Identity a synthetic dipeptide-derived small molecule built on a Pro-Gly core, designed as a dipeptide analog of the racetam nootropic piracetam. It is a prodrug of cycloprolylglycine (cPG) — an endogenous cyclic dipeptide naturally present in the mammalian brain — which is its main active metabolite. Crucially, it is orally bioavailable and crosses the blood-brain barrier after being swallowed. ## Development & history - Designed in 1996 at the V.V. Zakusov Research Institute of Pharmacology (Russian Academy of Medical Sciences, Moscow) by Tatiana Gudasheva, Sergei Seredenin and colleagues — as a dipeptide analog of piracetam (the hypothesis: piracetam's pyrrolidine ring mimics a proline residue and its N-acetamide mimics glycine).
- The result was active at ~1000× lower doses than piracetam by weight (~ vs ~) with a broader cognitive + anxiolytic + neuroprotective profile. (Note: the "1000×" reflects potency and mechanism, not 1000× the benefit — a common misreading.)
- Approved and prescribed in Russia (and neighbouring countries) as a nootropic/neuroprotective medicine. ## Mechanism (as proposed) Noopept is hydrolysed and cyclised to cycloprolylglycine (cPG), an endogenous neuropeptide that modulates AMPA glutamate receptors (key to synaptic transmission and long-term potentiation). It also upregulates BDNF and NGF in the hippocampus (the same neurotrophic theme as Semax/Selank), with cholinergic, antioxidant, anti-inflammatory and HIF-1-mediated (hypoxia-neuroprotective) effects reported. The mechanism is complex, not fully elucidated, and distinct from the classical racetams.