38 replies to this topic

[jackinbox]

There is very little information on some racetams:

http://en.wikipedia.org/wiki/Racetam

Nefiracetam is probably not too hard to get but the testicules scare doesn't help to popularize it. Some doesn't look to be nootropic (like Levetiracetam and Seletracetam) and others seems to have potential, like Rolziracetam, Nebracetam. Anyone has more information on those two racetams? Effect, side-effect, availability?

[spacey]

Yeah I've been wondering about them too, although there seems to be a bit too little information.

[awarren]

I'm sorry I can't be more specific, but the most I know is that a lot of these racetams are used for epilepsy treatment.

[Ben]

You guys are gonna love this! The definitive document on the entire Racetam family, obscures included!

Nice find! 5 stars for you!

[jackinbox]

Thanks Iso. All we need now is a chemist and some guinea pigs It's not a complete list. Those are missing:
Etiracetam
Phenylpiracetam
Nefiracetam
Rolziracetam
Coluracetam
Brivaracetam
Seletracetam
Rolipram

Of course, they are not all nootropics.

[StrangeAeons]

Levitiracetam is also known as Keppra and I've seen it used in the hospital for seizure patients; from what I understand it's fast replacing Dilantin for seizure control, which is a good thing; until recently we've just been trying to use GABA agonists to control them.

[425runner]

The definitive document on Sunifiram and Unifiram was found last night! The full PDF too, not some weak abstract...

Summary: Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancers

Full PDF available here: Pharmacological Characterization of DM232 (Unifiram) and DM235 (Sunifiram), New Potent Cognition Enhancers

Wow! That's great info - thanks for sharing! Finally some scientific facts not just anecdotal evidence lol.

[Pike]

oh my. how exciting! unfortunately, since it seems to be so effective, it will probably never hit the public nootropics markets.

[catfanatic1979]

I honestly wish we could get ahold of some of this stuff.

[kismet]

One would think there's a reason why they *remained* obscure. But, no... not on this sub-forum.

[kilgoretrout]

One would think there's a reason why they *remained* obscure.

Yea, mutant scientists with no eyelids muttering secret hyper-languages wearing wierd silver spandex jump-suits with big giant malformed alien-like craniums kept locked up shuffling strangely about secret government labs who are trying desperately to keep all the really good stuff to themselves, OBVIOUSLY!!!

Edited by kilgoretrout, 27 August 2009 - 09:18 PM.

[NG_F]

Does anyone know of a quality reliable source for Nefiracetam? It's currently in phase 2 trials to be used as a drug for abulia/apathy in strokes,alzheimers and other Neurodegenerative conditions.

I have a particular interest as I have a lesion which the neuro's are attributing most likely to a small stroke in the anterior portion of the head of the left Caudate area in the basal ganglia.

Needless to say my quality of life has been going downhill in the last 2 years.

Any suggestions for the Nef or other supps that may help would greatly be appreciated.

Thanks in advance.

[Pike]

http://teamliferesea...;products_id=35

this is currently the only nefiractam vendor that I know of. It's beyond expensive... $90 for 20 grams of powder.

[StrangeAeons]

I'm not an expert, but per my understanding nef has fallen out of favor because it can cause toxicity to the testicles of some sort. A Google search revealed the company trying to market it for this indication, though. Obviously in your case there's a fair amount of risk:benefit calculations going on, so I would recommend trying to enroll in a clinical trial.
In lieu of that I would at least try pharmaceutical-grade piracetam first; it's amply cheaper, safer, and easier to acquire and may yield similar benefit.

[skinniest200]

oh my. how exciting! unfortunately, since it seems to be so effective, it will probably never hit the public nootropics markets.

I honestly wish we could get ahold of some of this stuff.

Everything is available in bulk, nobody is interested enough to take the risk. Sources can probably be found in 5 minutes.

[yowza]

oh my. how exciting! unfortunately, since it seems to be so effective, it will probably never hit the public nootropics markets.

I honestly wish we could get ahold of some of this stuff.

Everything is available in bulk, nobody is interested enough to take the risk. Sources can probably be found in 5 minutes.

Money is a limiting factor too. This stuff is kind of expensive. I'd definitely be willing to order some if I had the income.

Good point though about this stuff being available in bulk.

[425runner]

At 1000x potency, a pound synthesized would be millions of doses. Just a matter of raising the funds to get a minimum production quantity made.

right...good point. In this economy it's hard to justify spending $100s on exotic nootropics.

[skinniest200]

Did anybody read this post from 1fast400?

http://forums.1fast4.../topic2181.html

All right... time for a reality check.

The reasons I don't think offering sunifiram would be a good idea:

1. It is no doubt patented, and since it is a new pharmaceutical, there is a high likelihood that any company that tries to sell it would get sued ASAP.

2. Potency does not necessarily correlate with maximal activity. Racetam nootropics tend to have bell-shaped dose-response curves. So the question you want answered is not how potent a compound is, but how strong the effect is at the dose which has the maximal effect. For example, some steroids that are considerably more potent on an mg per mg basis are much less desirable in terms of effects. Accordingly, here is a quote from one of the sunifiram studies:

The maximal antiamnesic effect of DM235 was obtained with the dose of 0.001 mg kg–1 i.p. and maintained up to 0.1 mg kg–1 i.p. The DM235-induced antiamnesic effect was of the same intensity as that exerted by the well-known nootropic drugs piracetam (30 mg kg–1 i.p.), aniracetam (100 mg kg–1 p.o.) or rolipram (30 mg kg–1 p.o.) (Fig. 2A and )

3. There are no human studies on this compound. So we know nothing about the toxicity, side effects, or pharmacokinetics in humans. I agree that it is promising, but self-experimentation with drugs like this - especially ones with an active dose of 1 mcg/kg - is dangerous. Not only that, but with a bell-shaped dose response curve, you have to hit a very narrow dosage range to achieve an effect, which is much more difficult if the doses are miniscule. It is possible that even a fraction of a milligram too much could make it so it had no nootropic effect at all.

If it's really the same intensity of effect as the common racetams, only using a lower dose, then it's not that interesting to me. Sources were found though, in case somebody else is interested.

[Ichoose2live]

For those who are curious, I have collected all the studies of Nebracetam and I have copied and pasted their results.

Nebracetam was first synthesized in Germany, probably around the year 1988. It has stronger general effects than Piracetam but weaker central cholinergics effects than those of directly acting cholinergics agents. No side effects are observed. [1]

RESULTS SUMMARY:
Nebracetam increases the noradrenaline and dopamine and turnover in the forebrain and brain stem. Nebracetam act as an antidepressant suggested that this action is--at least partly--mediated by the central noradrenaline system. [2]

Nebracetam increases alpha-wave mainly in the frontal area at high frequency (above 9.5 Hz) and an associated decrease of slow-wave and of fast-wave. This suggests that Nebracetam might activate linguistic learning and memory process in normal subjects. [3]

Nebracetam has a tyramine-like, catecholamine releasing property. Although a large dose of Nebracetam has a direct cardiac depressant action, it does not affect muscarinic mechanisms in the heart. [4]

The affinity order of Nebracetam was: M1-muscarinic (m) ACh receptor greater than M2-mACh receptor greater than alpha 2-adrenoceptor greater than beta-adrenoceptor greater than alpha 1-adrenoceptor greater than nicotinic ACh receptor. Nebracetam seems to act on M1-mACh receptors, and its long-term administration probably induces the down-regulation of mACh receptors, mainly M1-mACh receptors in the hippocampus and striatum and M2-mACh receptors in the cerebellum. [5]

Nebracetam significantly protected and reduce the rate of neuronal loss against impairment of the striatal responses under the conditions of hypoglycemia. Nebracetam exert neuroprotective actions against hypoglycemic/hypoxic brain injury by activating energy metabolism. [6]

Nebracetam has a beneficial effect on memory that has been impaired by scopolamine or by cerebral ischemia. [7]

Nebracetam induced a rise of [Ca2+]i in the medium with 1 mM Ca2+ and without Ca2+ (plus 1 mM EGTA). Nebracetam seems to act as an agonist for human M1-muscarinic receptors. [8]

Nebracetam facilitates the ganglionic muscarinic transmission through acting on presynaptic sites. [9]

Nebracetam may have protective actions on the destruction of hippocampal cholingergic neurons as well as memory impairment induced by AF64A administration. [10]

The cognitive enhancing effect of nebracetam involves not only cholinergic mechanisms but also involves lymbic and hippocampal noradrenergic mechanisms. [11]

Nebracetam exert neuroprotective actions against not only ischemia but also glutamate toxicity. [12]

Nebracetam (10(-5) and 10(-4) M) completely protected against striatal dopaminergic impairment induced by L-glutamate and NMDA, respectively. Therefore, nebracetam seems to produce a neuroprotective action by interacting, at least in part, with NMDA receptor-operated Ca2+ channels. [13]

It is suggested that the direct effects of nebracetam on nAChRs and mAChRS, which were induced only by a rather high concentration, as compared with the clinically expected plasma level, may be a contributing factor to the clinical effectiveness of the drug only if there is some critical change in the sensitivity to the drug. [14]


Of several neurotransmitter-related substances measured in the CSF, a marked rise of AChE activity was observed. It is suggested that the mechanisms of action of Nebracetam are based on its transit into the CSF as well as the activation of intracerebral acetylcholinergic systems. [15]

Nebracetam enhances acetylcholine release from presynaptic sites of dog stellate ganglia not by blocking presynaptic M2 muscarinic autoreceptors but by accelerating acetylcholine formation, and by increasing choline uptake when acetylcholine is depleted. [16]

In cultured cerebellar granule cells, nebracetam attenuates the external Ca2+ influx derived from the activation of N-methyl-D-aspartate receptor-gated rather than voltage-gated Ca2+ channels. [17]

Nebracetam protects against ischemic delayed neuronal cell death in the hippocampus. [18]

Nebracetam is a possible therapeutic agent for the restoration of cerebral energy metabolism against microsphere-induced, sustained cerebral ischemia. [19]

It is unlikely that Nebracetam at a pharmacologically effective dose alters dopamine or serotonin uptake in the brain nerve terminal under normal conditions. [20]

There are evidence for a possible action of nebracetam on 5-HT metabolism in the ischaemic brain. [21]

Cultured astrocytes treated with either nebracetam or piracetam showed decreased intracellular ATP and PCr levels. The addition of nebracetam and dBcAMP to cultures caused an increase of PCr content in astrocytes. The astrocytes treated with nebracetam showed a decrease in 3H-valine incorporation. Nootropic drugs change morphometric parameters (cell area, perimeter and form factor) of cultured astrocytes. It can be concluded that nootropics have differentiated influence on both the energetic metabolism and morphology of rat astrocytes in vitro. [22]

We can clearly see the lack of medical study in human (about two studies?). Futhermore, the study [5] doesn't seem to be very positive for a long-term usage of Nebracetam.

Edited by Ichoose2live, 05 March 2011 - 02:25 AM.

[CIMN]

I've been interested in nebracetam,thanks for that.

i wonder why the other racetam drugs aren't produced as much as the common few seen around, why is that?

Edited by CIMN, 21 August 2012 - 08:22 PM.

[renfr]

I've been interested in nebracetam,thanks for that.

i wonder why the other racetam drugs aren't produced as much as the common few seen around, why is that?

Because they're not researched enough. Studies are very scarce and who knows if those racetams are toxic or not whether on short-term or long-term use.
For instance nefiracetam is killer for your testicles and pramiracetam can cause extreme glutamate excitotoxicity and NOS damage at high doses. As for other racetams such as piracetam, aniracetam or oxiracetam they have been more studied and are considered as very safe.
Oxiracetam could be an exception on the long-term as it can cause stress and calcium damage on stressed individuals or at high doses and stress is known to be a factor of cell death.
I guess if you really want to try out those dark racetams, you will probably find a supplier on Alibaba or ask a lab to synthetize the molecule.

[CIMN]

I've been interested in nebracetam,thanks for that.

i wonder why the other racetam drugs aren't produced as much as the common few seen around, why is that?

Because they're not researched enough. Studies are very scarce and who knows if those racetams are toxic or not whether on short-term or long-term use.
For instance nefiracetam is killer for your testicles and pramiracetam can cause extreme glutamate excitotoxicity and NOS damage at high doses. As for other racetams such as piracetam, aniracetam or oxiracetam they have been more studied and are considered as very safe.
Oxiracetam could be an exception on the long-term as it can cause stress and calcium damage on stressed individuals or at high doses and stress is known to be a factor of cell death.
I guess if you really want to try out those dark racetams, you will probably find a supplier on Alibaba or ask a lab to synthetize the molecule.

Really? If your concerns are as true and dramatic as they sound then you should probably alert the rest of this forum by making a thread and sharing the references to what you have read on that. many people still use oxiracetam and pramiracetam here. can you link to the exact study you are referring to on oxiracetam?

Edited by CIMN, 22 August 2012 - 04:52 AM.

[renfr]

I've been interested in nebracetam,thanks for that.

i wonder why the other racetam drugs aren't produced as much as the common few seen around, why is that?

Because they're not researched enough. Studies are very scarce and who knows if those racetams are toxic or not whether on short-term or long-term use.
For instance nefiracetam is killer for your testicles and pramiracetam can cause extreme glutamate excitotoxicity and NOS damage at high doses. As for other racetams such as piracetam, aniracetam or oxiracetam they have been more studied and are considered as very safe.
Oxiracetam could be an exception on the long-term as it can cause stress and calcium damage on stressed individuals or at high doses and stress is known to be a factor of cell death.
I guess if you really want to try out those dark racetams, you will probably find a supplier on Alibaba or ask a lab to synthetize the molecule.

Really? If your concerns are as true and dramatic as they sound then you should probably alert the rest of this forum by making a thread and sharing the references to what you have read on that. many people still use oxiracetam and pramiracetam here. can you link to the exact study you are referring to on oxiracetam?

Yes oxiracetam and pramiracetam have reached a certain popularity on this forum but users typically get benefits from their use as the dosages are relatively low.
However, oxiracetam and pramiracetam stll have caused fatalities, the case of 1 user who took 12g of oxiracetam (huuuuuuuuuuuuuge dose) and kept in mind all his chemistry courses for exams and the day of the exams, he happened to have severe cognitive impairement and didn't remember a single thing.
I could also add myself in the fatalities, as I also experienced such effects from doses as low as 2g, this effect is likely due to calcium channel flows that trigger biological stress.
Some people might use high dosages of oxiracetam and experience nothing but benefits, I envy them, but other users might be more sensitive. I never saw someone getting extreme cognitive damage from oxiracetam, it's relatively safe but if you know such dosages trigger biological stress, you'd be careful as this is harmful for your neurons.
A fix to that is obviously lowering intake and possibly supplementing magnesium.

As for pramiracetam, it however caused more serious issues to one user who only took 1000mg, which is over the 100mg dosage recommended by most suppliers but still far away from the human dose supposed NOS damage that is around 5000mg and even more away from users who megadosed up to 11g.
The user was probably one of the harshest fatalities there, total cognitive impairement,his memory became poor and didn't improve and his cognitive skills sharply decreased. So yes again, this is a matter of sensitivity and one should always try low dosage and if needed under RDA to prevent massive damage in case of toxicity issues.

Last but not least, even some report that piracetam was harmful to them, you can look at Nootropix from Thailand who claims to have suffered damage from piracetam use, I don't know which dosage he did use but piracetam is like most of racetams a double faced molecule, for some they get depressed when using it, for others it relieves their mood. For Nootropix it makes him depressed, as for me it rather uplifts my mood.

Of course I can't check for veracity of user claims and tell you if what they say is true, however I and many other users read their posts and I find them enough serious to think it did happen.
There are probably people there who wants to get rid of racetams and disprove them, those liars such as the nootropic rookie who claim taking ultra mega dosages and then get brain lesions. First of all it's not surprising at all that those crazy dosages cause damage and second if it did cause damage that fool wouldn't use the same mega dosage for months straight.