Noopept
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| Systematic (IUPAC) name | |
| N-Phenylacetyl-L-prolylglycine ethyl ester | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Not approved (US) |
| Identifiers | |
| CAS number | 157115-85-0  |
| ATC code | ? |
| PubChem | CID 180496 |
| Chemical data | |
| Formula | C17H22N2O4 |
| Mol. mass | 318.367 g/mol |
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Noopept (Russian: Ноопепт; GVS-111, N-phenylacetyl-L-prolylglycine ethyl ester) is a medication 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 has patent applications in both the US and Russia.[1][2] It is not approved by the Food and Drug Administration for use in the United States or by the European Medicines Agency for use in Europe.
Mechanism of action[edit]
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This section needs more medical references for verification or relies too heavily on primary sources. (November 2012) |
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It is derived from the racetam family of drugs and shares similar mechanisms of action,[3][4] but is, according to studies, 1000 times more potent than the prototypical racetam drug, piracetam.[5] Animal studies have shown noopept to be neuroprotective and enhance memory in various tests.[6][7][8][9][10] Unusually for a peptide-derived compound, noopept displays both high oral bioavailability[11] and good blood–brain barrier penetration[12] 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[4]), and human studies have shown promising results, with potential application in the treatment of Alzheimer's disease.[13] It is also an "immunocorrector" in mice.[14]
It has been found to stimulate the expression of NGF and BDNF in rat hippocampus.[9] 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.[9]
Product information[edit]
In Russia, Noopept is considered a nootropic drug with neuroprotective properties. It is reported to improve learning ability and memory (including the initial processing of information, consolidation, and retrieval).[medical citation needed] It is also used to prevent the development of amnesia induced by electroshock.[15][unreliable medical source?][16][unreliable medical source?]
In studies Noopept helped to restore memory and other cognitive functions disturbed as a result of brain injury, local and global ischemia and prenatal damage (alcohol, hypoxia).[medical citation needed] The therapeutic effect of the drug in patients with organic disorders of the central nervous system appeared within 5-7 days of treatment. Also reported was the reduction or disappearance of anxiety, irritability, emotional lability and sleep disorders.[15][unreliable medical source?][16][unreliable medical source?]
References[edit]
- ^ US application 5439930, "Biologically active n-acylprolydipeptides having antiamnestic, antihypoxic and anorexigenic effects", published Aug 8, 1995
- ^ Patent of Russian Federation number 2119496
- ^ 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 Pharmacology 29 (1): 85–99. doi:10.1016/S0306-3623(96)00529-0. PMID 9195198.
- ^ a b Gudasheva 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 Pharmacokinetics 22 (3): 245–252. doi:10.1007/BF03189814. PMID 9358206.
- ^ 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. PMID 12596521.
- ^ 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 Pharmacology 10 (5): 549–553. doi:10.1097/00008877-199909000-00013. PMID 10780261.
- ^ 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 Neuroscience 21 (3): 117–124. doi:10.1016/S0736-5748(03)00031-5. PMID 12711349.
- ^ 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 Psychopharmacology 21 (6): 611–619. doi:10.1177/0269881106071335. PMID 17092975.
- ^ a b c Ostrovskaya 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 Medicine 146 (3): 334–337. doi:10.1007/s10517-008-0297-x. PMID 19240853.
- ^ 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 Medicine 134 (6): 528–530. doi:10.1023/A:1022940507519. PMID 12660828.
- ^ 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 Medicine 132 (4): 959–962. doi:10.1023/A:1013663126973. PMID 11782792.
- ^ 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 Medicine 129 (4): 359–361. doi:10.1007/BF02439270. PMID 10977920.
- ^ 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 Physiology 39 (3): 311–321. doi:10.1007/s11055-009-9128-4. PMID 19234797.
- ^ 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 Medicine 144 (1): 49–52. doi:10.1007/s10517-007-0251-3. PMID 18256750.
- ^ a b JSC LEKKO product page (http://www.lekko-pharm.ru/products/noopept/)
- ^ a b Noopept treatment with moderate encephalopathy cognitive impairment, NN Yakhno, MD http://www.noopept.ru/pic/n310920091.pdf
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