7 replies to this topic

[thedevinroy]

This thread is dedicated to the general discussion of Ampakines. Feel free to express your thoughts, feelings, and questions openly about this topic.

An Ampakine is a chemical that either modulates or sensitizes the AMPA receptor. An AMPA receptor is a type of glutamate receptor with a binding site for AMPA. When AMPA binds to the receptor, it boosts the activity of glutamate. Ampakines are especially of interest as a nootropic due to their cognition enhancing abilities and possible BDNF factors. Racetam drugs such as Piracetam, Aniracetam, and Pramiracetam have Ampakine properties.

Examples:

• 1-BCP
• Aniracetam
• CX-516
• CX-546
• CX-614
• CX-691 (Farampator)
• CX-717
• CX-1739
• CX-???
• Cyclothiazide
• Idebenone (at 10uM, toxicity at 25uM)
• IDRA-21
• LY-404,187
• LY-503,430
• Oxiracetam
• PEPA
• Piracetam
• Pramiracetam
• S-18986
• Sunifiram
• Unifiram

Questions to Spur Discussion:

• Have you any experience with unconventional Ampakines?
• Do you have any chemicals to add to the list of Ampakines?
• What do you expect the future to hold for stronger Ampakines?
• Are there potential negative effects from Ampakines that would make you hesitate to try one?
• Would you like to add any studies to determine effectiveness vs. toxicity?
• What else do you know about Ampakines that hasn't been shared? News? Science? Fun facts?

[thedevinroy]

Let me start by saying that the future holds the key to sleep apnea. CX-1739 is currently being researched for sleep apnea. This is a huge discovery because this affects many Americans, and hopefully, it will open the door to a variety of purposes and discoveries in understanding the AMPA receptors.

Also, I am wary of trying any compound with fluoride in its structure (LY-503,430, PEPA, Unifram). There's enough of that toxin to go around in our town water supplies and toothpaste.

The only reason to not try another Ampakine, that I can think of, is for fear of over excitation. Too much glutamate activity can cause seizures.

Edited by devinthayer, 27 June 2011 - 05:39 PM.

[Ampa-omega]

Hi there, its a shame most people here don't know more about the science of what they are buying (racetams) when looking for nootropic substances. glutaminergic and gaba signaling has all to do with the information processing in the brain, which is why ampakines may be what everyone is looking for when they want a nootropic substance. (although safety is always a valid concern to be on lookout)

I dont think the flouride issue may be valid with unifiram because it may be a different form of fluoride as a flourine, and which may also have totally different properties in comparison to flouride. fluoride is a concern though. its best to double check yourself as i don't really know


Also would like to add that cAMP and cGMP, and phosphorylation in general is highly relevant to glutaminergic signaling.

"BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype. The PDE9A enzyme is expressed primarily in the brain, with high concentrations in the cerebellum, neocortex, striatum, and hippocampus, and acts to limit the cGMP-mediated signal transduction which occurs following glutamate binding to NMDA receptors. Consequently selective PDE9A inhibitors were predicted to prolong intracellular responses to glutamate and enhance glutamate signalling, and since this process is known to be involved in learning and memory, PDE9A inhibitors should have a nootropic effect and may be useful in the treatment of Alzheimer's.[1]" http://en.wikipedia....iki/BAY_73-6691

and histaminergics may also have glutamate activity, such as Modafinil and ABT-239.

"ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia.[1][2][3][4] ABT-239 is more active at the human H3 receptor than comparable agents such as thioperamide, ciproxifan, and cipralisant. It was ultimately dropped from human trials after showing the dangerous cardiac side effect of QT prolongation,[5] but is still widely used in animal research into H3 antagonists / inverse agonists." http://en.wikipedia.org/wiki/ABT-239

The vigilance promoting drug modafinil increases extracellular glutamate levels in the medial preoptic area and the posterior hypothalamus of the conscious rat: prevention by local GABAA receptor blockade.
http://www.ncbi.nlm....pubmed/10088135

And If you interested in learning more about ampakines a good book i recommend is this one:
http://www.amazon.co...09206093&sr=8-4

Edited by Ampa-omega, 27 June 2011 - 08:36 PM.

[Ampa-omega]

also as this study shows:
http://www.ncbi.nlm....les/PMC1573432/

more than one glutaminergic substance may need to be used together to be effective in glutaminergic signaling.

Edited by Ampa-omega, 27 June 2011 - 08:28 PM.

[David J Meneses R]

I'm testing Aniracetam in quantity of 2 to 4 grams, for 3 weeks. The brand is SmartPowers. My impressions are: Very hard taste, ugly. And I do not feel something special "Mind improvement or memory enhancement. I'm not sure if that was for the brand or because I have not problems with my mind, IQ 140. With Noopept for the same brand I feel something, but not a real improvement. Only more lucid dreams and visual impressions, Not memory, but I do feel like in my computer writing, my brain was faster than my hands, so, I make a loot of mistakes.

[Reformed-Redan]

I think Ampakines (AMPA agonists, PAM's) are limited by NMDA channels, which are the predominant gateways for glutamate neurotransmission in the brain AFAIK. You'd have more luck with NMDA agonists; but, its always tricky with glutamate. Nicotine receptors have shown real good nootropic potential.

[megatron]

I have lost all belief in ampakines after my own experiences with Aniracetam and Sunifiram, and ScienceGuy's trial with IDRA-21, which produced an unfortunate negative outcome. I strongly believe that this is not the way to go, if significant and permanent improvements in cognition is the goal.

Edited by Megatrone, 11 September 2013 - 04:02 PM.

[Nobility]

+rep guys,
keep them going, good job guys.

+rep.. more +rep for helpers !!! good posts +rep!!!