N-Phenylacetyl-l-prolylglycine ethyl ester is promoted as anootropic and is aprodrug ofcyclic glycine-proline.[a][2] Other names include the brand nameNoopept (Russian:Ноопепт), developmental codeGVS-111, and proposedINNomberacetam.[2][3][4]
Its synthesis was first reported in 1996.[2] It is orally available. As of 2017, its metabolism and elimination half-life in humans were not well understood.[2]
It has been evaluated forneuroprotective effects in treating brain injuries and stroke.[5]
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 theneurotoxicity of excess calcium and glutamate, and to improve the bloodrheology".[5] Studies in rats suggest, Noopept is a prodrug of the endogenous dipeptidecycloprolylglycine.[6]Cycloprolylglycine is a modulator ofAMPA receptors and exerts neuroprotective effects dependent uponAMPA- andTrkB-Receptor activation.[7] In cell culture, cycloprolylglycine increasesbrain derived neurotrophic factor (BDNF).[8]
Some studies suggest that the pharmacological properties of Noopept are derived from its action as an activator ofHypoxia-inducible factor (HIF-1).[9][10]
Noopept is frequently dosed at 10–30 mg 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 0.1 mg/kg bodyweight to 10 mg/kg bodyweight.[unreliable medical source?][11] 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.[12]
Hungary: As of 25 August 2020, Noopept is added to the controlled psychoactive substances list, prohibiting production, sale, import, storage and use.[13]
Russia: Noopept in Russia is a drug of medicine and is available without a prescription.[14]
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 neither works as a CNS (central nervous system) depressant, nor as a CNS stimulant.[15] However, sale and supply for human consumption are prohibited.
United States: TheFood and Drug Administration has issued import alerts for imports of omberacetam, considering it an analog ofpiracetam.[16] FDA considers such racetam-family substances Active Pharmaceutical Ingredients (APIs) that require new drug applications and adequate labelling before being imported.[17] Similarly, warnings have been issued for claims of medical and pharmacological effects.[18] Despite these FDA enforcement actions, omberacetam is sold in over-the-counter supplements in the US, with some products formulated with dosages greater than pharmaceutical levels.[19]
^Referring to the cyclic dipeptide better known as cyclo(prolylglycyl), i.e. (S)-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione.[1] Not to be confused with acyclopropanyl moiety.
^abOstrovskaia RU, Gudasheva TA, Voronina TA, Seredenin SB (2002). "[The original novel nootropic and neuroprotective agent noopept]" [The original novel nootropic and neuroprotective agent noopept].Eksperimental'naia i Klinicheskaia Farmakologiia [Experimental and Clinical Pharmacology] (in Russian).65 (5):66–72.PMID12596521.
^Gudasheva TA, Boyko SS, Ostrovskaya RU, Voronina TA, Akparov VK, Trofimov SS, et al. (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.22 (3):245–252.doi:10.1007/BF03189814.PMID9358206.
^Gudasheva TA, Koliasnikova KN, Alyaeva AG, Nikolaev SV, Antipova TA, Seredenin SB (December 2022). "Neuroprotective Effect of the Neuropeptide Cycloprolylglycine Depends on AMPA- and TrkB-Receptor Activation".Doklady. Biochemistry and Biophysics.507 (1):264–267.doi:10.1134/S1607672922060047.PMID36786983.
^Gudasheva TA, Koliasnikova KN, Antipova TA, Seredenin SB (July 2016). "Neuropeptide cycloprolylglycine increases the levels of brain-derived neurotrophic factor in neuronal cells".Doklady. Biochemistry and Biophysics.469 (1):273–276.doi:10.1134/S1607672916040104.PMID27599510.S2CID254426990.
^Neznamov GG, Teleshova ES (March 2009). "Comparative studies of Noopept and piracetam in the treatment of patients with mild cognitive disorders in organic brain diseases of vascular and traumatic origin".Neuroscience and Behavioral Physiology.39 (3):311–321.doi:10.1007/s11055-009-9128-4.PMID19234797.S2CID3348153.
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