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why does oxiracetam have a "stimulant" effect?

A

Ampa-omega

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Apr 27, 2011
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this is another question of mine that i had but i think its very worthy of it's own thread

why does oxiracetam have a stimulant effect and aniracetam have a anxiolitic effect?
many users report that oxiracetam gives them some sort of an stimulant effect, which is quite strange because well i dont really know but oxiracetam is nmda selective and also has effect on acetylcholine in the brain..

on the other hand aniracetam has effect on 5htp, dopamine, and ampa receptors as well a7nicotinic receptors..which could explain its anxiolitic effect..

but oxiracetam sounds to me more of a productive nootropic than aniracetam, although aniracetam has that ampa receptor modulation it causes more states of "sleepiness" in comparison to oxiracetam (does anyone know how much higher aniracetam has an affinity for ampa receptors vs oxiracetam?)

can anyone explain this phenomenon?
 
The mechanism of action of many AMPAkines, and indeed binding affinities for a lot of receptors, are sparse and few between.

It's possible that aniracetam is just less selective for targets that produce a subjectively 'stimulating' experience.
 
Ampa-omega said:
can anyone explain this phenomenon?
Click to expand...

It isn't as mysterious as you may think. Drugs that have neutral/subtle effects tend to create a whole spectrum of subjective reactions in people. Just look at all the opinions on benzos.

For example: I personally found oxiracetam to be identical to Piracetam - ie. anxiogenic and depressing (suicidal). I did not find either to confer any cognitive enhanement. On the other hand I found nefiracetam and aniracetam great for cognitive enhancement and not as anxiogenic as the other two.

Also, I thought all 'racetams have basically the same mechanism of action, but different affinities? Anyone, please correct me if I'm wrong (I am actually wondering).
 
wow that is bizarre.

many user's responses have conflicting results.

im thinking they have a similar mechanism(you mean allosteric modulation?) but not the same, and yes different affinities.

by the way nice janus avatar.
 
aniracetam anxiolytic features are mediated by cholinergic, dopaminergic and serotonergic systems (nAChRs, 5-HT2A, dopamine D2 and D2-like receptors at least)
 
Oxiracetam's structure suggests it is at least partially metabolized to GABOB. GABOB is a GHB agonist and agonism at the GHB receptor produces stimulatory effects last I heard.

Incidentally, with respect to GABOB, I am aware it is available as a dietary supplement; however, I rather highly doubt that it crosses the blood-brain barrier due to its polarity. Oxiracetam looks like a reasonable prodrug with a much better chance of crossing the BBB.

Also, I thought all 'racetams have basically the same mechanism of action, but different affinities? Anyone, please correct me if I'm wrong (I am actually wondering).
Click to expand...

I think aniracetam may be distinct from the rest, solely because it has an imide linkage at N1 whereas all of the other racetams have an amide at N1; aniracetam has more in common with the ampakines than the other racetams as far as I can tell. The market availability of aniracetam has increased significantly recently and I'm hoping for a chance to try it.

The other racetams, without the imide linkage, seem to act via a novel AMPA allosteric site:

http://pubs.acs.org/doi/abs/10.1021/jm901905j

which is different from the previously-discovered aniracetam binding site.
 
Last edited:
atara said:
Oxiracetam's structure suggests it is at least partially metabolized to GABOB. GABOB is a GHB agonist and agonism at the GHB receptor produces stimulatory effects last I heard.

Oxiracetam looks like a reasonable prodrug with a much better chance of crossing the BBB.



I think aniracetam may be distinct from the rest, solely because it has an imide linkage at N1 whereas all of the other racetams have an amide at N1; aniracetam has more in common with the ampakines than the other racetams as far as I can tell. The market availability of aniracetam has increased significantly recently and I'm hoping for a chance to try it.

The other racetams, without the imide linkage, seem to act via a novel AMPA allosteric site:

http://pubs.acs.org/doi/abs/10.1021/jm901905j

which is different from the previously-discovered aniracetam binding site.
Click to expand...

yes the racetams have been noted to be slight derivatives of GABA.
where have you heard that ghb agonism causes stimulant effects? is that a similiar stimulant effect to say, caffeine?are you saying the oxiracetam is a downer, or an upper?
its worth noting that oxiracetam has been shown to increase gh levels, which could be explained by GABOB being a metabolic byproduct.

yes the benzoyl addition to aniracetam seems to give it the ampakine effects.

also if you look at this image sunifiram and aniracetam look the most related to the ampakines:
n2og0y.png
Cortex_pharm_AMPAkines.svg
 
Thats what allosteric positive modulators DO. Allosteric regulation has no effect if an orthosteric agonist is not bound. Not counting constitutive activation of course.
 
http://translate.google.co.uk/trans...rch?q=nefiracetam+testicles&hl=en&prmd=ivnsfd

Nefiracetam appears to inhibit testosterone synthesis, and also cause gross morphological changes, including atrophy, of the testicles, at least in the rat and dog.

Not something I would bother risking, certainly not when plenty of other, non-bollock shrinking racetams.


http://www.rt-pcr.com/showabstract.php?pmid=16007418 Report of renal damage in canines.


Nefiracetam seems pretty....iffy. I wouldn't reccomend taking it.
 
eh I had it a week w/o knowledge of this and still have
NSFW:
gigantic balls,
%) but this would be something to tell ppl with small ones.
 
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