Supplement of the Month: Noopept

November 03, 2015

Supplement of the Month: Noopept

 

What is Noopept?

            For a team of highly talented Russian scientist, Noopept was the answer to the low biological activity observed with one of the first nootropics, Piracetam. For a long time scientists were attempting to create a more potent analogue of Piracetam but failed to create one. That is until the team of Russian scientists decided draw upon their previous research findings, which found a possible mechanism of action behind Piracetams effects. In this study they noted that the amino acid proline is remarkably similar in structure to Piracetam, and that proline administered in a form that makes it’s way into the brain was able to induce memory loss.

  

They concluded that it could be possible that Piracetam can block the memory impairing effects of proline in the brain due to its similar structure1. They used this knowledge to create various Proline containing dipeptides, one of which was Noopept. The Noopept dipeptide consists of the amino acids proline and glycine, which are stabilized by an N-Phenylacetyl group and an ethyl ester group.

 

It was found that Noopept has a similar effect to Piracetam with the exception that it requires a much lower dose than Piracetam does, 5-10 mg Vs. 1,600-4,800 mg and that regardless of dose, it has even more nootropic activity than Piracetam.

            Noopept is often falsely believed to be part of a family of compounds called the racetams. Piracetam is part of this family and due to Noopept’s similarity to Piracetam it is often classed as a racetam. However a racetam must contain a 2-pyrrolidine core structure, which Noopept does not contain. As discussed earlier proline closely resembles Piracetam and this is likely why the proline structure in Noopept is often mistaken for the 2-pyrrolidone core structure in Piracetam.

            Noopept is quite unique amongst other nootropics because it seems that it is a pro-drug for a neuropeptide that our body produces. This peptide is called cyclo-prolylglycine, levels of which have been show to increase after Noopept administration2. Levels of Noopept however are undetectable in the brain an hour after administration, which suggests that Noopept itself likely has no biological activity2. This statement is reinforced by the fact that cyclo-prolylglycine seems to exert a nootropic effect when it is administered in its isolated form3.

What are Noopept’s applications?

            Noopept is a very interesting substance because it has a wide array of effects. It is strongly neuroprotective both via having an antioxidant effect in the brain and by regulating glutamate neurotransmission4. It has the ability to enhance memory and learning, likely via two distinct pathways, acetylcholine5 and neurotrophins6. It has a subtle anxiety reducing effect7. It seems to regulate the immune system8 and even seems to be protective against some of the deficits induced by diabetes9 and Alzheimer’s disease10. Overall it seems that Noopept exerts a general positive effect on cognitive health.

Pharmacology

            Unsurprisingly, Noopept exerts a wide variety of pharmacological effects on the brain. This article would turn into a book if all pharmacological effects were discussed so we will discuss only two of Noopept’s main pharmacological effects that are most relevant to this article, enhanced learning and memory.

            Noopept seems to cause a non-specific increase in learning and memory. There are two main pathways, which this seems to occur through. The first pathway seems to be the cholinergic system, which is not entirely unsurprising since piracetam, which Noopept was modelled after, also exerts its positive effects on memory via the cholinergic system. When rats and humans are administered drugs that block acetylcholine receptors, a marked decrease in memory is observed. Noopept seems to significantly counteract the memory decreasing effects of acetylcholine antagonists, which suggests that it somehow preserves acetylcholine activity5. The second pathway seems to be the neurotrophin system, specifically through the neurotrophins NGF and BDNF. It has been observed that administration of Noopept causes an increase in the levels of NGF and BDNF in a brain region called the hippocampus6. These two neurotrophins play a big role in memory and learning in part because they are responsible for the growth and generation of brain cells, which in this scenario is especially important since the hippocampus plays a crucial role in memory and learning. The effects of these neurotrophins on memory and learning will increase over time since they are gradually increasing the connectivity of the hippocampus11. This would mean that the administration of Noopept could potentiate itself over time.

How to take

            Noopept’s recommended dose is 10-30 mg per day. It is recommended that Noopept be taken for prolonged periods of time due to it having cumulative benefits over time. You can purchase Noopept here at 50 % off for the month of November.

Written by Emiel Bakker on behalve of Focus Supplements 

References

  1. Ostrovskaya, R. U., Trofimov, S. S., Tsybina, N. M., Gudasheva, T. A., Skoldinov, A. P., & Zakusov, V. V. (1985). Antagonism between pyracetam and proline in their effect on memory. Bulletin of Experimental Biology and Medicine, 99(3), 306-309.
  2. Gudasheva, T. A., Seredenin, S. B., Boyko, S. S., Ostrovskaya, R. U., Voronina, T. A., Akparov, V. K., . . . Zherdev, V. P. (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.
  3. Gudasheva, T. A., Boyko, S. S., Akparov, V. K., Ostrovskaya, R. U., Skoldinov, S. P., Rozantsev, G. G., . . . Seredenin, S. B. (1996). Identification of a novel endogenous memory facilitating cyclic dipeptide cyclo-prolylglycine in rat brain. FEBS Letters,391(1), 149-152.
  4. Ostrovskaya, R., Vakhitova, Y., Kuzmina, U., Salimgareeva, M., Zainullina, L., Gudasheva, T., . . . Seredenin, S. (2014). Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation. Journal of Biomedical Science, 21(1), 74-74.
  5. Radionova, K. S., Belnik, A. P., & Ostrovskaya, R. U. (2008). Original nootropic drug noopept prevents memory deficit in rats with muscarinic and nicotinic receptor blockade.Bulletin of Experimental Biology and Medicine, 146(1), 59-62. 
  6. Ostrovskaya, R. U., Gudasheva, T. A., Zaplina, A. P., Vahitova, J. V., Salimgareeva, M. H., Jamidanov, R. S., & Seredenin, S. B. (2008). Noopept stimulates the expression of NGF and BDNF in rat hippocampus. Bulletin of Experimental Biology and Medicine, 146(3), 334-337.
  7. Kondratenko, R. V., Derevyagin, V. I., & Skrebitsky, V. G. (2010). Novel nootropic dipeptide noopept increases inhibitory synaptic transmission in CA1 pyramidal cells. Neuroscience Letters, 476(2), 70-73.
  8. Kovalenko, L. P., Shipaeva, E. V., Alekseeva, S. V., Pronin, A. V., Durnev, A. D., Gudasheva, T. A., . . . Seredenin, S. B. (2007). Immunopharmacological properties of noopept. Bulletin of Experimental Biology and Medicine, 144(1), 49-52.
  9. Ostrovskaya, R. U., Seredenin, S. B., Zolotov, N. N., Ozerova, I. V., Ivanova, E. A., Kapitsa, I. G., . . . Gudasheva, T. A. (2014). Noopept normalizes parameters of the incretin system in rats with experimental diabetes. Bulletin of Experimental Biology and Medicine, 157(3), 344-349.
  10. Ostrovskaya, R. U., Belnik, A. P., & Storozheva, Z. I. (2008). Noopept efficiency in experimental alzheimer disease (cognitive deficiency caused by β-amyloid25–35 injection into meynert basal nuclei of rats). Bulletin of Experimental Biology and Medicine, 146(1), 77-80.
  11. Tyler, W. J., Alonso, M., Bramham, C. R., & Pozzo-Miller, L. D. (2002). From acquisition to consolidation: On the role of brain-derived neurotrophic factor signaling in hippocampal-dependent learning.Learning and Memory, 9(5), 224-237. 



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