Noopept
Also known as: GVS-111, N-phenylacetyl-L-prolylglycine ethyl ester, omberacetam, N-Phenylacetyl-L-Prolylglycine Ethyl Ester
Noopept is a prescription drug in Russia. Research use only in many jurisdictions. Check local regulations.
Overview
Dipeptide-derived nootropic developed in Russia and used across Eastern Europe as a cognitive enhancer and neuroprotective agent. Structurally related to piracetam but estimated to be approximately 1000× more potent by weight. Rapidly crosses the blood-brain barrier and is hydrolyzed to the endogenous neuropeptide cycloprolylglycine, which is proposed as its primary active metabolite.
Research Summary
Noopept (GVS-111) enhances AMPA-receptor function and increases expression of BDNF and NGF in the hippocampus and basal forebrain. Its active metabolite cycloprolylglycine acts as an endogenous neuropeptide with anxiolytic and cognition-enhancing properties. Russian clinical trials demonstrate cognitive improvement in subjects with cognitive impairment, with a better tolerability profile than piracetam at equipotent doses.
Dosing Range
low
5mg
moderate
10mg
high
20mg
Units: mg · Frequency: 1–3x daily oral or sublingual (8–12 week cycles)
Dosing ranges are aggregated from preclinical research and community protocols. Not medical dosing guidance.
Administration Routes
Reconstitution Notes
Oral: no reconstitution needed. Sublingual: dissolve powder directly under tongue. Intranasal: dissolve in sterile saline at 10mg/mL for nasal administration. Water-soluble at low concentrations.Step-by-step reconstitution guide →
Supplies you'll need
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Reported Side Effects
- Headache (especially without choline supplementation)
- Irritability
- Brain fog at high doses
- Insomnia (if taken too late in day)
- Initial increased anxiety in some users
- Mild nausea
Research Papers
2 peer-reviewed sourcesCommunity Experiences
Aggregated from public forums. Anecdotal — not clinical evidence.
Community reports on noopept dosing, choline pairing requirements, and comparison to racetams.
View original threadResearcher discussion on noopept's peptide-derived mechanism and sublingual vs. oral bioavailability.
View original threadOverview
Noopept (GVS-111, now also known as omberacetam) was developed at the Zakusov Institute of Pharmacology in Moscow as an improved analogue of piracetam. The goal was to create a compound with piracetam-like cognitive benefits but active at far lower doses — reducing side effects while maintaining or improving efficacy.
The result was a dipeptide ester structure (N-phenylacetyl-L-prolylglycine ethyl ester) that:
- Is absorbed orally and sublingually
- Crosses the blood-brain barrier rapidly
- Is hydrolyzed to cycloprolylglycine (CPG) — an endogenous dipeptide found naturally in the human brain
- CPG is proposed as the true active metabolite responsible for cognitive effects
Noopept is registered as a pharmaceutical drug in Russia (Noopept® tablets, 10mg) and is one of the most widely self-experimented nootropics in the international biohacking community.
Mechanism
AMPA Receptor Potentiation
At the synapse level, noopept and/or cycloprolylglycine enhances AMPA-type glutamate receptor responsiveness:
- Increases receptor conductance (current per channel opening)
- Enhances long-term potentiation (LTP) — the synaptic strengthening mechanism underlying memory formation
- Improves signal-to-noise ratio in hippocampal and cortical circuits
This AMPA potentiation is distinct from piracetam's mechanism (thought to involve membrane fluidity) and explains noopept's much greater potency by weight.
BDNF and NGF Upregulation
Noopept administration increases mRNA expression of:
- BDNF in hippocampus: Supports synaptic plasticity, neuron survival, and memory consolidation
- NGF in basal forebrain: Supports cholinergic neuron maintenance (the system most depleted in Alzheimer's disease)
These effects are particularly relevant for neuroprotective applications and have generated interest in noopept as a prophylactic cognitive supplement.
Cycloprolylglycine (CPG) as Active Metabolite
CPG is an endogenous mammalian neuropeptide at nanomolar brain concentrations. Research shows:
- Anxiolytic properties: CPG modulates GABA-A receptor complex
- Nootropic effects: Independent of direct AMPA action
- Anti-amnestic activity: Reduces forgetting in scopolamine amnesia models
The prodrug model — noopept → CPG — parallels how many pharmaceutical peptides require metabolic conversion to their active form.
Acetylcholine System Interaction
Noopept preserves cholinergic neurotransmission through:
- NGF support for basal forebrain cholinergic neurons
- Indirect enhancement of acetylcholine release via improved neural signaling efficiency
This explains why choline supplementation is typically recommended alongside noopept — supporting the cholinergic system reduces headache and brain fog side effects associated with increased demand on the system.
Racetam Comparison
| Compound | Relative potency | Half-life | Main mechanism | |----------|-----------------|-----------|----------------| | Piracetam | 1× | ~5 hours | Membrane fluidity, AMPA | | Aniracetam | ~3–5× | ~1–2 hours | AMPA, mGluR | | Oxiracetam | ~3–4× | ~8 hours | AMPA, NMDA | | Pramiracetam | ~7×| ~5 hours | Choline uptake | | Noopept | ~1000× | ~1 hour (rapid) | AMPA, BDNF/NGF, CPG |
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