Noopept, ≥98%

Chemical Information:

Technical Information:

Modes of Action:

Noopept (GVS-111) is a compound with neuroprotective and cognition enhancing properties that is derived from the racetam family. It is used in neuroscience studies and in research related to protection against cognitive impairment. Animal studies have shown Noopept to be neuroprotective and enhance memory in various tests.[1] [2] [3] 

Noopept has been shown to have anti-inflammatory action in rats and mice[4], and to normalize the response of benzodiazepine binding to stress.[5] Chronic administration of Noopept decreases the activity of stress-induced kinases and increases the expression of BDNF in the hypothalamus and hippocampus in rats.[6]

Noopept shows competitive binding to AMPA receptor sites in the rat brain with IC50 of 80 microM.[7] Noopept appears to have concentration-dependent effects on the DNA-binding activity of transcriptional factor HIF-1.[8] Furthermore, it appears to have neuroprotective effects in PC12 cells by protecting against oxidative damage and tau phosphorylation.[9]

In animal studies, the phagocytic activity of macrophages was increased along with stimulated immune response to various antigens, and increased activity of white blood cells in the spleen.[10]

Further Scientific Research:

Please note that this is not a complete account of the research available for Noopept, but is meant to give the reader a picture of the type of research conducted to-date. For more information, please refer to PubMed.

Clinical Reviews:

A few Russian reviews have noted greater efficacy of Noopept when compared to the original racetam Nootropic (Piracetam).[11] [12]

A 2003 review entitled “The Evolution of the Neuroprotection Concept” (in Russian) explains the potential role of Noopept as a neuroprotective agent. According to the article, Noopept is able to decrease the extent of cell damage in blood vessels in the brain, as well as reduce excess levels of calcium, glutamate, and free radicals.[13]

Human Studies:

There have been a few human studies on the effects of Noopept, although most have significant room for improvement in their methodology. In one study, researchers examined the effects of Noopept on patients with stroke. 60 patients with stroke were treated with Noopept daily over a course of 2 months. The authors reported significant cognitive improvement and mild improvement in global assessment categories for the Noopept group. They also mentioned a high level of safety.[14]

A 2009 study on 60 patients with respiratory tuberculosis found that Noopept helped reduce anxiety and decreased the negative side effects of anti-tuberculosis drugs administered concurrently.[15]

Noopept’s effects on EEG rhythms was studied in patients with cognitive impairment caused by cerebral trauma or disease. Increased alpha- and beta-EEG rhythms in frontal areas were noted, and decreased the rhythms in occipital areas of the brain. The changes were more pronounced in patients who had suffered from a vascular disease than in those with cerebral trauma.[16]

A 2007 Russian study examined the meteoadaptogenic (ability to adapt to changes in temperature) abilities conferred on healthy volunteers taking Noopept. The authors found that Noopept was effective at increasing the ability to adapt to temperature changes and also improved the psychological component.[17]

Animal Studies:

In 2015, a study was conducted on the effects of Noopept on cognitive processes and functional states of neural mitochondria (from rat neocortex). The study found that the cognitive effects of Noopept were related to its effects on mitochondrial function.[18]

A study on rats with streptozotocin-induced diabetes found that Noopept had normalizing effects on concentrations of incretin GLP-1 and insulin (both decreased after poisoning with streptozotocin). The mechanism for these effects was not found.[19] Another study found that Noopept had the capacity to reduce blood glucose levels in rats with streptozotocin-induced diabetes. Again, the underlying mechanism was not found.[20] 

A 2012 study on rats examined Noopept’s anti-inflammatory abilities. Rats poisoned with carrageenan and concanavalin A (to induce excessive inflammation) were then treated with Noopept. The authors found that high doses of Noopept (5 mg/kg) decreased the inflammatory response to the poisons. Cytokines, IL-6 interleukin, and TNF-alpha all had significantly lower levels in animals that were treated with Noopept prior to poisoning. [4]

A second study from 2012 examined the exploratory behavior of mice treated with various Nootropic substances, including Noopept. The study used two strains of mice. BALB/c mice, who are characterized by greater anxiety and lower exploratory behavior, had the greatest responses to the Nootropics. Noopept seemed to confer anti-anxiety effects and improved ability for exploration in BALB/c mice.[21] [22]

In 2010, the effects of Noopept on stress factors in rat brains was studied. Chronic (28 days) treatment of low dose Noopept (0.5mg/day), decreased stress factors in the hippocampus and hypothalamus. Specifically, the activity of stress-induced kinases SAPK/JNK 46/54 and pERK ½ was decreased significantly. In the hypothalamus, BDNF protein increased somewhat. The authors concluded that Noopept has activity with respect to some of the pathogenic mechanisms of Alzheimer’s disease.[23]

A 2008 study examined the effects of Noopept on memory in rats. Animals were treated with cholinoceptor antagonists (scopolamine and mecamylamine). The authors noted that Noopept abolished the negative effects of these poisons.[24]

A 2007 study looked into the effects of Noopept on memory and learning in BALB/c mice. Noopept prevented the development of cognitive defects in response to poisoning with scopolamine.[25]

References:

• [1] 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.
• [2] 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.
• [3] 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.
• [4] Alekseeva SV, Kovalenko LP, Tallerova AV, Gudasheva TA, Durnev AD. (2012) [An experimental study of the anti-inflammatory action of noopept and its effect on the level of cytokines]. (Article in Russian). Eksp Klin Farmakol, 75(9):25-7
• [5] Iarkova MA. (2011). [Analysis of the binding capacity of the benzodiazepine site of gabaa receptor in mice C57BL/6 and BALB/C pretreated with anxiolytics]. (Article in Russian) Eksp Klin Farmakol, 74(8):3-7.
• [6] Ostrovskaia RU, Vakhitova IuV, Salimgareeva MKh, Iamidanov RS, Sadovnikov SV, Kapitsa IG, Seredenin SB. (2010). [On the mechanism of noopept action: decrease in activity of stress-induced kinases and increase in expression of neutrophines]. (Article in Russian) Eksp Klin Farmakol, 73(12):2-5.
• [7] Firstova IuIu, Vasil'eva EV, Kovalev GI. (2011) [Studying specific effects of nootropic drugs on glutamate receptors in the rat brain]. (Article in Russian). Eksp Klin Farmakol, 74(1):6-10.
• [8] Vakhitova YV, Sadovnikov SV, Borisevich SS, Ostrovskaya RU, A Gudasheva T, Seredenin SB. (2016). Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept. Acta Naturae, 8(1):82-9.
• [9] Ostrovskaya RU, Vakhitova YV, Kuzmina USh, Salimgareeva MKh, Zainullina LF, Gudasheva TA, Vakhitov VA, Seredenin SB. (2014). Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation. J Biomed Sci, 21(1): 74.  21(1): 74. Published odate. Forto PubMed. nd  meant to give the reader a picture of the type of research conducted to-date. For
• [10] Kovalenko LP, Shipaeva EV, Alekseeva SV, Pronin AV, Durnev AD, Gudasheva TA, Ostrovskaja RU, Seredenin SB. (2007). Immunopharmacological properties of noopept. Bull Exp Biol Med, 144(1):49-52.
• [11] Ostrovskaia RU, Gudasheva TA, Voronina TA, Seredenin SB. (2002). [The original novel nootropic and neuroprotective agent noopept] (Article in Russian). Eksp Klin Farmakol, 65(5):66-72
• [12] Gudasheva TA, Skoldinov AP. (2012). [Design of the novel dipeptide neuropsychotropic drug preparations] (Article in Russian). Eksp Klin Farmakol, 66(2):15-9.
• [13] RU Ostrovskaia. (2003). [Evolution of the neuroprotection concept]. Eksp Klin Farmakol, 66(2):32-7.
• [14] Amelin AV, Iliukhina AIu, Shmonin AA. (2011). [Noopept in the treatment of mild cognitive impairment in patients with stroke] (Article in Russian). Zh Nevrol Psikhiatr Im S S Korsakova, 111(10 Pt 1):44-6.
• [15] Mordyk AV, Lysov AV, Kondria AV, Gol'dzon MA, Khlebova NV. (2009). [Prevention of neuro- and cardiotoxic side effects of tuberculosis chemotherapy with noopept] (Article in Russian). Klin Med (Mosk), 87(5):59-62.
• [16] Bochkarev VK, Teleshova ES, Siuniakov SA, Davydova DV, Neznamov GG. (2008). [Clinical and electroencephalographic characteristic of noopept in patients with mild cognitive impairment of posttraumatic and vascular origin] (Article in Russian). Zh Nevrol Psikhiatr Im S S Korsakova, 108(11):47-54
• [17] Shabanov PD, Ganapol'skiĭ VP, Aleksandrov PV. (2007). [Meteoadaptogenic properties of peptide drugs in healthy volunteers] (Article in Russian). Eksp Klin Farmakol, 70(6):41-7
• [18] Zhiliuk VI, Mamchur VI, Pavlov SV. (2015). [Role of functional state of neuronal mitochondria of cerebral cortex in mechanisms of nootropic activity of neuroprotectors in rats with alloxan hyperglycemia] (Article in Russian). Eksp Klin Farmakol, 78(2):10-4.
• [19] Ostrovskaya RU, Zolotov NN, Ozerova IV, Ivanova EA, Kapitsa IG, Taraban KV, Michunskaya AM, Voronina TA, Gudasheva TA, Seredenin SB. (2014). Noopept normalizes parameters of the incretin system in rats with experimental diabetes. Bull Exp Biol Med, 157(3):344-9.
• [20] Ostrovskaya RU, Ozerova IV, Gudascheva TA, Kapitsa IG, Ivanova EA, Voronina TA, Seredenin SB. (2014). Comparative activity of proline-containing dipeptide noopept and inhibitor of dipeptidyl peptidase-4 sitagliptin in a rat model of developing diabetes. Bull Exp Biol Med, 156(3):342-6.  
• [21] Vasil'eva EV, Salimov RM, Kovalev GI. (2012). [Effects of nootropic drugs on behavior of BALB/c and C57BL/6 mice in the exploratory cross-maze test] (Article in Russian). Eksp Klin Farmakol, 75(7):3-7
• [22] AP Bel’nik, RU Ostrovskaya, II Poletaeva. (2009) Genotype-dependent characteristics of behavior in mice in cognitive tests. The effects of Noopept. Neurosci Behav Physiol, 39(1):81-6.
• [23] Zhiliuk VI, Levykh AÉ, Mamchur VI. (2012). [Platelet hyperreactivity and antiaggregatory properties of nootropic drugs under conditions of alloxan-induced diabetes in rats]. (Article in Russian). Eksp Klin Farmakol, 75(4):38-41.
• [24] Radionova KS, Belnik AP, Ostrovskaya RU. (2008). Original nootropic drug noopept prevents memory deficit in rats with muscarinic and nicotinic receptor blockade. Bull Exp Biol Med, 146(1):59-62
• [25] Belnik AP, Ostrovskaya RU, Poletaeva II. (2007). Dipeptide preparation Noopept prevents scopolamine-induced deficit of spatial memory in BALB/c mice. Bull Exp Biol Med, 143(4):431-3