Noopept
Noopept (omberacetam, GVS-111) is a peptide-derived nootropic first synthesized in 1996 and developed as a prescription medication in Russia.12 It has become one of the most widely used cognitive enhancers,2 often taken in combination 'stacks' with other nootropics. Noopept is commonly attributed with temporarily enhancing concentration, focus, and memory recall.3 Daily use may lead to dependence, with withdrawal reportedly causing negative cognitive effects.
Contents
Dosage & Duration
Dosage
Repeated redosing across a single day, reaching a cumulative intake of 50 mg over eight hours, was described as excessive and not recommended, with a mild transient headache reported.
Duration
Subjective Effects
Effects vary widely by individual, dose, and context.
Physical
Cognitive
Visual
Enhancements
Reagent Testing
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Pharmacology
Pharmacodynamics
Noopept (omberacetam) functions as a prodrug of the endogenous dipeptide cycloprolylglycine.4 The active metabolite modulates AMPA receptors and exerts neuroprotective effects that appear dependent upon both AMPA receptor and TrkB receptor activation.5 In cell culture studies, cycloprolylglycine has been shown to increase brain-derived neurotrophic factor (BDNF).6 Additional research suggests that noopept may act as an activator of hypoxia-inducible factor (HIF-1), which could contribute to its pharmacological profile.7 Rat studies have attributed its effects to antioxidant activity, anti-inflammatory action, and the ability to inhibit neurotoxicity from excess calcium and glutamate, as well as improvements in blood rheology.3
Pharmacokinetics
Noopept is orally bioavailable and acts as a prodrug, being metabolized to the active dipeptide cycloprolylglycine.4 As of 2017, its metabolism and elimination half-life in humans were not well characterized.8
Tolerance
Harm Potential
Addiction & Dependence
Psychological
LowDaily use is reported to create dependency, suggesting some potential for psychological habituation with regular administration.
Physical
LowWithdrawal from daily use reportedly causes negative cognitive effects and impaired ability, indicating some degree of physical adaptation with chronic use.
History & Culture
Noopept was developed by a Russian pharmaceutical company during the 1970s and remains a prescription medication in Russia.3 Its synthesis was first formally reported in scientific literature in 1996.9 The compound has been evaluated for potential neuroprotective…
Legality
By Country
References
Source Pages
Citations
- (n.d.). Omberacetam. Inxight. https://drugs.ncats.io/drug/4QBJ98683M1
- (June 2021). Five Unapproved Drugs Found in Cognitive Enhancement Supplements. Neurology. Clinical Practice, 11(3), e303–e307. https://doi.org/10.1212/cpj.000000000000096012
- (2002). [The original novel nootropic and neuroprotective agent noopept]. Eksperimental'naia i Klinicheskaia Farmakologiia, 65(5), 66–72. https://pubmed.ncbi.nlm.nih.gov/12596521/1234
- (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. https://doi.org/10.1007/bf0318981412
- (December 2022). Neuroprotective Effect of the Neuropeptide Cycloprolylglycine Depends on AMPA- and TrkB-Receptor Activation. Doklady. Biochemistry and Biophysics, 507(1), 264–267. https://doi.org/10.1134/s16076729220600471
- (July 2016). Neuropeptide cycloprolylglycine increases the levels of brain-derived neurotrophic factor in neuronal cells. Doklady. Biochemistry and Biophysics, 469(1), 273–276. https://doi.org/10.1134/s16076729160401041
- (September 2020). Cognitive Enhancer Noopept Activates Transcription Factor HIF-1. Doklady. Biochemistry and Biophysics, 494(1), 256–260. https://doi.org/10.1134/s16076729200501291
- (2004). [Interspecies differences of noopept pharmacokinetics]. Eksperimental'naia i Klinicheskaia Farmakologiia. https://pubmed.ncbi.nlm.nih.gov/15079908/1
- Jia X, Gharibyan AL, Ohman A, Liu Y, Olofsson A, & Bhanu PS. (2015). Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation. Journal of Biomedical Science. https://doi.org/10.1186/s12929-015-0130-012
Further Reading
Examine.com: N-Phenylacetyl-L-prolylglycine ethyl ester
Gudasheva et al. 2002 - The original novel nootropic and neuroprotective agent noopept
IJEST 2021 - Finding the optimal dosage for nootropic agent Noopept
Neznamov & Teleshova 2009 - Comparative studies of Noopept and piracetam- Ostrovskaya et al. 2018 - Pharmacokinetics of noopept and its active metabolite cycloprolyl glycine in rats
- PubChem: 1-(2-Phenylacetyl)-L-prolylglycine ethyl ester
Automated synthesisInformation aggregated and synthesized using an autonomous workflow built by Josie Kins.
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