N-Phenylacetyl--prolylglycine ethyl ester is promoted as a

nootropic Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic supplements or drugs and other substances that are claimed to improve cognitive function or to promote re ...

and is a

prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...

cyclic glycine-proline Cyclic glycine-proline (cGP) is a small neuroactive peptide Neuropeptides are chemical messengers made up of small chains of amino acids that are synthesized and released by neurons. Neuropeptides typically bind to G protein-coupled receptors ...

. Other names include the brand name Noopept (russian: link=no, Ноопепт), developmental code GVS-111; proposed

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

omberacetam. Its synthesis was first reported in 1996. It is orally available, as of 2017 its metabolism and elimination half-life were not well understood, and cycloprolylglycine has not been measured in humans following administration. In cell culture, cycloprolylglycine increases

brain derived neurotrophic factor Brain-derived neurotrophic factor (BDNF), or abrineurin, is a protein found in the and the periphery. that, in humans, is encoded by the ''BDNF'' gene. BDNF is a member of the neurotrophin family of growth factors, which are related to the canon ...

(BDNF). It has been evaluated for

neuroprotective Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal los ...

effects in treating brain injuries and stroke.

Pharmacology

One oft-cited study (originally published in Russian) conducted on rats, suggests that Noopept works via the "antioxidant effect, the anti-inflammatory action, and the ability to inhibit the neurotoxicity of excess calcium and glutamate, and to improve the blood

rheology Rheology (; ) is the study of the flow of matter, primarily in a fluid ( liquid or gas) state, but also as "soft solids" or solids under conditions in which they respond with plastic flow rather than deforming elastically in response to an appl ...

". Some studies suggest that the pharmacological properties of Noopept are derived from its action as an activator of

Hypoxia-inducible factor Hypoxia-inducible factors (HIFs) are transcription factors that respond to decreases in available oxygen in the cellular environment, or hypoxia. They are only present in parahoxozoan animals. Discovery The HIF transcriptional complex wa ...

(HIF-1).

Most of the effects of Noopept could be explained by its action as an activator of HIF-1.

Dosage

Noopept is frequently dosed at 10-30mg per day. However, there is no solid evidence indicating that any dose of Noopept is optimal. Few human trials have ever been carried out on Noopept, and as one meta-analysis notes, animal studies have used doses ranging from 0.1mg/kg bodyweight to 10mg/kg bodyweight. Furthermore, no long-term studies have been done to evaluate the lasting effects of chronic use at any given dose; the longest human study lasted for 56 days. There is, therefore, no dose of Noopept which may be called "safe".

Legal status

*Hungary: As of 25 August 2020, Noopept is added to the controlled psychoactive substances list, prohibiting production, sale, import, storage and use. *Russia: Noopept in Russia is a drug of medicine and is available without a prescription. *United Kingdom: Contrary to popular belief, omberacetam is not illegal to produce, supply, or import under the Psychoactive Substance Act in the UK, which came into effect on May 26, 2016 because it does neither work as a CNS (central nervous system) depressant, nor as a CNS stimulant. However, sale and supply for human consumption are prohibited. *United States: The

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

has issued import alerts for imports of omberacetam, considering it an analog of

piracetam Piracetam is a drug marketed as a treatment for myoclonus. It is also used as a cognitive enhancer to improve memory, attention, and learning. Evidence to support its use is unclear, with some studies showing modest benefits in specific populat ...

. FDA considers such racetam-family substances Active Pharmaceutical Ingredients (APIs) that require new drug applications and adequate labelling before being imported. Similarly, warnings have been issued for claims of medical and pharmacological effects. Despite these FDA enforcement actions, omberacetam is sold in over-the-counter supplements in this US with some products formulated with dosages greater than pharmaceutical levels.

References

{{DEFAULTSORT:Phenylacetyl-L-prolylglycine ethyl ester, N- Racetams Pyrrolidines Ethyl esters Russian drugs

Pharmacology

Dosage

Legal status

See also

References