# Omberacetam — Research Peptide Profile

> Omberacetam (Noopept, GVS-111): a Russian dipeptide nootropic with one 53-patient trial vs piracetam plus BDNF and neuroprotection data. Full review.

Source: https://peptpedia.org/peptide/omberacetam | Published: 2026-09-18 | Last updated: 2026-09-18

Omberacetam, marketed in Russia as Noopept, is a dipeptide-derived nootropic developed at the Zakusov Institute of Pharmacology as a piracetam analog active at far lower doses. A 53-patient Russian trial found 20 mg/day comparable to piracetam 1200 mg/day over 56 days, with 1.8-fold fewer undesirable effects. It acts partly as a prodrug for the endogenous cyclic peptide cycloprolylglycine. It has no FDA or EMA approval and no Western replication trials.

## Overview

Omberacetam is the international nonproprietary name for Noopept (development code GVS-111), a synthetic N-acylprolyl dipeptide ethyl ester designed by Gudasheva and colleagues at the Zakusov Research Institute of Pharmacology in Moscow as a peptide-logic analog of piracetam. Chemically it is N-phenylacetyl-L-prolylglycine ethyl ester (C17H22N2O4, 318.4 g/mol), a small molecule built on a Pro-Gly dipeptide scaffold rather than a classical oligopeptide. It is registered as a drug in Russia, where it is sold as 10 mg oral tablets, and it has the most human-relevant evidence base of any compound in the grey-market nootropic peptide category: a 56-day randomized comparative trial against piracetam in 53 patients with mild cognitive disorders of vascular and post-traumatic origin. Preclinically, it raises hippocampal NGF and BDNF expression, protects neurons from glutamate and amyloid toxicity, and attenuates tau hyperphosphorylation in cellular Alzheimer models. It is rapidly hydrolyzed in vivo, and one of its metabolites, the endogenous diketopiperazine [cycloprolylglycine](/peptide/cyclic-glycine-proline) (cPG), is itself bioactive and likely mediates part of the effect. No Western regulator has reviewed it, and the clinical literature remains almost entirely Russian.

## Molecular Profile

- **Category:** cognitive-enhancement
- **Molecular formula:** C17H22N2O4
- **Molecular weight:** 318.4 g/mol
- **CAS number:** 157115-85-0
- **Amino acid sequence:** N-phenylacetyl-L-prolylglycine ethyl ester (dipeptide mimetic)
- **Also known as:** Noopept, GVS-111, N-Phenylacetyl-L-Prolylglycine Ethyl Ester, Noopept Ethyl Ester
- **Half-life:** Short for the parent ester (rapid hydrolysis in rodents); the cycloprolylglycine metabolite persists longer
- **Solubility:** Lipophilic ethyl ester; poorly soluble in water, supplied as oral tablets in clinical use
- **Storage:** Store dry, protected from moisture (ester hydrolysis); tablets at room temperature.

## Mechanism of Action

Omberacetam's pharmacology combines neurotrophic, anti-excitotoxic, and prodrug components. Acute and chronic administration increased NGF and BDNF mRNA in rat hippocampus, with the hippocampal neurotrophin response present after a single dose (PMID: 19240853). It protected hippocampal HT-22 neurons from glutamate toxicity and preserved calcium homeostasis in cultured slices, indicating anti-excitotoxic activity (PMID: 27265136). In an A-beta(25-35) PC12 cell model it attenuated apoptosis and tau hyperphosphorylation while protecting mitochondrial function (PMID: 25096780). As an ethyl ester it is hydrolyzed to release cycloprolylglycine, an endogenous cyclic dipeptide detected in brain after dosing (PMID: 30378564), which itself modulates IGF-1 bioavailability. Clinically it shows a balanced profile of nootropic, mild psychostimulant, and anxiolytic effects rather than pure stimulation (PMID: 19234797).

## Key Research Findings

- Omberacetam is the INN for Noopept (GVS-111), a dipeptide-scaffold nootropic registered as a drug in Russia, with verified identity C17H22N2O4 (318.4 g/mol), CAS 157115-85-0.
- It has the strongest human evidence in its class: a 56-day randomized trial in 53 patients where 20 mg/day matched piracetam 1200 mg/day with 1.8-fold fewer undesirable effects.
- It is a prodrug: the ester hydrolyzes rapidly, releasing cycloprolylglycine, an endogenous IGF-1-related diketopiperazine that reaches the brain and carries its own pharmacology.
- Preclinical work shows hippocampal NGF/BDNF upregulation, anti-excitotoxic protection, and attenuated tau hyperphosphorylation, but no human Alzheimer or Western replication trial exists.

## Omberacetam Pharmacokinetics: A Fast-Hydrolysis Prodrug

Omberacetam's pharmacokinetics are defined by rapid ester hydrolysis: the parent compound disappears quickly, while its metabolite cycloprolylglycine persists and reaches the brain. This is one of the few grey-market nootropics with actual published pharmacokinetic studies.

### Absorption and Hydrolysis

- Interspecies pharmacokinetic work published in 2004 documented measurable but species-variable exposure of the parent compound after dosing, establishing early that GVS-111 does not circulate unchanged for long (PMID: 15079908).
- A 2018 rat pharmacokinetic study tracked Noopept and its active metabolite cycloprolylglycine simultaneously, confirming rapid conversion of the parent ester and persistence of the diketopiperazine metabolite (PMID: 30378564).
- Clinical dosing is oral (10 mg tablets twice daily in the human trial), consistent with an ester prodrug designed for gut absorption followed by systemic hydrolysis.

### The Cycloprolylglycine Dimension

- Cycloprolylglycine (cPG), the diketopiperazine formed from Pro-Gly, is an endogenous compound also generated from IGF-1 metabolism; in rat pharmacokinetic work it was orally available and reached both plasma and brain tissue, unusual behavior for a peptide-class molecule; no human cerebrospinal fluid data has been published (PMID: 30378564).
- The metabolite is pharmacologically active in its own right: a 2002 study documented antithrombotic activity for both GVS-111 and cyclo-L-prolylglycine (PMID: 12109290), and later work links cPG to normalization of IGF-1 function in the aging brain.
- This prodrug architecture complicates interpretation of in vitro Noopept results: effects seen with the ester in cell culture may be mediated by cPG in vivo, and potency rankings between the two forms have not been definitively mapped.

## Safety & Tolerability

Omberacetam has the best human tolerability data of any compound in this category: one 56-day comparative trial reported 1.8-fold fewer undesirable effects than piracetam, with effects that were transient and of insignificant severity. That said, the human record is a single small Russian trial plus regional clinical reports, long-term safety is uncharacterized, and no Western regulator has reviewed the compound.

**Human data status:** Human data consist of one 56-day randomized comparative trial (53 enrolled, 41 completed) and Russian clinical reports. No large, placebo-controlled, or Western-standard safety trial exists, and post-marketing data outside Russia is absent.

**Regulatory status:** Registered as a drug (Noopept) in Russia and some CIS states; not approved by the FDA or EMA; sold elsewhere as a supplement or research compound.

- In the 53-patient trial, Noopept at 20 mg/day for 56 days produced 1.8-fold fewer undesirable effects than piracetam at 1200 mg/day; the effects attributable to Noopept (sleep disturbance, blood pressure increase in two patients) were transient and of insignificant severity. (evidence tier: human-interventional; [PMID 19234797](https://pubmed.ncbi.nlm.nih.gov/19234797/))
- A dedicated in vitro study found Noopept did not stimulate cell proliferation, addressing the theoretical concern that a neurotrophin-elevating compound might have proliferative effects. (evidence tier: in-vitro; [PMID 30788746](https://pubmed.ncbi.nlm.nih.gov/30788746/))
- Rat pharmacokinetic studies show the parent ester hydrolyzes rapidly to the endogenous metabolite cycloprolylglycine, meaning systemic exposure is partly to an endogenous compound rather than a wholly xenobiotic molecule. (evidence tier: animal; [PMID 30378564](https://pubmed.ncbi.nlm.nih.gov/30378564/))
- In streptozotocin-diabetic rats given 0.5 mg/kg intraperitoneally for 14 days, Noopept was administered without reported toxicity while cognitive measures were assessed; animal tolerability at research doses does not establish human long-term safety. (evidence tier: animal; [PMID 31356906](https://pubmed.ncbi.nlm.nih.gov/31356906/))

## Dosing Information (Research Context)

The published human trial used 20 mg/day orally (two 10 mg doses) for 56 days in patients with mild cognitive disorders. Russian clinical use of Noopept follows the same oral tablet format. Animal studies have used 0.5-10 mg/kg, typically intraperitoneally. No injectable human protocol exists in the published literature.

| Route | Dose | Frequency | Notes |
| --- | --- | --- | --- |
| Oral (human trial) | 20 mg/day (2 x 10 mg) | Twice daily for 56 days | Comparative trial vs piracetam 1200 mg/day (PMID: 19234797) |
| Intraperitoneal (rat) | 0.5 mg/kg | Daily for 14 days | Streptozotocin-diabetic rat study (PMID: 31356906) |

## Researched Effects

- **Cognitive Restoration in Mild Cognitive Disorders** (evidence: moderate): In the pivotal human trial, 53 patients with mild cognitive disorders of vascular or post-traumatic origin were randomized to Noopept 20 mg/day or piracetam 1200 mg/day for 56 days. Noopept improved MMSE, BCRS, and CCSE scores from the second to third week, matched piracetam in overall nootropic extent at a 60-fold lower dose, and produced a more balanced activating-plus-anxiolytic profile with 1.8-fold fewer undesirable effects (PMID: 19234797). It is the only controlled human efficacy evidence for the compound and has never been replicated outside Russia.
- **Neurotrophic Upregulation (NGF and BDNF)** (evidence: moderate): In rat hippocampus, a single Noopept administration increased mRNA for both NGF and BDNF, while 28-day chronic treatment produced sustained neurotrophin elevation; cortical effects were smaller and directionally mixed (PMID: 19240853). This places omberacetam in the same neurotrophin-elevating class as Semax, though through a chemically distinct dipeptide scaffold and possibly through its cPG metabolite.
- **Neuroprotection: Anti-Excitotoxic and Anti-Apoptotic** (evidence: moderate): Noopept improved viability of hippocampal HT-22 neurons in a glutamate toxicity model (PMID: 27265136) and protected PC12 cells from A-beta(25-35) injury, preserving calcium homeostasis, lowering reactive oxygen species, and protecting mitochondrial function (PMID: 25096780). The protective pattern spans excitotoxic, oxidative, and amyloid insults in cell systems.
- **Tau and Amyloid Effects in Alzheimer Models** (evidence: preliminary): In the A-beta(25-35) PC12 model, omberacetam attenuated tau hyperphosphorylation and apoptosis (PMID: 25096780), and the developers reported cognition-restoring effects in several animal Alzheimer models. These are cellular and animal findings; no human Alzheimer trial exists, and the compound's clinical record is limited to mild cognitive disorders of vascular and traumatic origin.
- **Metabolic and Developmental Effects in Diabetic Models** (evidence: preliminary): In streptozotocin-diabetic prepubertal rats, 14 days of Noopept at 0.5 mg/kg intraperitoneally improved cognitive measures and was investigated for effects on the pubertal process, reflecting a research thread on diabetes-associated cognitive impairment (PMID: 31356906). This is single-study animal evidence in a specialized model.

## Research Applications

- Neuroscience
- Cognitive Research
- Alzheimer's Disease Models
- Neuroprotection Studies
- Diabetes-Related Cognitive Research

## Key Studies

### Comparative studies of Noopept and piracetam in the treatment of patients with mild cognitive disorders in organic brain diseases of vascular and traumatic origin

Neznamov GG, Teleshova ES — *Neuroscience and Behavioral Physiology* (2009) — [PMID 19234797](https://pubmed.ncbi.nlm.nih.gov/19234797/) | [doi:10.1007/s11055-009-9128-4](https://doi.org/10.1007/s11055-009-9128-4)

The pivotal human study: a 56-day randomized comparative trial in 53 patients (37 with vascular-origin emotionally labile disorder, 16 with post-concussional syndrome) comparing Noopept 20 mg/day with piracetam 1200 mg/day; 41 completed. Noopept improved MMSE, BCRS, and CCSE scores from weeks 2-3, showed equal nootropic extent to 60-fold higher-dosed piracetam, and produced a balanced nootropic, antiasthenic, and anxiolytic profile with 1.8-fold fewer undesirable effects. CGI ratings favored Noopept in both patient groups. It remains the only controlled human efficacy trial and has not been replicated outside Russia.

### Pharmacokinetics of noopept and its active metabolite cycloprolyl glycine in rats

Boyko SS, Zherdev VP, Shevchenko RV — *Biomeditsinskaya Khimiya* (2018) — [PMID 30378564](https://pubmed.ncbi.nlm.nih.gov/30378564/) | [doi:10.18097/PBMC20186405455](https://doi.org/10.18097/PBMC20186405455)

This pharmacokinetic study measured Noopept and its diketopiperazine metabolite cycloprolylglycine together in rats, documenting rapid hydrolysis of the parent ethyl ester and persistence of the bioactive metabolite. It formalized the prodrug model of omberacetam action: the administered ester is a delivery form, and part of the pharmacology belongs to cycloprolylglycine, an endogenous compound that also arises from IGF-1 metabolism.

### Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation

Ostrovskaya RU, Vakhitova YV, et al. — *Journal of Biomedical Science* (2014) — [PMID 25096780](https://pubmed.ncbi.nlm.nih.gov/25096780/) | [doi:10.1186/s12929-014-0074-2](https://doi.org/10.1186/s12929-014-0074-2)

In PC12 cells injured by A-beta(25-35), Noopept (10 micromolar, added 72 hours before the toxin) protected cell viability, calcium homeostasis, mitochondrial function, and neurite outgrowth, reduced reactive oxygen species, and attenuated tau hyperphosphorylation and apoptosis. It is the most-cited mechanistic paper behind anti-Alzheimer claims for omberacetam, and it is openly accessible, which aided independent scrutiny.

### Noopept stimulates the expression of NGF and BDNF in rat hippocampus

Ostrovskaya RU, Gudasheva TA, et al. — *Bulletin of Experimental Biology and Medicine* (2008) — [PMID 19240853](https://pubmed.ncbi.nlm.nih.gov/19240853/)

Northern blot analysis showed that a single Noopept administration increased NGF and BDNF mRNA in rat hippocampus, while 28-day chronic treatment maintained hippocampal neurotrophin elevation; cortical expression was unchanged or reduced after single dosing and only slightly increased chronically. The study anchors the neurotrophin mechanism of omberacetam and documents regional specificity of the effect.

### Dipeptide Piracetam Analogue Noopept Improves Viability of Hippocampal HT-22 Neurons in the Glutamate Toxicity Model

Antipova TA, Nikolaev SV, et al. — *Bulletin of Experimental Biology and Medicine* (2016) — [PMID 27265136](https://pubmed.ncbi.nlm.nih.gov/27265136/)

In immortalized hippocampal HT-22 neurons exposed to toxic glutamate concentrations, Noopept improved viability, demonstrating anti-excitotoxic protection in a standard in vitro model of excitotoxic neuronal death. Together with calcium-dynamics work in cultured hippocampal slices, it supports a membrane-stabilizing, anti-excitotoxic component of omberacetam action.

### Effects of noopept on cognitive functions and pubertal process in rats with diabetes

Gürbüz P, Düzova H, Yildiz A, et al. — *Life Sciences* (2019) — [PMID 31356906](https://pubmed.ncbi.nlm.nih.gov/31356906/)

In prepubertal Sprague-Dawley rats with streptozotocin-induced type 1 diabetes, 14 days of Noopept at 0.5 mg/kg intraperitoneally was studied across six arms (control, diabetes, noopept, insulin, and combinations) with cognitive and pubertal-development endpoints. The study, from a Turkish group independent of the Russian developers, explored diabetes-associated cognitive impairment and adds rare independent-group animal data to the omberacetam literature.

## Frequently Asked Questions

### Is omberacetam the same as Noopept?

Yes. Omberacetam is the international nonproprietary name; Noopept is the Russian trade name; GVS-111 is the development code. All three refer to N-phenylacetyl-L-prolylglycine ethyl ester (C17H22N2O4, CAS 157115-85-0), the dipeptide-derived nootropic developed at the Zakusov Institute of Pharmacology in Moscow.

### Is omberacetam a racetam?

Not structurally. Racetams share a 2-oxopyrrolidine ring; omberacetam is an N-acylprolyl dipeptide ethyl ester designed with peptide logic as a piracetam analog. It is grouped with racetams functionally because it targets the same nootropic niche and was benchmarked against piracetam, but its chemistry and its prodrug relationship to cycloprolylglycine are distinct.

### What human evidence exists for omberacetam?

One 56-day randomized comparative trial: 53 patients with mild cognitive disorders of vascular or post-traumatic origin received Noopept 20 mg/day or piracetam 1200 mg/day. Noopept matched piracetam's nootropic effect with 1.8-fold fewer undesirable effects and a more balanced anxiolytic profile (PMID: 19234797). The rest of the human literature consists of Russian clinical reports; there are no Western or placebo-controlled replication trials.

### How does omberacetam relate to cycloprolylglycine?

Omberacetam is an ethyl-ester prodrug that hydrolyzes rapidly in the body, releasing cycloprolylglycine (cPG), a cyclic dipeptide that is itself endogenous (it also forms during IGF-1 metabolism). Rat pharmacokinetics show the parent ester disappears quickly while cPG persists and reaches the brain (PMID: 30378564), so part of omberacetam's effect is likely cPG pharmacology, including modulation of IGF-1 bioavailability.

### Is omberacetam approved anywhere?

It is registered as a drug in Russia (sold as Noopept 10 mg tablets) and some neighboring states. It is not approved by the FDA or EMA. Outside those markets it is sold as a supplement or research compound, a regulatory gray zone with no quality-control guarantees.

## Related Peptides

- [Semax](https://peptpedia.org/peptide/semax)
- [Cyclic Glycine-Proline](https://peptpedia.org/peptide/cyclic-glycine-proline)
- [Dihexa](https://peptpedia.org/peptide/dihexa)
- [Cerebrolysin](https://peptpedia.org/peptide/cerebrolysin)

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