Overview

Noopept (GVS-111) is a synthetic dipeptide-derived nootropic compound that acts as a prodrug for cycloprolylglycine (CPG), an endogenous neuropeptide that modulates AMPA receptor function and has neurotrophic activity. Developed in Russia in the 1990s, Noopept is estimated to be approximately 1000 times more potent by weight than piracetam (though this comparison is mechanistically distinct). It is available as a prescription medication in Russia for cognitive disorders and widely used globally as a cognitive enhancer.

Mechanism of Action

After oral absorption, Noopept is cleaved to release cycloprolylglycine (CPG), which acts as an AMPA receptor modulator (ampakine activity) that enhances glutamatergic neurotransmission and promotes LTP (long-term potentiation). Additionally, Noopept stimulates BDNF and NGF expression in the hippocampus and cortex via TrkB receptor pathway sensitization. It also demonstrates anxiolytic activity through GABA-A receptor modulation and reduces oxidative stress in neuronal tissues. Alpha wave EEG activity is increased, associated with relaxed attention.

Potential Benefits

  • Cognitive enhancement including memory consolidation and recall
  • BDNF and NGF elevation in hippocampus
  • Anxiolytic effects without sedation
  • Neuroprotection in ischemia and excitotoxicity models
  • Enhanced verbal memory and learning in clinical studies
  • High oral bioavailability with rapid CNS penetration

Research Dosage Notes

The following reflects doses used in published research studies. This is not medical advice.

Typical cognitive enhancement dose: 10–30 mg once or twice daily, sublingual or oral. Russian clinical dose: 5–10 mg twice daily. Cycle with breaks to prevent tolerance.

Amino Acid Sequence

N-phenylacetyl-L-prolyl-glycine ethyl ester (prodrug for CPG dipeptide)

Side Effects & Safety

  • Generally well-tolerated at recommended doses
  • Headache (may indicate choline deficiency)
  • Irritability or anxiety at high doses
  • Mild nausea

Synergistic Compounds

The following compounds have been studied alongside Noopept for potential complementary or synergistic effects:

SemaxSelankRacetamsAlpha-GPC

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References & Further Reading

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