Get Your Mind Right: Noopept Addition

by Erik Tremblay

Noopept Structure Importance and Racetams

Noopept, also knowns as (Omberacetam), is a peptide containing a modified form of the amino acid Glycine giving it the chemical structure name N-phenylacetyl-L-prolylglycine ethyl ester which is used as a nootropic. The fact that the molecular structure contains a pyrrolidone structure, it is often referred to and classified in the group of compounds that are referred to as racetams, however that is technically incorrect. Noopept contains a pyrrolidone structure, but it’s not a 2-oxo-pyrrolidine which all racetams contain. A pyrrolidone structure falls into the class of lactams, meaning they are cyclic compounds that contain an Amide group. Noopept does contain a 2-pyrrolidone structure, which is 5 membered ring that contains an Amide group (Nitrogen bonded to a carbon that is double bonded to an oxygen) which allows them to produce mind-enhancing effects due to their ability to act on different neurological pathways. This has led the class of racetams to become popular as nootropic compounds, and many different versions have been produced. Noopept is is derived from racetams and was first synthesized with the racetam backbone structure of the 2-pyrrolidone ring, however in Noopept this ring is bonded to a phenyl-group. A phenyl group is a benzene ring that is attached to another substituent. Benzene rings are cyclic hexenes, meaning that it is a 6-carbon structure with double bonds, however the benzene ring has alternating double bonds. They are significant in chemistry due to their stability because they are able to undergo resonance and rearrange during reactions. The attachment of the benzene ring allows it to be much more potent than the mother of all nootropics, piracetam which was the first to be synthesized back in the 1950s as a treatment for epilepsy by Corneliu E. Giurgea. Compared to piracetam, Noopept also contains an ethyl-ester group branching off the opposite end of the phenyl group. This helps to sterically block enzymes that break down the molecule and inhibit its effects such as the class of amine oxidase enzymes. The addition of the ethyl-ester group makes it harder for the enzyme to get to the nitrogen containing group it has the affinity to bind to. Noopept has been reported as 1000x more potent in the same doses1.

Mechanism of Action

The reason Noopept is such an effective Nootropic is due to it’s ability to influence different neurotransmitters through different mechanisms.

Blood-Brain Barrier is Not so Much of a Barrier

The structure of racetams allow them to pass through the blood brain barrier relatively easily compared to other compounds. The BBB is a highly selective, semi-permeable membrane that separates what in the circulating blood is allowed to cross the membrane into the brain and cerebral spinal fluid, effectively allowing it to enter the CNS (Central Nervous System). The structure of Noopept as compared to other racetams is what allows it to more readily pass through this barrier which is why it is so effective in small doses. Once Noopept passes through this barrier, it is able to work on different pathways.

ADMA and NDMA Pathways

ADMA (Asymmetric dimethylarginine) and NDMA (N-methyl-D-aspartate) are ionotropic glutamate receptors which are stimulated by Noopept. Ionotropic receptors result in the opening of transmembrane ion-channel proteins to allow the movement of vital ions Na+, K+,Ca2+, and/or Cl- when activated by a neurotransmitter, in this case Noopept. Glutamate receptors are throughout the CNS but are located majorly in the brain and act as the bodies most prominent excitatory class of neurotransmitters and a precursor to GABA. Glutamate receptors are vital for neural communication and memory which is why taking Noopept is so effective in boosting focus as it stimulates these vital communicating receptors. Having proper ion flow through the cell membranes are also crucial in neural communication as they aid in the depolarization and hyperpolarization of cells be mediating charged ions throughout the cell membrane to cause it to turn from normally negative to more positive by the addition of positive cations (Na+,K+, Ca2+) or efflux (pump out) of negative anion (Cl-). The depolarization and repolarization of a cell is vital for its ability to conduct nerve impulses and communicate with the body.

Noopept and Acetylcholine

Acetylcholine is the neurotransmitter that works at the neuromuscular junction to stimulate motor neurons and begin the contraction process.The two major types of acetylcholine receptors are muscarinic acetylcholine receptor and nicotinic acetylcholine receptors, which are stimulated by both their corresponding compounds (muscarine and nicotine), however the compound of acetylcholine can stimulate both of these receptors. Acetylcholine is a common target for focus-enhancing supplements and some aim at working by increasing acetylcholine levels, preventing the breakdown of the molecule by the enzyme acetylcholinesterase, or encouraging it’s re-uptake in the synaptic cleft; however noopept does not work with acetylcholine in any of these methods. Noopept actually has the ability to enhance the effects of the neurotransmitter Acetylcholine by aiding in the neurotransmitters’ action on the acetylcholine receptors. Noopept iscapable of working on acetylcholine receptors to make them more sensitive so they are more easily and more likely to be activated.

Dosage

Noopept is much more potent than common racetams and other nootropics so they are not required in large doses. Noticeable performace enhancing effects can be seen in doses as little as 10mg, and this dose can be safely increased up to the 30mg range but it is not recommended to go over that[2][3].

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[1] Vakhitova YV, Sadovnikov SV, Borisevich SS, Ostrovskaya RU, A.Gudasheva T, Seredenin SB. Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept. Acta Naturae. 2016;8(1):82-89.

[2] Kolbaev, S. N., et al. “Effect of Noopept on Dynamics of Intracellular Calcium in Neurons of Cultured Rat Hippocampal Slices.” Bulletin of Experimental Biology and Medicine, vol. 164, no. 3, 2018, pp. 330–333., doi:10.1007/s10517-018-3983-3.

[3] Ostrovskaya RU, Vakhitova YV, Kuzmina US, et al. Neuroprotective effect of novel cognitive enhancer noopept on AD-related cellular model involves the attenuation of apoptosis and tau hyperphosphorylation. Journal of Biomedical Science. 2014;21(1):74. doi:10.1186/s12929-014-0074-2.

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