Omberacetam (Noopept)
A synthetic proline-containing dipeptide nootropic (GVS-111), marketed as Noopept, reported to enhance memory and provide neuroprotection at doses far below classical racetams.
Overview
Omberacetam is the scientific/INN-style name for the compound sold and widely discussed as Noopept (development code GVS-111). Chemically it is N-phenylacetyl-L-prolylglycine ethyl ester, a proline-containing dipeptide synthesised at the Institute of Pharmacology of the Russian Academy of Medical Sciences. It was engineered by reproducing the structural features of the classical nootropic piracetam within a dipeptide, yielding a compound active at 10-30 mg/day versus piracetam's gram-scale dosing (Ostrovskaya et al., 2002).
Pharmacologically, noopept acts as a prodrug: it is hydrolysed to N-phenylacetyl-L-prolylglycine and then cyclised to cycloprolylglycine, an endogenous neuropeptide, with release of phenylacetic acid. Reported effects span memory enhancement across acquisition, consolidation and retrieval, a selective anxiolytic action, and neuroprotection in models of ischaemia, oxidative stress and amyloid toxicity.
Human evidence is modest and concentrated in Russian clinical studies. Clinical studies in patients with mild cognitive impairment of post-traumatic and vascular origin reported symptomatic improvement with noopept 20 mg/day, accompanied by favourable EEG changes (Bochkarev et al., 2008; Amelin et al., 2011). Much of the mechanistic and neuroprotective data remains preclinical. Note: a separate noopept entry exists in this wiki; this page covers the same molecule under its scientific name -- omberacetam and Noopept are the same compound.
Mechanism of Action
After oral administration noopept is hydrolysed to the free acid and cyclised to cycloprolylglycine (cPG), a naturally occurring brain dipeptide. A central proposed pathway is enhanced hippocampal expression of nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) (Ostrovskaya et al., 2008), promoting synaptic plasticity. Additional actions include potentiation of acetylcholine currents at very low concentrations, weak AMPA-receptor interaction, stabilisation of HIF-1, and reduction of oxidative and glutamate-excitotoxic damage, giving both cognitive-enhancing and neuroprotective profiles in preclinical models.
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Safety Profile
Side effects are generally mild and may include headaches, insomnia, irritability, and gastrointestinal discomfort. It is contraindicated in individuals with severe hepatic or renal impairment and during pregnancy or lactation. Omberacetam may enhance the effects of other nootropics and psychostimulants, so careful dose management is recommended.
Pharmacokinetic Profile
- Tmax
- Mechanism of Action
References (4)
- [1]Ostrovskaya RU, Gudasheva TA, Voronina TA, Seredenin SB The original novel nootropic and neuroprotective agent noopept Eksperimental'naia i Klinicheskaia Farmakologiia (2002)
→ Foundational review describing GVS-111/noopept as a proline-containing dipeptide designed from the piracetam pharmacophore, retaining nootropic activity orally with a wide therapeutic margin.
- [2]Bochkarev VK, Teleshova ES, Siuniakov SA, Davydova DV, Neznamov GG Clinical and electroencephalographic characteristic of noopept in patients with mild cognitive impairment of posttraumatic and vascular origin Zhurnal Nevrologii i Psikhiatrii im. S.S. Korsakova (2008)
→ In patients with mild cognitive impairment of post-traumatic and vascular origin, noopept produced clinical improvement accompanied by EEG changes (increased alpha/beta and reduced delta power).
- [3]Amelin AV, Iliukhina AIu, Shmonin AA Noopept in the treatment of mild cognitive impairment in patients with stroke Zhurnal Nevrologii i Psikhiatrii im. S.S. Korsakova (2011)
→ Noopept 20 mg/day over an extended course produced significant cognitive improvement in stroke patients with mild cognitive impairment.
- [4]Ostrovskaya RU, et al. Noopept stimulates the expression of NGF and BDNF in rat hippocampus Bulletin of Experimental Biology and Medicine (2008)
→ Noopept increases hippocampal expression of the neurotrophins NGF and BDNF, a proposed basis for its cognitive and neuroprotective effects.
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