• N&PD Moderators: Skorpio

CX717 and AMPAKINES

btw cx717 was first discovered in 1993...isn't any other pharmas pursuing this area and if so is there anything else that looks even more promising?
 
The first time I have used this compound I took about 300mg. It was a little bit exciting, the waiting for the action to take place. I have expected it to be similar to Modafinil, perhaps also because of the modulation of the glutamergic pathway. It is different, they may be some aspects these two share, but Modafinil is definately more promoting wakefullness and motivation, especially the last one may be caused through the involvation of the dopamine, which is not present in Ampalex so far as I know. Taking Modafinil, you feel clearly after 2 hours that you are "on" some psychic active agent. Ampalex is different here, after 1 hour of ingestion, one feels something taking place (you know what I mean, a change in your feeling, thoughts, for example when you feel hyperactive on coffein) but it is much more slight. Even with 600mg (the dose I use usually now) one does not feel "high" or strongly affected, the psychic sideffects are not so strong present as with other pharmaceuticals.

But there is a change, it is really difficult for me to describe it, I only can try. I can notice it when I am learning something or I have to understand correletions between some mechanism (for example in molecular biology etc.) to visualize the things I hear in the university or I read about. Sometimes the effect on the memory is very strong noticable, especially after learning for tests. The cognition is enhanced but not on the way it happens with modafinil (or higher dosages of modafinil). With modafinil one sometimes has a kind of thinking that is very concentrated, but it can dimnish the outside thinking, you focus on one way towards a solution and don`t see the others (as I sad difficult to describe), one would say that the phantasy is a little bit limited, if this is the right word for that. With Ampalex this is not the case, much more it may be helpfull to see other ways, to combine the learned informations and to see the links between issues. For me it was also interesting to notice, that the effect wasn`t very strong on the first day but it was on the second and stronger on the third one. I don`t know if this is caused by the growth factors or by some other mechanism.
Now I am using often a mixture of just a small ammount of modafinil (never more then 50mg, usually 30-40mg) and 600mg Ampalex. Sometimes adding green tee.
Modafinil gives me the state of totally wakefullness, which combined with the effects of Amaplex are simply great allowing one unbelievable concentration and allow an easier understanding and memorizing of the lectures.

I have tried many nootropics and although I know that here are enough enthusiasts who don`t want to hear this and will come up with the argument that I should not compare myself to all other people (what works for you won`t work for someone else and so on and on....) I have to say, that I have only used 2 or 3 that have ever worked.
Modafinil, Ampalex and perhaps green tee as addition to those 2. Everything else was totaly useless or even caused a state, where my abilities were more dimnished than enhanced. Perhaps are my claims higher, but the nootropic market is, as I have mentioned before a little bit absurd, giving nearly any psychological active agent the word "nootropic" as an attachment. So this is how I want to end this short report. You want me in the end to say if I think ampalex works.
And in my subjective opinion I can say: Yes, it does.
http://www.imminst.org/forum/index.php?s=&act=ST&f=169&t=14847&st=0

The tests with the military weren't so hot (CX717 didn't promote wakefulness any better than a cup of coffee). They don't sound all that interesting to me.

Acute Effects of the Ampakine Farampator on Memory and Information Processing in Healthy Elderly Volunteers

Ampakines act as positive allosteric modulators of AMPA-type glutamate receptors and facilitate hippocampal long-term potentiation (LTP), a mechanism associated with memory storage and consolidation. The present study investigated the acute effects of farampator, 1-(benzofurazan-5-ylcarbonyl) piperidine, on memory and information processes in healthy elderly volunteers. A double-blind, placebo-controlled, randomized, cross-over study was performed in 16 healthy, elderly volunteers (eight male, eight female; mean age 66.1, SD 4.5 years). All subjects received farampator (500 mg) and placebo. Testing took place 1 h after drug intake, which was around Tmax for farampator. Subjects performed tasks assessing episodic memory (wordlist learning and picture memory), working and short-term memory (N-back, symbol recall) and motor learning (maze task, pursuit rotor). Information processing was assessed with a tangled lines task, the symbol digit substitution test (SDST) and the continuous trail making test (CTMT). Farampator (500 mg) unequivocally improved short-term memory but appeared to impair episodic memory. Furthermore, it tended to decrease the number of switching errors in the CTMT. Drug-induced side effects (SEs) included headache, somnolence and nausea. Subjects with SEs had significantly higher plasma levels of farampator than subjects without SEs. Additional analyses revealed that in the farampator condition the group without SEs showed a significantly superior memory performance relative to the group with SEs. The positive results on short-term memory and the favorable trends in the trail making test (CTMT) are interesting in view of the development of ampakines in the treatment of Alzheimer's disease and schizophrenia.
http://www.nature.com/npp/journal/v32/n6/abs/1301257a.html

Farampator is 1-(benzofurazan-5-ylcarbonyl) piperidine, the synth is listed in this patent: http://www.freepatentsonline.com/6730677.html
 
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yes, that thread re-inaugurated my interst

i have seen faramptor and some others but nothing that looks promising moreso than Ampalex or CX717

there are a few studies that i do not have full text acces to though that hint at possible AMPAKINES of a noteworthy nature
 
Check that patent again

As the data in Table 1 show, the present compounds produced a dose-dependent increase in the amplitude of the EPSP and were effective at concentrations as low as 3 uM. The majority of the tested compounds were equally or more effective, up to a factor of about fifty, than the reference compound, CX516, in increasing AMPA receptor function. Compounds 2, 4, and 6-9 were particularly effective.
 
no, that;s the point, these are IMO functional enhancement compounds

either to restore normalcy or above in those with conditions that impede energy, focus, et al, or to create a supraphysiological energy and focus in normal individuals without risk of undue sides (in general), tolerance, and addictive potential (if used responsibly)
 
oh, and while i can not say for a fact there likely is some recreational potential at very high doses, but not optimal and worthwhile in comparison to other agents more known for such...
 
looking at that patent again (thank you, nuke) i believe it shows the compound 1-(Benzofurazan-5-ylcarbonyl)-4-cyanopiperidine (8) to be about 50-fold as potent at AMPA agonism as CX516 and likely as with Compound 2 would be able to express improved cognition and function at doses perhaps 50-100x lesser than needed with CX516
 
ampakines sound like garbage to me, so do the racetams. i thought it's bad to have the glutaminergic stimulated>doesn't it cause cell death/seizures and what not, guess not is small controlled doses, so i guess taking hi doses of an ampakine is bad, much like taking ampa itself. it's weird that they develope an agonist as an alzheimers drug as memantine is an antagonist or atleast at nmda but i think most(but not all) nmda antagonists also antagonize ampa(i could be wrong) but they both share many similar attributes

I would be more intersted in an ampa blocker, i know vincamine/vinpocetin are... but a full blocker would be better
 
A glutaminergic agonist would be excitotoxic, yes.
However, these AMPA drugs are positive modulators, not direct agonists.
 
On the same note ,does aniracetam share any of ampakine features here,that is having any affinity for AMPA receptors? (Meaning mostly allosteric modulation,not direct)
 
wikipedia has some interesting stuff on CX717 under the "discussion" tab [referring to it's structure]
 
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