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Coluracetam

Coluracetam

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228 replies to this topic

#1 computeTHIS

  • Location:US

Posted 05 October 2011 - 04:23 AM


I know there are plenty of other obscure racetams, but this one caught my interest being a "choline uptake enhancer" and having the potential to restore optic nerve damage: en.wikipedia.org/wiki/Coluracetam

This sounds amazing to me, is anyone familiar with this one? Oddly enough, Google-ing it pulls up a bunch of chemical suppliers.
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#2 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 05 October 2011 - 04:29 AM

ive also been looking the obscure racetams,

you could buy this from alibaba i think.

anyways why is it that only 4 racetams (pira,ani,oxi,prami) are usually sold and the others not? can someone explain that to me
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#3 Cephalon Re: Coluracetam

  • Location:Cologne

Posted 05 October 2011 - 04:52 AM

Isn't plain Piracetam a choline uptake enhancer as well? That's the reason you might get headaches if not combining it with a choline source.
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#4 computeTHIS Re: Coluracetam

  • Location:US

Posted 05 October 2011 - 04:55 AM

Coluracetam (1996):

The pharmacological properties of MKC-231 (2-(2-oxopyrrolidin-1-yl)-N- (2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl) acetoamide, CAS 135463-81-9) in comparison with an acetylcholinesterase (AChE) inhibitor, tacrine (CAS 1684-40-8) were studied. MKC-231(10(-10)-10(-6) moll) significantly increased high affinity choline uptake (HACU) when it was incubated with the hippocampal synaptosomes of ethylcholine mustard aziridinium ion (AF64A) treated rats, but not of normal rats. MKC-231 did not affect the AChE activity, [3H]- quinuclidinyl benzilate binding, and [3H]-pirenzepine binding. Oral administration of MKC-231 (1-10 mg/kg) significantly improved the learning deficits in the Morris' water maze of AF64A-treated rats, but it did not produce any significant side effects, like tremor, salivation or hypothermia, which were observed in rats treated with high doses of tacrine. Tacrine (0.1-3 mg/kg p.o.) failed to ameliorate the learning deficits in AF64A-treated rats. These results suggest that MKC-231 is a novel and quite unique compound, which improves the memory impairment induced by AF64A through the enhancement of HACU without any side effects at the effective doses.
PMID: 8740080 [PubMed - indexed for MEDLINE]


→ source (external link)

Edited by computeTHIS, 05 October 2011 - 04:59 AM.

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#5 computeTHIS Re: Coluracetam

  • Location:US

Posted 05 October 2011 - 04:57 AM

Also: braincellsinc.com/pipeline/bci-540

From the link, (BCI-540 aka Coluracetam)

Favorable Profile

BrainCells identified and selected BCI-540 to develop because of its favorable neurogenic profile similar to antidepressants available on the market today. In addition, BCI-540 appears to act as an AMPA potentiator as well as enhance choline uptake, providing a unique profile that may be optimal for the treatment of both depression and anxiety – an area with a strong market need.
Because it benefits from a novel mechanism that does not act on serotonin or norepinephrine receptors, BCI-540 has the potential to treat unresponsive and partially responsive patients with depression, especially in those patients that present with concomitant anxiety. In addition, potential improvements in safety and tolerability may help further differentiate this drug candidate from SSRIs and SNRIs.
Identified in a Different Indication

BrainCells in-licensed BCI-540 from Mitsubishi Pharmaceutical Corporation in August 2006 and is currently developing it for the treatment of patients with Major Depressive Disorder (MDD) and anxiety. Mitsubishi Pharma had previously developed the compound extensively in a different CNS indication, then suspended the program when the drug met safety expectations but did not reach the defined efficacy endpoints. BrainCells has repositioned the drug and has completed an exploratory Phase 2a study in depression with anxiety.
Clinical Results

Results from the Phase 2a trial suggest BCI-540 has the potential to treat a difficult-to-treat population, people with MDD who have failed previous treatments, and have a co-morbid anxiety disorder. Read press release.»


Edited by computeTHIS, 05 October 2011 - 05:02 AM.

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#6 computeTHIS Re: Coluracetam

  • Location:US

Posted 05 October 2011 - 05:44 AM

anyways why is it that only 4 racetams (pira,ani,oxi,prami) are usually sold and the others not? can someone explain that to me

Some of them have little nootropic/medicinal value at all. Did you read about Nefiracetam? It's like the one you take when you want your nads to shrivel up and fall off. I think the others just haven't been researched enough to safely sell them.

Isn't plain Piracetam a choline uptake enhancer as well? That's the reason you might get headaches if not combining it with a choline source.

I was under the impression it was an AChE inhibitor.

Edited by computeTHIS, 05 October 2011 - 05:45 AM.

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#7 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 05 October 2011 - 07:53 AM


anyways why is it that only 4 racetams (pira,ani,oxi,prami) are usually sold and the others not? can someone explain that to me

Some of them have little nootropic/medicinal value at all. Did you read about Nefiracetam? It's like the one you take when you want your nads to shrivel up and fall off. I think the others just haven't been researched enough to safely sell them.

Isn't plain Piracetam a choline uptake enhancer as well? That's the reason you might get headaches if not combining it with a choline source.

I was under the impression it was an AChE inhibitor.


i think nefir works it just needs the right dose figured out, its sort of in a similiar situation prami was.
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#8 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 05 October 2011 - 04:41 PM

i still wonder though who controls this racetams market, it doesn't seem to be regulated by anyone.. so why is there only 4 recatams, i don't see there being any consortium and discussion making these the choice. The market seems more random and distributers just follow along.

anyways.. coluracetam does seem overlooked if it can regenerate ocular nerves, and potentiate ampa receptors.. and would combine nicely with nefiracetam (nefiracetam helps potentiate glutamatergic currents),
which begs the question why it isnt seen more around? Is it just overlooked and underfunded? its even more interesting that its composition has a quinolin group, that might bring some interesting property.

Edited by Ampa-omega, 05 October 2011 - 04:42 PM.

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#9 Introspecta Re: Coluracetam

  • Location:Massachusetts U.S

Posted 05 October 2011 - 04:51 PM

People are afraid to use Nefiracetam due to the dog study of it lowering testosterone and shrinking the nuts. I tried Nefi and personally it made me so numb, and partially depressed due to how numb i was that i couldn't take it. It did make me focus and sometimes felt very calm, but then all of a sudden i'd be anxious. It was very unstable and not a good experience for me.
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#10 computeTHIS Re: Coluracetam

  • Location:US

Posted 05 October 2011 - 04:58 PM

From the previously linked press release:

SAN DIEGO, Calif., June 14, 2010 – BrainCells Inc., a company leading the scientific research
of neurogenesis using its proprietary neural stem cell platform technology to identify novel
compounds for the treatment of central nervous system (CNS) diseases, announced today
findings from an exploratory, dose ranging Phase 2a clinical trial not powered for statistical
significance. The trial evaluated BCI-540 for the treatment of patients with major depressive
disorder (MDD) with anxiety who had previously failed an average of two antidepressants. While
there was no difference between the overall treatment group and placebo on scales for
depression and anxiety, further analysis showed a positive efficacy signal in a subset of patients
with MDD and general anxiety disorder (GAD), which warrants further study.

“Co-morbid depression and anxiety remains a significant unmet need, representing
approximately 40 percent of depressed patients. BCI-540 elicited a stronger response in this
group of patients, providing us direction for additional studies to better understand its
therapeutic potential,” said Allan Young, MB, ChB, Ph.D., FRCPsych, FRCPC, director of the
Institute of Mental Health at the University of British Columbia and lead investigator of the trial. “I
look forward to its next step in development.”

The six-week trial was randomized, double-blind and placebo-controlled to determine whether
80 milligrams of BCI-540 dosed orally once or three times daily (TID) improves symptoms in
patients with MDD and anxiety who had previously failed an average of two antidepressants.
The trial measured change from baseline at week two, four and six for 101 evaluable patients
with a variety of commonly used patient and physician-rated scales including the Hamilton
Rating Scales for Anxiety (HAM-A) and Depression (HAM-D).

At week six, in the overall population there was no benefit of BCI-540 on HAM-A or HAM-D
compared to placebo. However, in patients who were dosed TID, 36% responded compared to
19% in the placebo group. Within this group, depression symptoms of those with co-morbid
GAD improved by 12.2 points on HAM-D compared to 5.5 points in the placebo group
(p<0.008). BCI-540 was well tolerated, with a side effect profile similar to placebo.

“Neurogenesis is an exciting new field that is demonstrating potential in many different CNS
diseases including depression and anxiety,” said Carrolee Barlow, M.D., Ph.D., chief scientific
and medical officer at BrainCells. “BCI-540 began to separate from placebo by four weeks,
which is in line with our understanding of how neurogenesis progresses in the brain. It is an
important clinical finding that we’ll take forward as we investigate the therapeutic opportunity of
BCI-540 in this difficult-to-treat population.”

BCI-540 is a bifunctional molecule that works to treat mood disorders through two mechanisms
of action, AMPA potentiation and choline uptake enhancement. BrainCells identified through its
platform the compound’s ability to help new neurons differentiate and survive, two important
aspects of the neurogenesis process. Experiments conducted by BrainCells confirmed
appropriate changes in behavioral models for depression, without affecting serotonin levels,
potentially eliminating side effects typically associated with selective serotonin reuptake
inhibitors (SSRIs) like Prozac. Currently, only 30 to 40 percent of people with depression fully
respond to current treatments.


That sounds awesome.
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#11 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 05 October 2011 - 05:04 PM

People are afraid to use Nefiracetam due to the dog study of it lowering testosterone and shrinking the nuts. I tried Nefi and personally it made me so numb, and partially depressed due to how numb i was that i couldn't take it. It did make me focus and sometimes felt very calm, but then all of a sudden i'd be anxious. It was very unstable and not a good experience for me.


What dose were you taking?
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#12 Dirk_Diggler Re: Coluracetam

  • Location:USA

Posted 05 October 2011 - 05:39 PM

anyways why is it that only 4 racetams (pira,ani,oxi,prami) are usually sold and the others not? can someone explain that to me


Because those are the ones that have been studied the most. When you take something that has little human studies, you are really taking a huge risk.

BTW, nefiracetam just sounds like it would do something that would make your nuts fall off. Nefiracetam? Everytime I hear that I just think of Nosferatu for some reason...
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#13 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 05 October 2011 - 05:45 PM

but why are they the ones studied the most?

There is even a huge discrepancy in the amount of studies with piracetam compared to the other 3 racetams of the common 4. Going by that logic they would be deemed a lot less 'safer' then piracetam. But again just because something is studied more doesn't mean it is safer or more effective, it is likely to be more, with more evaluation, but that primarily comes done to the quality of the studies. anyway i still advocate protective caution and do your research.

Edited by Ampa-omega, 05 October 2011 - 06:26 PM.

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#14 manic_racetam Re: Coluracetam

  • Location:USA

Posted 05 October 2011 - 06:38 PM

*
POPULAR


anyways why is it that only 4 racetams (pira,ani,oxi,prami) are usually sold and the others not? can someone explain that to me


Because those are the ones that have been studied the most. When you take something that has little human studies, you are really taking a huge risk.

BTW, nefiracetam just sounds like it would do something that would make your nuts fall off. Nefiracetam? Everytime I hear that I just think of Nosferatu for some reason...


The sound of nefiracetam has always reminded me of death a little bit. I'm guessing because it contains similar sounds as necrosis or necrophilia? Yeah, maybe it's more indicative of personal subconscious states... whatever ;)

I had a detailed post about nefiracetam written when my browser crashed.... but I may as well rewrite it since there's all this speculation going on. I think ignorance and fear is the main reason that keeps people from considering the benefits of nefiracetam.

First of all I disagree with correlating toxicity studies done on dogs with humans. Mainly because there are quite a few commonly ingested substances that have highly toxic reactions on dogs. Coffee and chocolate cause kidney damage in canines right?

Anyway, the human equivalent for the lower oral dosages from the dog study would be a little over 7,000mg / day. (180mg/kg for 8kg dog is about 7,300mg for 70kg human) You can use this allometric scaling calculator to make these conversions from animal to human dosages even if you don't understand it, just fill in the blanks. (I hope I did that right)

Phase 2b human trials with nefiracetam are currently being conducted by Neuren Pharmaceuticals, marketed as Motiva for post stroke apathy at dosages up to 900mg.

There is potential for nefiracetam as a treatment for addiction as well. I noticed the benefits while experimenting personally and I think it may have something to do with the cAMP related activity per this study which stopped self administration of morphine and methamphetamine in rats.

I found an effective dose at 150mg three times per day. If you want more detailed report you can see my other post, or for very thorough speculative toxicity research, and some interesting studies on nefi's nicotinergic mechanisms by Chrono go here.
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#15 computeTHIS Re: Coluracetam

  • Location:US

Posted 05 October 2011 - 07:09 PM

What are the best avenues at finding Coluracetam? Would anyone have an interest in splitting an order of it?
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#16 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 05 October 2011 - 07:21 PM

i am interested, i can't pitch in at the moment but maybe in your next order i can if you will order a second time.
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#17 manic_racetam Re: Coluracetam

  • Location:USA

Posted 05 October 2011 - 09:36 PM

What are the best avenues at finding Coluracetam? Would anyone have an interest in splitting an order of it?


It's hard to say no to a promising novel racetam. This one (coluracetam) sounds really interesting.

I'd be interested but so far all suppliers I've found are in China, and the two available companies seem to have a one-star reputation.
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#18 computeTHIS Re: Coluracetam

  • Location:US

Posted 06 October 2011 - 03:55 AM

I found 10 suppliers, all in China, which I've submitted quote requests to. We'll see what happens.
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#19 manic_racetam Re: Coluracetam

  • Location:USA

Posted 06 October 2011 - 04:43 AM

Sweet. Keep us posted
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#20 AbolishtheState Re: Coluracetam

  • Location:Springfield, OH

Posted 16 October 2011 - 09:41 AM

I found 10 suppliers, all in China, which I've submitted quote requests to. We'll see what happens.


Have you had any luck, yet? I would also be interested in experimenting with this racetam. If we are all able to get our hands on some, it would be really interesting to do an informal group study. Since this substance is relatively new and these forums have little information about it, such a study would help to jump start interest and reassure those who find themselves interested. Perhaps, leading to more demand and eventually a better supply. Establishing basic information such as dosing best practices, possible dangers or side effects, expected benefits, and synergy with other substances would go a long way toward creating a market for this novel noot--assuming the results are positive.
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#21 computeTHIS Re: Coluracetam

  • Location:US

Posted 17 October 2011 - 05:43 AM

Unfortunately, only 4 of them responded and only 2 of them are producing it. One is $1322/10g and the other is $800/5g. I haven't located custom chemical manufacturers in the US, but I'm thinking the only other option would be to find college or University faculty who might have an interest in producing it. I was able to locate the chemical synthesis sheets if they might be of interest.

What do you think?
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#22 QuantumTubule Re: Coluracetam

  • Location:earth

Posted 17 October 2011 - 07:06 AM

Post the chemical synthesis reports they will be useful to some
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#23 computeTHIS Re: Coluracetam

  • Location:US

Posted 17 October 2011 - 08:47 PM

Here's the paper I found (attached), this is likely what the Chinese manufacturers are using for their reference. The version without Chinese annotations is inaccessible due to copyright.

I think it's notable that while clinical trials seem to indicate it's very well tolerated, it proved to be a dead end for Alzheimer's treatment. Meaning that this one is likely less potent in neurogenesis than some other options, such as Ladostigil. Still, I'm incredibly intrigued by something with the potential to heal optic nerve damage.

Attached Files


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#24 manic_racetam Re: Coluracetam

  • Location:USA

Posted 20 October 2011 - 09:07 PM

The one company in China that responded from alibaba contacted me asking what quantities I was interested in. I said I'd like 10g's first and after laboratory results I'd need a kilogram. They never responded, which raises suspicions about their product (as far as purity and if genuine or not).

Another company in Cameroon with no buyer feedback quoted a 50g sample at $240USD. Don't know about you guys but I don't think I'm willing to take that risk.

Unrelated note: Plenty of Chinese suppliers offering 1kg of adrafinil for 600 bucks. If I liked the effects of that one more I'd be tempted.
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#25 computeTHIS Re: Coluracetam

  • Location:US

Posted 21 October 2011 - 02:29 AM

The one company in China that responded from alibaba contacted me asking what quantities I was interested in. I said I'd like 10g's first and after laboratory results I'd need a kilogram. They never responded, which raises suspicions about their product (as far as purity and if genuine or not).


I submitted a quote request to them for 1kg and they never responded to me.

Another company in Cameroon with no buyer feedback quoted a 50g sample at $240USD. Don't know about you guys but I don't think I'm willing to take that risk.


Can they offer a purity report for it as well? I vaguely recall some people here finding labs to perform purity checks. The combined cost of product+purity-check may be worthwhile here. If it checks out, I would inquire if 1kg quantities may be even cheaper.

The Chinese manufacturer quoting me $1322/10g also included a purity report in their reply. It seems to me that this is the only manufacturer who's been frequently supplying it. I would contact university faculty about producing it for experimentation but it won't be until November/December until I get the time to pursue that line of inquiry.
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#26 computeTHIS Re: Coluracetam

  • Location:US

Posted 14 December 2011 - 11:18 AM

It just occurred to me that BrainCells Inc is trying to out-licence Coluracetam for the treatment of co-morbid depression and anxiety. (http://www.braincell...ipeline/bci-540). Does this mean they're trying to get a company to bring it to market? Their clinical trials were concluded in June of last year, I wonder what the hold-up is on getting this to market.
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#27 Ark Re: Coluracetam

  • Location:Kent Washington

Posted 20 December 2011 - 12:25 AM

Bump on a early next year bulk order, who wants this??
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#28 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 20 December 2011 - 12:48 AM

if we can get a good source then i think people may be willing to try this out
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#29 Ark Re: Coluracetam

  • Location:Kent Washington

Posted 20 December 2011 - 01:59 AM

Hint Hint CerebralHealth.com aka Synaspe?~
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#30 Ampa-omega Re: Coluracetam

  • Location:united states

Posted 20 December 2011 - 05:33 AM

why dont you contact him at his site or send him an email for a request for coluracetam?
i would buy it if he supplied it

Edited by Ampa-omega, 20 December 2011 - 05:34 AM.

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