Noopept (Russian: Ноопепт; GVS-111, N-phenylacetyl-L-prolylglycine ethyl ester) is a peptide promoted and prescribed in Russia and neighbouring countries as a nootropic. The registered brand name Noopept (Ноопепт) is trademarked by the manufacturer JSC LEKKO Pharmaceuticals. The compound is patented in both the US and Russia with patent of Russian Federation number 2119496, US Patent number 5,439,930 issued 8/8/1995. It is sold as a dietary supplement in the US and as a medicine in other countries.
Mechanism of action
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It is derived from the racetam family of drugs and shares similar mechanisms of action, but is, according to studies, 1000 times more potent than the prototypical racetam drug, piracetam. Animal studies have shown noopept to be neuroprotective and enhance memory in various tests. Since it is a peptide-derived compound, noopept is degraded by enzymes in the GI tract and liver. Its oral bioavailability has been shown to be much lower than other routes of administration, with serum concentrations reaching 10% of IV levels per-orally.[not in citation given (See discussion.)] It does show good blood–brain barrier penetration in rats (although a previous study concluded that "GVS-111 itself was not found in rat brain 1 h after 5 mg/kg i.p. administration up to limit of detection" and that administration of Noopept only increases the concentration of endogenous nootropic cyclo-L-prolylglycine), and human studies have shown promising results, with potential application in the treatment of Alzheimer's disease. It is also an "immunocorrector" in mice.
It has been found to stimulate the expression of NGF and BDNF in rat hippocampus. Expression of the studied neurotropic factors in the cerebral cortex was below the control after single administration of Noopept, while chronic administration caused a slight increase in BDNF expression. In the hippocampus, expression of mRNA for both neurotrophins increased after acute administration of Noopept. Chronic treatment with Noopept was not followed by the development of tolerance, but even potentiated the neurotrophic effect.
^Solntseva EI, Bukanova JV, Ostrovskaya RU, Gudasheva TA, Voronina TA, Skrebitsky VG (1997). "The effects of piracetam and its novel peptide analogue GVS-111 on neuronal voltage-gated calcium and potassium channels". General Pharmacology29 (1): 85–99. doi:10.1016/S0306-3623(96)00529-0. PMID9195198.
^ abGudasheva TA, Boyko SS, Ostrovskaya RU, Voronina TA, Akparov VK, Trofimov SS, Rozantsev GG, Skoldinov AP, Zherdev VP, Seredenin SB (1997). "The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine". European Journal of Drug Metabolism and Pharmacokinetics22 (3): 245–252. doi:10.1007/BF03189814. PMID9358206.
^Ostrovskaia RU, Gudasheva TA, Voronina TA, Seredenin SB (2002). "The original novel nootropic and neuroprotective agent noopept" [The original novel nootropic and neuroprotective agent noopept]. Eksperimentalnaia i klinicheskaia farmakologiia (in Russian) 65 (5): 66–72. PMID12596521.
^Ostrovskaya RU, Romanova GA, Barskov IV, Shanina EV, Gudasheva TA, Victorov IV, Voronina TA, Seredenin SB (1999). "Memory restoring and neuroprotective effects of the proline-containing dipeptide, GVS-111, in a photochemical stroke model". Behavioural Pharmacology10 (5): 549–553. doi:10.1097/00008877-199909000-00013. PMID10780261.
^Pelsman A, Hoyo-Vadillo C, Gudasheva TA, Seredenin SB, Ostrovskaya RU, Busciglio J (2003). "GVS-111 prevents oxidative damage and apoptosis in normal and Down's syndrome human cortical neurons". International Journal of Developmental Neuroscience21 (3): 117–124. doi:10.1016/S0736-5748(03)00031-5. PMID12711349.
^Ostrovskaya RU, Gruden MA, Bobkova NA, Sewell RD, Gudasheva TA, Samokhin AN, Seredinin SB, Noppe W, Sherstnev VV, Morozova-Roche LA (2007). "The nootropic and neuroprotective proline-containing dipeptide noopept restores spatial memory and increases immunoreactivity to amyloid in an Alzheimer's disease model". Journal of Psychopharmacology21 (6): 611–619. doi:10.1177/0269881106071335. PMID17092975.
^ abcOstrovskaya RU, Gudasheva TA, Zaplina AP, Vahitova JV, Salimgareeva MH, Jamidanov RS, Seredenin SB (2008). "Noopept stimulates the expression of NGF and BDNF in rat hippocampus". Bulletin of Experimental Biology and Medicine146 (3): 334–337. doi:10.1007/s10517-008-0297-x. PMID19240853.
^Romanova GA, Shakova FM, Gudasheva TA, Ostrovskaya RU (2002). "Impairment of learning and memory after photothrombosis of the prefrontal cortex in rat brain: Effects of Noopept". Bulletin of Experimental Biology and Medicine134 (6): 528–530. doi:10.1023/A:1022940507519. PMID12660828.
^Ostrovskaya RU, Mirsoev TK, Romanova GA, Gudasheva TA, Kravchenko EV, Trofimov CC, Voronina TA, Seredenin SB (2001). "Proline-containing dipeptide GVS-111 retains nootropic activity after oral administration". Bulletin of Experimental Biology and Medicine132 (4): 959–962. doi:10.1023/A:1013663126973. PMID11782792.
^Boiko SS, Ostrovskaya RU, Zherdev VP, Korotkov SA, Gudasheva TA, Voronina TA, Seredenin SB (2000). "Pharmacokinetics of new nootropic acylprolyldipeptide and its penetration across the blood–brain barrier after oral administration". Bulletin of Experimental Biology and Medicine129 (4): 359–361. doi:10.1007/BF02439270. PMID10977920.
^Neznamov GG, Teleshova ES (2009). "Comparative studies of Noopept and piracetam in the treatment of patients with mild cognitive disorders in organic brain diseases of vascular and traumatic origin". Neuroscience and Behavioural Physiology39 (3): 311–321. doi:10.1007/s11055-009-9128-4. PMID19234797.
^Kovalenko LP, Shipaeva EV, Alekseeva SV, Pronin AV, Durnev AD, Gudasheva TA, Ostrovskaja RU, Seredenin SB (2007). "Immunopharmacological properties of noopept". Bulletin of Experimental Biology and Medicine144 (1): 49–52. doi:10.1007/s10517-007-0251-3. PMID18256750.