Pinealon

Pinealon (EDR) is a synthetic tripeptide composed of three amino acids — glutamic acid, aspartic acid, and arginine (Glu-Asp-Arg) — originally isolated from Cortexin, a neuroprotective polypeptide complex derived from bovine brain tissue. With a molecular weight of approximately 418.4 Da, it is one of the smallest neuroprotective peptides studied in the Khavinson bioregulator family. Unlike most therapeutic peptides that operate through cell-surface receptor binding, Pinealon's compact size allows it to cross lipid bilayers, including the nuclear membrane, enabling it to interact directly with DNA and regulate gene transcription. It has demonstrated binding in the promoter regions of genes including CASP3, NES, GAP43, APOE, SOD2, PPARA, PPARG, and GPX1 — many of which govern neuronal survival, apoptosis, and antioxidant defense.

The primary mechanism of Pinealon centers on its epigenetic regulatory capacity. By modulating the expression of genes involved in neuronal metabolism and oxidative stress resistance, Pinealon can suppress the accumulation of reactive oxygen species (ROS) in neuronal cells, reduce necrotic cell death, and preserve the structure of dendritic spines — the small protrusions on neurons that are critical for synaptic communication. Loss of dendritic spines is a hallmark of neurodegenerative diseases such as Alzheimer's and Huntington's disease. Research has also demonstrated that Pinealon supports the expression of 5-tryptophan hydroxylase, the rate-limiting enzyme in serotonin biosynthesis, suggesting roles in mood regulation and neuroprotective signaling. Additionally, its effects on antioxidant enzyme gene expression (SOD2, GPX1) indicate a capacity to bolster the brain's intrinsic defenses against oxidative damage.

The current body of research on Pinealon consists predominantly of preclinical animal studies and a limited number of small human trials, primarily conducted in Russia at the Saint Petersburg Institute of Bioregulation and Gerontology. These studies have shown promising results in models of Alzheimer's disease, Huntington's disease, and traumatic brain injury sequelae, as well as in prenatal hypoxia models assessing oxidative stress. A small clinical study involving oral Pinealon in patients with cerebral asthenia following cranial trauma reported improvements in memory, headache severity, emotional balance, and work performance. While these findings are encouraging, large-scale randomized controlled trials conducted by independent Western research groups are absent, and the peptide remains classified as a research compound outside Russia.

Pinealon was developed by Professor Vladimir Khavinson and his colleagues at the Saint Petersburg Institute of Bioregulation and Gerontology in Russia, as part of a decades-long programme investigating short peptide bioregulators. Khavinson's group originally derived neuroprotective peptides by fractionating Cortexin — a polypeptide complex extracted from bovine and porcine cerebral cortex tissue that had been used clinically in Russia since the Soviet era. Through systematic analysis of Cortexin's active constituents, they identified the tripeptide Glu-Asp-Arg (EDR) as a key component responsible for its neuroprotective and gene-regulatory activity. The synthetic version was designated Pinealon and developed as a "cytogen" — a class of synthesized short peptides in Khavinson's taxonomy, distinct from the naturally derived "cytomaxes." The name reflects its targeting of pineal gland and cortical neural tissue. Over the course of his 40-year research career, Khavinson authored more than 775 scientific publications and 196 patents, and introduced six peptide-based pharmaceuticals and 64 peptide food supplements into clinical practice across Russia and CIS countries.

Pinealon has been studied in the context of Alzheimer's and Huntington's disease models, prenatal hypoxia, cerebral asthenia, and general aging. A key 2011 publication in Rejuvenation Research confirmed its ability to suppress ROS accumulation and reduce necrotic cell death in cerebellar granule cells and other neuronal cell types. Subsequent work published in the 2010s and 2020s continued to characterize its epigenetic mechanisms and role in preserving dendritic spine morphology. In Russia, Pinealon is commercially available as a dietary supplement (biologically active additive, or BAA) in capsule form under the Cytogen product line, marketed by NPCRIZ (Scientific-Production Center of Revitalization and Health). International awareness of Pinealon has grown in recent years alongside wider interest in Khavinson peptides as a class of experimental neuroprotective and anti-aging agents.