Noopept

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Noopept
Noopept.svg
Systematic (IUPAC) name
N-Phenylacetyl-L-prolylglycine ethyl ester
Clinical data
Legal status Unscheduled (US)
Identifiers
CAS number 157115-85-0 YesY
ATC code ?
PubChem CID 180496
ChemSpider 157065 N
Chemical data
Formula C17H22N2O4 
Mol. mass 318.367 g/mol
 N (what is this?)  (verify)

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.[1] It is sold as a dietary supplement in the US and as a medicine in other countries.

Mechanism of action[edit]

It is derived from the racetam family of drugs and shares similar mechanisms of action,[2][3] but is, according to studies, 1000 times more potent than the prototypical racetam drug, piracetam.[4] Animal studies have shown noopept to be neuroprotective and enhance memory in various tests.[5][6][7][8][9] 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.[10][not in citation given (See discussion.)] It does show good blood–brain barrier penetration[11] 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[3]), and human studies have shown promising results, with potential application in the treatment of Alzheimer's disease.[12] It is also an "immunocorrector" in mice.[13]

It has been found to stimulate the expression of NGF and BDNF in rat hippocampus.[8] 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.[8]

Product information[edit]

Noopept Box Front
Noopept blister pack

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.[14][unreliable medical source?][15][unreliable medical source?]

In animal studies, Noopept helped to restore memory and other cognitive functions disturbed as a result of ischemia as well as damage due to hypoxia (a condition in which the body or region of the body is deprived of adequate oxygen supply).[16] 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.[14][unreliable medical source?][15][unreliable medical source?]

It has also been observed to reverse and prevent learned helplessness neurosis in rats after long term (21 day) treatment.[17]

References[edit]

  1. ^ PatentGenius.com http://www.patentgenius.com/patent/5439930.html
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  9. ^ 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. 
  10. ^ 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. 
  11. ^ 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. 
  12. ^ 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. 
  13. ^ 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. 
  14. ^ a b JSC LEKKO product page (http://www.lekko-pharm.ru/products/noopept/)
  15. ^ a b Noopept treatment with moderate encephalopathy cognitive impairment, NN Yakhno, MD http://www.noopept.ru/pic/n310920091.pdf
  16. ^ Noopept reduces the postischemic functional and metabolic disorders in the brain of rats with different sensitivity to hypoxia. PMID 19529857. Retrieved 12 November 2013. 
  17. ^ Studies of long-term noopept and afobazol treatment in rats with learned helplessness neurosis. PMID 17369939. Retrieved 15 September 2013.