Noopept

Also known as: GVS-111, Omberacetam

Evidence: Clinical

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Overview

Omberacetam, a synthetic dipeptide prodrug of cycloprolylglycine; Russian human and animal studies report memory benefits linked to BDNF and NGF upregulation.

Noopept (omberacetam, N-phenylacetyl-L-prolylglycine ethyl ester) is a synthetic dipeptide that is metabolized to cycloprolylglycine, an endogenous neuropeptide. It is reported to be active at roughly 1000-fold lower doses than piracetam by weight, which reflects potency per milligram rather than a larger effect. Animal work shows increased NGF and BDNF expression in the hippocampus, and Russian clinical studies report improvements in mild cognitive impairment and reduced anxiety and irritability.

Benefits

Memory, learning, neuroprotection

Dosing reference

Research dose: 10 mg twice daily by mouth (20 mg daily), the dose used in the Russian clinical studies
Range: 10000 to 20000 mcg, 2x daily

Oral tablet, 10 mg twice daily for 1.5 to 2 months in the published studies (Neznamov and Teleshova, 2009; Amelin et al., 2011). Community protocols run 10 to 30 mg daily, above any tested dose at the top end. Rat work shows oral absorption with intact passage into brain, then conversion to cycloprolylglycine; human elimination is slower than in rats and varies widely between people, and no human metabolites were detectable at the clinical dose (Boiko et al., 2004; Boyko et al., 2018). N/A-by-design: oral tablet, so reconstitution fields are null.

Mechanism

Noopept (ethyl N-phenylacetyl-L-prolylglycinate, GVS-111) is a synthetic dipeptide ester designed as a topological analog of piracetam's beta-turn (Gudasheva et al., 2018). In rats it is absorbed orally, crosses the blood-brain barrier intact and is converted to cyclo-L-prolylglycine, an endogenous peptide with a similar activity profile (Boyko et al., 2018; Gudasheva et al., 2018). Acute dosing raised NGF and BDNF mRNA in rat hippocampus, and 28-day dosing did not produce tolerance (Ostrovskaya et al., 2008). In HEK293 reporter assays it increased DNA binding of HIF-1 and of no other transcription factor tested, which its developers propose as the primary mechanism (Vakhitova et al., 2016). Elimination is slower in humans than in rats or rabbits and varies widely between individuals, with no metabolites detectable in human plasma at the clinical dose (Boiko et al., 2004).

Evidence

Clinical: at least one published human trial or an approved drug

Acute dosing raised NGF and BDNF mRNA in rat hippocampus; 28 days of dosing potentiated rather than blunted the effect (Ostrovskaya et al., 2008)
Randomised comparison against piracetam in mild cognitive disorders of vascular and post-traumatic origin reported comparable or better cognitive scores on 10 mg twice daily (Neznamov and Teleshova, 2009)
Open 12-month study in 60 patients after stroke reported improved MMSE and verbal association scores after 2 months on 20 mg daily (Amelin et al., 2011)
Increased DNA binding of HIF-1 in a reporter assay and of no other transcription factor tested (Vakhitova et al., 2016)
Elimination is slower in humans than in rats or rabbits and highly variable between individuals, with no human plasma metabolites at the clinical dose (Boiko et al., 2004; Boyko et al., 2018)
Human-trial status: registered and marketed in Russia as 10 mg tablets after trials in mild cognitive impairment (Gudasheva et al., 2018). No approval elsewhere; US market surveillance found it sold undeclared in supplements at up to 40.6 mg per serving (Cohen et al., 2021)

References

Side effects

Headache, irritability, and sleep disturbance are the commonly reported effects, particularly at higher doses, and some users report brain fog on abrupt discontinuation. It was well tolerated in Russian clinical trials but has no independent long-term safety data and is not approved outside Russia.

Storage

Storage: Room temperature
Lyophilized: 24+ months

Pharmacology

Half-life: Not quantified in humans; elimination is slower in humans than in rats or rabbits and varies widely between individuals (Boiko et al., 2004)
Bioavailability: Orally absorbed with intact passage across the blood-brain barrier in rats (Boyko et al., 2018); no human bioavailability figure published, and no sublingual data exist
Molecular weight: 318.37 Da
Sequence: N-phenylacetyl-Pro-Gly ethyl ester (synthetic dipeptide ester, PubChem CID 180496)