Neuroscience Research Compound · For laboratory research use only

Omberacetam (Noopept)

Also known as GVS-111, Noopept

Formula
C17H22N2O4
CAS
157115-85-0

Overview

Omberacetam (N-phenylacetyl-L-prolylglycine ethyl ester, also known as Noopept or GVS-111) is a synthetic proline-containing dipeptide designed as an analogue of piracetam1,3. Its solid-state and physicochemical properties, including crystal structure and polymorphism, were characterised in detail in 20256.

Published research is predominantly preclinical. Studies have examined its metabolism in rat brain, neurotrophin expression in rat hippocampus, an amyloid-beta toxicity model in PC12 cells, electrophysiology in rat hippocampal slices and transcription factor activity in neuroblastoma cells1,2,3,4,5.

Mechanism of action

As described in the research literature

As described in the research literature, omberacetam itself was not detected in rat brain at early time points, whereas levels of cyclo-L-prolylglycine rose; its formation from omberacetam in the presence of plasma and brain enzymes was shown in vitro. The authors proposed that omberacetam acts as a prodrug of this endogenous cyclic dipeptide1.

Other studies have examined several candidate pathways. Increased hippocampal NGF and BDNF mRNA expression was reported in rats by Northern blot2. In rat hippocampal slices, increased firing of GABAergic interneurons in the CA1 stratum radiatum was abolished by alpha7 nicotinic acetylcholine receptor antagonists4. In SH-SY5Y cells, omberacetam increased the DNA-binding activity of the transcription factor HIF-1, with evidence pointing to inhibition of HIF prolyl hydroxylase5.

Research areas

What published studies have examined

Metabolism and the cyclo-prolylglycine metabolite

Rat brain samples were analysed by HPLC, gas chromatography and GC-MS for possible metabolites, and the formation of cyclo-prolylglycine was examined in vitro with plasma and brain enzymes1.

Sources [1]

Neurotrophin expression

NGF and BDNF mRNA levels in rat cerebral cortex and hippocampus were measured in short-term and 28-day rat studies2.

Sources [2]

Amyloid-beta cellular model

PC12 cells exposed to amyloid-beta 25-35 were used to examine cell viability, apoptosis, intracellular calcium, reactive oxygen species, mitochondrial membrane potential, tau phosphorylation at Ser396 and neurite outgrowth, with and without omberacetam pretreatment3.

Sources [3]

Hippocampal electrophysiology and HIF-1 signalling

Whole-cell patch-clamp recordings from rat hippocampal slices examined the role of alpha7 nicotinic receptors on interneurons in the response to omberacetam4. Separate in vitro work in SH-SY5Y cells examined HIF-1 DNA-binding activity, HIF1-alpha stabilisation and related gene expression changes5.

Sources [4] [5]

Specifications

Molecular formula
C17H22N2O4
Molecular weight
318.4 g/mol
CAS number
157115-85-0
Form
Measured units (packs of 30 or 60), or a pre-dissolved liquid at 30 mg/mL in a 30 mL bottle
Storage
Units: store in a cool, dry place in the sealed pouch, away from direct light. Liquid: keep the bottle tightly closed, stored cool and away from direct light.
Solubility and reconstitution
Supplied ready to use: units are pre-measured and the liquid is pre-dissolved, so no reconstitution is required.

References

  1. 1

    The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine.

    Gudasheva TA, Boyko SS, Ostrovskaya RU, et al. European Journal of Drug Metabolism and Pharmacokinetics, 1997.

  2. 2

    Noopept stimulates the expression of NGF and BDNF in rat hippocampus.

    Ostrovskaya RU, Gudasheva TA, Zaplina AP, et al. Bulletin of Experimental Biology and Medicine, 2008.

  3. 3

    Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation.

    Ostrovskaya RU, Vakhitova YV, Kuzmina USh, et al. Journal of Biomedical Science, 2014.

  4. 4

    Effect of nootropic dipeptide noopept on CA1 pyramidal neurons involves α7AChRs on interneurons in hippocampal slices from rat.

    Kondratenko RV, Povarov IS, Kolbaev SN, et al. Neuroscience Letters, 2022.

  5. 5

    Cognitive Enhancer Noopept Activates Transcription Factor HIF-1.

    Zainullina LF, Ivanova TV, Sadovnikov SV, et al. Doklady Biochemistry and Biophysics, 2020.

  6. 6

    Physicochemical and structural analysis of N-phenylacetyl-L-prolylglycine ethyl ester (Noopept) - An active pharmaceutical ingredient with nootropic activity.

    Araj SK, Szeleszczuk Ł, Gubica T, et al. Journal of Pharmaceutical and Biomedical Analysis, 2025.

This page is provided for research and educational reference only. It does not constitute medical advice, dosing guidance, or a recommendation for use. All compounds are strictly for laboratory and in-vitro research purposes.

RUO. For research purposes only. Not for human consumption. Not for veterinary use.

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