Educational reference, not medical advice. This page summarizes information from published research and regulatory filings for educational purposes. It is not a recommendation to use any compound and should not replace guidance from a licensed healthcare provider. Most peptides discussed here are not approved for the uses described.
What it is
Noopept is the international non-proprietary name for omberacetam, designated GVS-111 in the original Russian medicinal-chemistry literature. Chemically it is N-phenylacetyl-L-prolylglycine ethyl ester — a proline-glycine dipeptide with an N-terminal phenylacetyl group and a C-terminal ethyl ester. It is small (about 318 Da) and orally bioavailable.
Although the active molecule is a dipeptide, Noopept is more accurately described as a peptidomimetic. It was designed as a small-molecule analog of piracetam (the prototypical "racetam" nootropic), and its in vivo activity is attributed in part to a metabolite — cycloprolylglycine — which the Gudasheva group identified as the principal brain metabolite and as a structural analog of an endogenous neuropeptide of the same name.
History
Noopept was synthesized in the mid-1990s at the Zakusov Research Institute of Pharmacology by Tatiana Gudasheva and colleagues, building on a structural-activity program aimed at miniaturizing piracetam-like nootropics into dipeptide-sized molecules with improved oral bioavailability. The 1996 medicinal-chemistry paper described the antiamnesic activity of N-acylprolyl dipeptides, and the 1997 pharmacokinetic paper identified cycloprolylglycine as the dominant brain metabolite.
The compound was approved by the Russian regulator in 2007 for cognitive impairment associated with cerebrovascular disease and post-traumatic encephalopathy, dispensed as 10 mg oral tablets under the trade name Noopept (omberacetam).
Outside Russia and a small number of CIS countries, Noopept has not been submitted as a drug application. It is widely sold over the counter in many Western jurisdictions as a "nootropic" supplement, on the grounds that the FDA has not classified it as a drug and has not taken enforcement action against the substance per se.
Regulatory status
Noopept is approved in Russia and several CIS countries for cognitive disorders. It is not approved by the FDA, EMA, MHRA, Health Canada, or the TGA. The FDA has not scheduled Noopept and does not regulate it as a drug; in 2019 the FDA issued a warning letter to a U.S. seller marketing Noopept and other unapproved substances with drug-like claims, but the substance itself remains uncontrolled. In the UK, Noopept fell under the Psychoactive Substances Act 2016, restricting commercial sale.
Internationally, Noopept's status is a patchwork: legal as a supplement in some countries, sold by research-chemical suppliers in others, and not legally marketable as either a drug or supplement in still others. Buyers should check local regulations.
How researchers describe its action
The published mechanism account is multi-faceted and not centered on a single classical receptor:
- Cycloprolylglycine generation. Noopept is rapidly metabolized in rat brain to cycloprolylglycine, a structural analog of an endogenous neuropeptide thought to have neuroprotective effects of its own.
- NGF and BDNF upregulation. Ostrovskaya and colleagues reported that Noopept increases nerve growth factor and brain-derived neurotrophic factor expression in the rat hippocampus.
- Antioxidant and anti-apoptotic effects. Pelsman and colleagues described protection of cultured cortical neurons (including neurons from individuals with Down's syndrome) against oxidative damage and apoptosis.
- AMPA and NMDA receptor modulation. Several Russian-language studies report modulation of glutamatergic transmission, which is part of the proposed link to the cognitive effects.
These mechanisms are characterized primarily in rodent and cell-culture studies. Mechanistic data in healthy human tissue is limited.
Half-life and dosing intervals
Noopept has a very short plasma half-life — published estimates fall in the range of 16 to 23 minutes after oral administration. The parent compound is rapidly hydrolyzed to cycloprolylglycine, which has a longer effective half-life in brain and is thought to account for the prolonged behavioral effects observed in rodent studies despite the rapid clearance of the parent dipeptide.
The Russian label for Noopept specifies 10 mg orally twice daily, escalating to 10 mg three times daily after 2 weeks if needed, for a typical course of 1.5 to 3 months. These are the doses studied in the published clinical literature in Russia.
Reconstitution example
Branded Noopept is supplied as 10 mg oral tablets and does not require reconstitution. Research-grade Noopept is sold as a bulk powder, typically in 10 mg or 20 mg quantities suitable for oral capsule preparation. Injection is not the labeled route, and the molecule is designed around oral bioavailability.
If a research protocol requires solution dosing for cell culture work, Noopept is soluble in DMSO or ethanol; supplier-specific vehicle guidance applies.
What to know
- Oral, not injectable. Noopept was designed as an oral peptidomimetic; the approved formulation is a tablet.
- Short parent half-life, longer metabolite effect. The clinical effect is attributed partly to the cycloprolylglycine metabolite, which outlasts the parent dipeptide.
- Regulatory patchwork. Noopept is approved in Russia, sold OTC as a supplement in some Western countries, and restricted in others. Local regulations vary substantially.
- Limited Western clinical data. Almost all efficacy evidence comes from Russian-language journals and rodent studies. There has been no Phase III trial registered with the FDA or EMA.
- Reported adverse effects in the Russian labeling are uncommon and include irritability, sleep disturbance, and increases in blood pressure in hypertensive patients. Long-term safety in non-Russian populations has not been characterized.
- Not strictly a peptide. Noopept is a proline-glycine dipeptide ester — accurately described as a peptidomimetic rather than a classical peptide drug.
Sources
- 1.Gudasheva TA, Voronina TA, Ostrovskaya RU, Rozantsev GG, Vasilevich NI, Trofimov SS, Kravchenko EV, Skoldinov AP, Seredenin SB (1996). Synthesis and antiamnesic activity of a series of N-acylprolyl-containing dipeptides. European Journal of Medicinal Chemistry.
- 2.Gudasheva TA, Boyko SS, Akparov VKh, Ostrovskaya RU, Skoldinov SP, Rozantsev GG, Voronina TA, Asmakova LS, Seredenin SB (1997). The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine. European Journal of Drug Metabolism and Pharmacokinetics.
- 3.Pelsman A, Hoyo-Vadillo C, Gudasheva TA, Seredenin SB, Ostrovskaya RU, Busciglio J (2003). GVS-111 prevents oxidative damage and apoptosis in normal and Down's syndrome human cortical neurons. International Journal of Developmental Neuroscience.
- 4.Ostrovskaya RU, Gudasheva TA, Zaplina AP, Vahitova JV, Salimgareeva MH, Jamidanov RS, Seredenin SB (2007). Noopept stimulates the expression of NGF and BDNF in rat hippocampus. Bulletin of Experimental Biology and Medicine.