials needed for extended research blocks using the 20 mg vial.
Peptide Vials (Pinealon, 20 mg each):
- check10‑day cycle ≈ 1 vial
- check20‑day cycle ≈ 2 vials
- check28‑day cycle ≈ 3 vials
Insulin Syringes (U‑100):
- checkPer day: 1 syringe
- check10‑day cycle: 10 syringes
- check20‑day cycle: 20 syringes
- check28‑day cycle: 28 syringes
Bacteriostatic Water (10 mL bottles): Use 3.0 mL per vial for reconstitution.
- check10‑day cycle (1 vial): 3 mL → 1 × 10 mL bottle
- check20‑day cycle (2 vials): 6 mL → 1 × 10 mL bottle
- check28‑day cycle (3 vials): 9 mL → 1 × 10 mL bottle
Alcohol Swabs: One for the vial stopper + one for the injection site each day.
- checkPer day: 2 swabs
- check10‑day cycle: 20 swabs
- check20‑day cycle: 40 swabs
- check28‑day cycle: 56 swabs → recommend 1 × 100‑count box
Mechanism of Action (MOA)
Pinealon (Glu-Asp-Arg, single-letter code EDR) was synthesized as part of Khavinson's directed-synthesis program for short cytomedins, in which the amino-acid composition of clinically active organ-extract peptide preparations was analyzed to identify the shortest active sequences mediating tissue-specific bioregulator effects. The parent preparation Epithalamin (a bovine pineal extract) had been used in Russian clinical practice for neuroendocrine and age-related disorders since the 1980s, and Pinealon was derived as one of the active short-peptide fractions targeting the central nervous system and pineal gland. Mechanistically, Khavinson's model holds that short bioregulatory peptides penetrate cell and nuclear membranes by passive diffusion and bind specific DNA sequences in gene promoter regions through electrostatic and steric complementarity, thereby altering local chromatin condensation, histone modification patterns, and transcription factor accessibility. For Pinealon, the targeted tissues include the brain (cerebral cortex, hippocampus) and the pineal gland, with documented effects on neuronal gene programs related to cell-cycle regulation (PCNA, p21), neurotrophic signaling, and oxidative stress response [3]. Linkova and colleagues showed that EDR treatment alters PCNA and p21 expression in neuronal cultures, supporting a mechanism of cell-cycle modulation relevant to neuroregeneration. A 2024 study in International Journal of Molecular Sciences reported that EDR protects fibroblast-derived induced neurons from age-related changes, including reductions in markers of senescence and oxidative damage [4]. Pinealon also has demonstrated antihypoxic and neuroprotective activity in rodent models of cerebral ischemia, with reduced infarct volume and improved functional recovery when administered prophylactically or shortly after ischemic insult. Pharmacokinetically, Pinealon (like other short Khavinson tripeptides) has a very short plasma half-life (under 5 minutes when given parenterally), but biological effects on gene expression and neuronal phenotype persist for days to weeks, consistent with epigenetic rather than receptor-occupancy mediated activity. Administration is parenteral (subcutaneous or intramuscular injection) or oral; published rodent protocols use 10–100 mcg subcutaneously or intranasally per dose. Oral capsule formulations are used in outpatient Russian bioregulator practice at 1–20 mg/day across 10–30 day cycles, repeated 2–4 times per year. Although oral bioavailability of tripeptides is theoretically poor (typically under 5–10%), Khavinson-school protocols use higher milligram doses orally on the empirical basis that observed effects appear despite low absolute systemic exposure. Effects on the central nervous system include reductions in lipid peroxidation markers in brain tissue, normalization of EEG patterns in encephalopathy models, and reported improvements in attention, memory, and mood in observational Russian clinical use. Pinealon does not bind classical neurotransmitter receptors, does not engage the HPA axis, and is not metabolized to bioactive larger peptides; its effects are attributed to short-peptide gene-regulatory activity rather than direct receptor pharmacology. Western mechanistic validation by ChIP-seq, ATAC-seq, or controlled human pharmacodynamic studies remains absent, and all clinical efficacy claims rest on preclinical and observational evidence.
Clinical Trial Efficacy Highlights
- starLinkova and colleagues reported that EDR (Pinealon) modulates expression of PCNA and p21 in neuronal cultures, supporting effects on cell-cycle regulation relevant to neuroregeneration [3].
- starA 2024 study in International Journal of Molecular Sciences demonstrated that EDR peptide protects fibroblast-derived induced neurons from age-related changes, with reductions in senescence markers and oxidative damage [4].
- starKhavinson and Anisimov documented that several short peptide bioregulators including the EDR tripeptide family support increased mean and maximum lifespan in rodent aging studies when administered cyclically across the animal's life course [5].
- starIn rodent cerebral ischemia models, Pinealon administration before or shortly after ischemic insult reduced infarct volume and improved neurologic recovery, supporting a neuroprotective profile consistent with the parent Epithalamin preparation.
- starAntihypoxic effects of Pinealon have been demonstrated in mouse models of hypobaric and normobaric hypoxia, with extended survival time and reduced markers of brain oxidative damage compared to controls.
- starPinealon was shown to inhibit cell death and reduce the level of reactive oxygen species in rat cerebellar neurons subjected to hyperhomocysteinemia in vitro, supporting a direct cytoprotective effect on neurons under metabolic stress [6].
- starRussian observational use of Pinealon in patients with age-related cognitive decline, post-stroke encephalopathy, and chronic cerebral ischemia reports improvements in subjective memory, attention, and emotional stability, though randomized controlled trials are absent.
- starCombination of Pinealon with other Khavinson peptides (Epitalon, Cortagen, Cerebrolysin) is described in Russian gerontology protocols for complex bioregulator therapy, with the rationale of complementary tissue-specific gene regulation [7].
Side Effects & Tolerability Profile
Clinical subjects transiently report mild side effects. Slowly escalating the titration dose represents the single most effective intervention to limit side effects.
- warningPinealon is generally well tolerated in Russian observational use; reported side effects are mild and infrequent, most commonly transient injection-site discomfort with subcutaneous administration.
- warningOccasional mild headache or fatigue has been reported at higher doses, typically resolving on dose reduction or course completion.
- warningGastrointestinal upset (mild nausea, loose stools) is occasionally reported with oral capsule formulations, particularly at higher milligram doses.
- warningNo tolerance, dependence, or withdrawal phenomena have been reported, consistent with the proposed epigenetic rather than receptor-occupancy mechanism.
- warningHypersensitivity reactions are rare; allergic skin reactions to peptide preparations should prompt discontinuation.
- warningNo HPA axis activation, hormonal disturbance, or significant metabolic effects have been reported with research-typical doses.
- warningDrug interaction data are not available; theoretical interactions with melatonin-modulating drugs or hormonal therapies are unstudied.
- warningReproductive, pregnancy, and lactation safety data are absent; use during these periods is not recommended.
Subcutaneous Injection Technique
Most research peptides require subcutaneous injection into fatty tissue. Never inject directly into a blood vessel or deep muscle tissue unless clinically detailed.
1. Site Selection
Common locations include the abdomen (2 inches from navel), outer upper arms, or thighs.
2. Sanitization
Thoroughly clean the selected site, stopper and vial top using 70% isopropyl alcohol prep swabs.
3. Angle & Push
Pinch the skin and insert the needle at a 45 to 90-degree angle. Depress plunger smoothly.
4. Site Rotation
Rotate injection sites continuously to avoid lipodystrophy or tissue scarring.
Frequently Asked Questions
What is the typical Pinealon dosage?expand_more
Published rodent protocols use 10–100 mcg subcutaneously or intranasally per dose. Outpatient Russian bioregulator practice uses 1–20 mg orally per day across 10–30 day cycles, repeated 2–4 times yearly. There is no Western clinical reference standard.
How is Pinealon administered?expand_more
Pinealon is administered subcutaneously, intranasally, or orally. Subcutaneous and intranasal routes achieve higher absolute bioavailability; oral capsules at higher milligram doses are used in outpatient bioregulator practice despite poor expected absorption.
Can Pinealon be stacked?expand_more
Pinealon is commonly combined with other Khavinson bioregulators such as Epitalon, Cortagen, and Cerebrolysin in Russian neurogerontology protocols. Mechanistic complementarity is the rationale; controlled-trial evidence for combination dosing is limited.
What are the side effects of Pinealon?expand_more
Side effects are mild and infrequent: occasional injection-site discomfort, transient headache or fatigue, and rare gastrointestinal upset with oral use. No serious adverse events are documented; Western-standard safety trials are lacking.
Is Pinealon FDA approved?expand_more
No. Pinealon is registered in Russia under peptide-bioregulator and dietary supplement legislation but is not approved by the FDA, EMA, or MHRA. In the United States and EU it is sold only as a research chemical and is not licensed for therapeutic use.
Academic References & Study Citations
Khavinson VK, Malinin VV. Gerontological aspects of genome peptide regulation. Karger Publishers, Basel; 2005. View Scientific Paper →
Khavinson VK, Popovich IG. Short peptides regulate gene expression. Bull Exp Biol Med. 2017;162(3):288-292. View Scientific Paper →
Lin'kova NS, Drobintseva AO, Orlova OA, et al. Peptide regulation of cell renewal processes in cultures of skin fibroblasts in elderly people. Adv Gerontol. 2016;29(2):202-208. View Scientific Paper →
Khavinson VK, Lin'kova NS, Tarnovskaya SI. Short peptides as protectors of neuronal damage induced by hypoxia. Int J Mol Sci. 2024;25(5):2496. View Scientific Paper →
Anisimov VN, Khavinson VK. Peptide bioregulation of aging: results and prospects. Biogerontology. 2010;11(2):139-49. View Scientific Paper →
Arutjunyan A, Kozina L, Stvolinskiy S, Bulygina Y, Mashkina A, Khavinson V. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia. Int J Clin Exp Med. 2012;5(2):179-85. View Scientific Paper →
Khavinson VK, Kuznik BI, Tarnovskaya SI, Lin'kova NS. Peptides and CCL11 and HMGB1 as molecular markers of aging. Adv Gerontol. 2014;27(2):359-66. View Scientific Paper →
Khavinson VK, Kvetnoy IM, Popovich IG, Anisimov VN. Mechanisms of biological activity of short peptides: cell-tissue specificity. Bull Exp Biol Med. 2020;168(3):378-381. View Scientific Paper →