Noopept

links: Nootropics Racetams reference: 4-13-2021

Noopept (Omberacetam) (GVS-111) #

• AKA (N-Phenylacetyl-L-prolylglycine ethyl ester) Converted into phenylacetic acid, prolylglycine, and Cycloprolylglycine, a naturally-produced neurodipeptide which I think is how noopept exerts its effects.
• I believe it is much more glutamatergic than the other racetams; its vasodilatory effects can cause headaches which seem to be not uncommon. It can be used to kill NMDA antagonist trips (like Ketamine).
  • The drug action is based on the Antioxidant effect, the antiinflammatory action, and the ability to inhibit the neurotoxicity of excess calcium and glutamate, and to improve the blood rheology.
• Piracetam (400mg/kg (=~4.6g HED)) increased Alpha waves/Beta waves1 EEG activity in the left frontal cortex, and Alpha waves activity in both the right cortex and Hippocampus. Noopept (0.2mg/kg (=~2.27g HED)) increased Alpha waves/Beta waves1 activity… in all brain areas. The effect of Noopept in the alpha/beta1 ranges was replaced by increased beta2 activity after the eighth injection, while no effects were observed after the ninth one. R
• AMPA agonist: Studying specific effects of nootropic drugs on glutamate receptors in the rat brain

Memory #

• R decreased cerebral cortex BDNF and NGF acutely! HED = ~5.67 ip (which I guess is 100% absorption). Studies on isolated neurons of Helix lucorum showed that Noopept increases sensitivity of the postsynaptic membrane to acetylcholine.

• R Noopept will make you a non-fearful rat.

  • Respectively: 2, 3, 4 = 0.05, 0.1, 0.5 mg/kg = 0.56, 1.13, 5.67 HED | 5, 6, 7 = 100, 300, 600 mg/kg = 1.13, 3.39, 6.78 HED. Not a good sign for high dose piracetam chads.

• Novel nootropic dipeptide Noopept increases inhibitory synaptic transmission in CA1 pyramidal cells (2010)

  • It was suggested that Noopept mediates its effect due to the activation of inhibitory Interneurons terminating on CA1 pyramidal cells. Results of current clamp recording of inhibitory interneurons residing in stratum radiatum confirmed this suggestion.

• Nootropic dipeptide noopept enhances inhibitory synaptic transmission in the hippocampus (2010)

  • 1mM significantly increased the frequency of spike-dependant spontaneous IPSCs whereas spike-independent mIPSCs remained unchanged, as well as the kinetic parameters (rise and decay time). It increasess the firing of GABA Interneurons.
    • I wouldn’t jump to the conclusion that this “inhibits memory” or something. I think it just makes you more selective, right? Or, it’s more like it enhances recall at the expense or encoding? However:
      • The original novel nootropic and neuroprotective agent noopept (2002)
        • In contrast to piracetam facilitating only the early stages of the memory process, noopept positively influences the Memory consolidation and retrieval steps as well… produces an additional selective anxiolytic action. The pronounced neuroprotective effect of noopept was demonstrated both in vivo (in cases of various forms of brain ischemia) and in vitro (on various neuronal models).

• Noopept improves the spatial memory and stimulates prefibrillar beta-amyloid antibody production in mice

• Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept

  • Increase in HIF-1α DNA-binding activity. Indeed, this may be its main MOA.
    • Its effects on HIF suggest that it shouldn’t be used continuously. -Peat. Interesting, since It is known that activation of the HIF system is now regarded as one of the main mechanisms of neuroprotection during hypoxia, cerebral ischemia, and neurodegenerative diseases. Relation to CO2??
  • Enhances Antioxidant activity.
  • Represses the stress-induced pSAK/JNK and pERK1.
  • 

Anecdote #

Laser focus basically. One thing while totally losing track of time. Similar to my experience with Oxiracetam, really, except less lateral.

Supplementation #

• Dose: 10-30mg oral @ ~10% bioavailability, so really you want sublingual/intranasal <=3mg.
• Duration: 20-60 minute onset -> 2 hour peak -> 3 hour offset. Thus plenty of people take it multiple times per day.
• The longest human trial was 56 days, which was safe - thus many people cycle it for 2 or 3 months with a few weeks break afterwards. There’s no determined “safe” dose. Like most other racetams, it has no tolerance - reverse, if anything.

Formulation #

• Fat-soluble, but chemspider says 1.3mg/mL in water, and requires hours of stirring. Then how tf does science.bio have it at 10x that? It does have acetate and BKC for stability and is meant to be refrigerated…

Actually it looks to be plenty soluble in water. The double bonded O in the amides should participate in resonance which would give the O’s a delta negative charge and the nitrogen a delta positive charge, but the benzene, as well as the CH’s in the pentose, and the methyl group, should make it fat soluble. I don’t know much about solubility in fat, but Van Der Waal and Electrostatic attractions are marginally weaker than hydrogen bonds (~3 vs ~1), which this will definitely form due to its polarity, so taking it with fat and water is a good idea to cover all bases (especially since electrostatic attraction is present in all chemical interactions, so is present in the formation of hydrogen bonds as well, fat isn’t unique). The ethyl ester will hydrolyze?

Bacteriostatic water - 10mL $2.12 + shipping. This stuff contains 9mg/mL or 9% benzyl alcohol, which fucks your nose up a good bit

• What’s more, deionized water is quite reactive to CO2. It doesn’t stay deionized forever.