Noopept

Noopept (GVS-111, omberacetam) is a small synthetic molecule (MW 318.37) — N-phenylacetyl-L-prolylglycine ethyl ester — classified as a dipeptide analogue or cyclic-prolylglycine (CPG) prodrug. It was developed at the Zakusov Institute of Pharmacology in Moscow and registered as an over-the-counter nootropic in Russia in the early 2000s. It is not a true peptide by strict biochemical definition. Noopept has not been evaluated by the FDA, EMA, or MHRA. The Western-indexed human evidence base is extremely limited: a PubMed search for "noopept" returns fewer than 20 indexed publications, almost entirely preclinical or Russian-language studies. No completed or registered interventional trials appear on ClinicalTrials.gov.

Noopept is a prodrug that is hydrolysed in vivo to cycloprolylglycine (CPG) and phenylacetic acid. CPG acts as a positive allosteric modulator of AMPA-type glutamate receptors. Additional reported effects include: increase in BDNF and NGF expression (animal studies), modulation of acetylcholinergic transmission, antioxidant activity, and anti-amnesic effects in rodent models. The AMPA modulation is considered the primary cognitive mechanism, analogous to drugs in the racetam family, but the exact receptor pharmacology is less well characterised than for piracetam or aniracetam. The dipeptide character means it is sometimes — misleadingly — grouped with peptide therapeutics, but its pharmacokinetics, regulatory pathway, and safety profile follow small-molecule drug standards.

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

Russian OTC regimen: 10 mg orally, 2–3 times daily (20–30 mg/day). Typical course 1.5–3 months.

Studied regimens (not recommendations)

Clinical studies used 5–20 mg/day orally for 28–90 days. No parenteral studies in humans.

No established or recommended human dose.

What is not established

• Efficacy for any specific disease indication (AD, TBI, stroke)

• Long-term safety beyond 3 months

• Comparative effectiveness vs other nootropics

• Dose-response relationship

• Safety and efficacy of chronic use

Established label risks

Registered OTC in Russia; no boxed warnings. Reported mild side effects: headache, dizziness, irritability, sleep disturbance, gastrointestinal discomfort.

Human-study signals

No serious adverse events reported in published Russian studies. Low total published human n limits signal detection.

Unknowns and product-quality risks

• No Western regulatory safety review

• GHS classification: acute oral toxicity Category 4 (harmful if swallowed) in some MSDS listings

• No long-term human safety data

• No drug interaction studies with antidepressants, antipsychotics, or stimulants

• Research chemical products lack regulatory quality assurance

• Drug is often sold as a "peptide" despite not being one, creating confusion about identity and purity standards

• No systematic human data on withdrawal, tolerance, or dependence

• May potentiate effects of caffeine or stimulants (anecdotal)

• No dedicated studies in hepatic or renal impairment

• Pregnancy and lactation: no adequate data

• No paediatric safety data

• Interaction with warfarin, anticonvulsants, or antipsychotics not studied

• WADA: not identified by exact name in the 2026 List. This page records a current Russian governmental approval, so S0 cannot be inferred merely from lack of FDA/EMA approval. Athletes should obtain a current case-specific classification.

• US DEA: not scheduled

• CAS 157115-85-0; registered OTC in Russia, imported as dietary supplement in some non-EU markets

• Not on FDA 503A bulks list

• Not classified as a peptide by the European Pharmacopoeia

• No FDA- or EMA-standard RCT demonstrating efficacy in any condition

• Western-indexed English-language human evidence is very limited

• No long-term safety data meeting modern regulatory standards

• Mechanism at AMPA receptors is inferred from preclinical CPG studies; direct human receptor pharmacology not confirmed

• Dose range, optimal regimen, and PK/PD relationship for clinical use not validated

• Most original data in Russian with limited English methodological reporting

• Boundary-case classification (dipeptide analogue) creates confusion in peptide-vs-small-molecule regulatory frameworks

• Databases and registries: PubMed, PubChem, CAS, ClinicalTrials.gov, Russian State Register of Medicines

• Search terms: Noopept, GVS-111, omberacetam, 157115-85-0, neznamov, ostrovskaya

• Last searched: 2026-08-06

• Inclusion emphasis: human clinical data, regulatory records, identity databases, safety information

• PubMed search 2026-08-06: fewer than 20 total results; no registered interventional trials on ClinicalTrials.gov

1. PubChem CID 180496. https://pubchem.ncbi.nlm.nih.gov/compound/180496

2. Russian State Register of Medicines: Noopept (omberacetam) registration entry. https://grls.rosminzdrav.ru/

3. Ostrovskaya RU et al. (2001) Eksp Klin Farmakol. Russian preclinical data.

4. Neznamov GG et al. (2002) Zh Nevrol Psikhiatr Im S S Korsakova. Clinical pilot.

5. Firstova YY et al. (2011) Effects of nootropic drugs on glutamate receptors in rat brain. Eksp Klin Farmakol. PMID 21476267. https://pubmed.ncbi.nlm.nih.gov/21476267/

6. Gudasheva TA et al. (2001) Vopr Biol Med Farm Khim. Original dipeptide prodrug design.

7. ClinicalTrials.gov search for Noopept/GVS-111. https://clinicaltrials.gov/search?intr=Noopept (zero interventional trials as of 2026-08-06)

8. UNII PPV1N20H5B. https://precision.fda.gov/uniisearch/srs/unii/PPV1N20H5B

9. GHS Classification records — Noopept MSDS (various suppliers)