Given COLURACETAM's current lack of availability to the general public I decided to take the plunge and have some COLURACETAM manufactured via custom synthesis.
I initiated this process about 6 months ago; following which it took a couple of months for the custom synthesis laboratory to complete the manufacturing and purification process; after which purity was confirmed via both HPLC and HNMR ANALYSIS
Since then I have been comprehensively trialling it myself personally; and will now share my findings with the LONGECITY forum community
First of all, if anyone is considering also proceeding down the route of obtaining some COLURACETAM via custom synthesis, please kindly note the following:
1) COLURACETAM is very lengthy, complex and time consuming to synthesize; and hence if anyone wishes to consider having it custom synthesized it will be pretty expensive if you wish to end up with a product that isn't contaminated with potentially highly toxic impurities (at least one of the synthesis component ingredients is very toxic; whereas the final substance, COLURACETAM, is not)
2) If you wish to obtain COLURACETAM that is sufficiently pure, then my advice is to forget about CHINA; but instead obtain quotations from reputable custom synthesis laboratories in the UK, EUROPE or USA (there may be others in other countries).
3) I have had 500 grams of pure COLURACETAM (>99.9% PURITY) manufactured by a reputable EUROPEAN custom synthesis laboratory; it cost US$16,000; here is the INVOICE:
Regarding my personal trial of COLURACETAM, throughout the process I made a point of writing copious notes each and every day, logging my personal experiences and comments. Rather than type up the entirety of my notes, which would be somewhat lengthy, I will instead now summarize as concisely as I can the key points:
- PURITY ANALYSIS:
- APPEARANCE: COLURACETAM's appearance is that of a CREAM COLOURED POWDER
Where PIRACETAM and the other RACETAMS are pretty much all WHITE in colour, I could not but help notice how COLURACETAM's appearance is quite a bit different, in that it has a distinctly yellowy cream colour, as opposed to being pure white as per the other RACETAMS.
Here is a photo of COLURACETAM powder resting on top of a white piece of paper:
- TASTE: Unfortunately, COLURACETAM's taste is more akin to that of PRAMIRACETAM than OXIRACETAM, in that it tastes absolutely vile
Specifically, the taste is a potent combination of bitterness and an extremely unpleasant chemical taste, that lingers as an aftertaste.
- DOSAGE: The dosage of COLURACETAM used in the clinical study by Braincells Inc. was 80mg taken 1 - 3 times daily; consequently, I comprehensively evaluated the effects of COLURACETAM on myself when taken at a variety of doses, ranging from 10mg OD up to and including 80mg TID:
BRAINCELLS INC. ANNOUNCES RESULTS FROM EXPLORATORY PHASE 2A TRIAL OF BCI-540 [COLURACETAM] IN DEPRESSION WITH ANXIETY
Positive Signal Observed in Difficult-to-Treat Patient Population
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 [COLURACETAM] 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 [COLURACETAM] 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 [COLURACETAM] 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 [COLURACETAM] 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 [COLURACETAM] 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 [COLURACETAM] 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 [COLURACETAM] in this difficult-to-treat population.”
BCI-540 [COLURACETAM] 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.
- ADMINSTRATION METHOD: Wishing to ensure optimal absorption of COLURACETAM I took all my doses SUBLINGUALLY; wherein, aside from the awful taste, there was no issues with taking COLURACETAM in this manner.
- MEASURING DOSES: All doses were measured precisely using my laboratory research scales that are accurate to 0.0001g (= 0.1mg):
- STORAGE: Upon the advice of the CHEMIST who oversaw the synthesis of the COLURACETAM I store it in a COOL and VERY DRY place and within a storage container that protects against the effects of UV LIGHT, wherein I use pharmaceutical amber glass jars:
- BEFORE COMMENCING TRIAL: Before commencing taking any COLURACETAM, firstly I underwent baseline blood tests for LIVER and RENAL FUNCTION as well as TESTOSTERONE, DHT, and ESTRADIOL; and secondly, I stopped taking any and all RACETAMS for a period of 1 week, as a washout period.
- TEST DOSES: Prior to taking COLURACETAM at the dosage range used in the study (80mg 1-3 times daily) I first took test doses of 1mg and then 10mg COLURACETAM to rule out ALLERGIC / NEGATIVE REACTIONS. Suffice to say I did not react in any way negatively to the TEST DOSES.
- USAGE FEEDBACK SUMMARY:
Without a doubt, COLURACETAM's pharmacological effects appear to be significantly more potent, profound and widespread than all the other RACETAMS.
Summary of both postive and negative effects experienced as follows:
The following is a list of any and all POSITIVE effects that I have personally experienced when taking COLURACETAM, wherein the potency of the individual effect ranged from WEAK to STRONG. Accordingly, I have allocated an indicator, comprising a number between 1 and 10, wherein the higher the number the stronger the effect and counterwise the lower the number the weaker the effect, (please kindly note that these are solely my own personal experiences and were not placebo controlled):
- ENHANCED MEMORY (both SHORT-TERM and MEDIUM-TERM MEMORY): 3
I have personally found that with respect to the NOOTROPIC effect(s) of all the RACETAMS, whilst I have experienced improvements in concentration and working capacity / productivity, I have never experienced a noticable ongoing improvement in memory. COLURACETAM is the only RACETAM that I have taken wherein I noticed an improvement in MEMORY, both with regards to SHORT-TERM and MEDIUM-TERM MEMORY. To put matters into perspective, the memory improvement has been mild, yet still significant; whereas I have experienced no such improvement at all with the other RACETAMS.
- IMPROVED CONCENTRATION: 5
- IMPROVED WORKING CAPACITY / PRODUCTIVITY: 7
- INCREASED ENERGY & STAMINA: 4
- INCREASED ALERTNESS & LUCIDITY: 3
- ANXIOLYTIC: 10
- ANTIDEPRESSANT: 5
- IMPROVED OLFACTORY SENSITIVITY (both sense of taste and smell): 4
- IMPROVED VISION: 3
- ENHANCED ENJOYMENT OF MUSIC: 6
- CAFFEINE, POTENTIATION OF ITS STIMULATORY EFFECTS / PARTIAL REVERSAL OF TOLERANCE: 4
- INCREASED / IMPROVED SOCIABILITY 7
This effect was totally unexpected; and first become noticable in that it partially rekindled the stimulatory effect of CAFFEINE when I was suffering a pre-existing state of CAFFEINE TOLERANCE; this effect remains as long as I continue to take the COLURACETAM, but quickly vanishes if I stop taking the COLURACETAM. As a consequence I am finding that I now drink less COFFEE and TEA and their stimulating effects are greater.
NEGATIVE EFFECTS (SIDE EFFECTS):
Personally, I found that at a dosage of 80mg BID I experienced daytime drowsiness to the extent that I had instances wherein I felt like I needed to go and lie down; this wasn't an unpleasant feeling, more akin to an extreme relaxation to the extent that it was sedating. Reducing the dosage eliminated this side effect entirely.
I experienced intermittent manifestation of nausea which was most certainly dosage dependant, wherein reducing the dosage eliminated this side effect entirely. Also, the instances of nausea typically occured when I began experimenting with taking the COLURACETAM in combination with other substances, such as HYDERGINE and PIRACETAM.
N.B. I will do my best to expand on the information within this initial post as and when I have some more free time (I unfortunately have a crazy work schedule)
1) My feedback regarding my personal experience with taking COLURACETAM is purely ANECDOTAL; furthermore, it has in no way been PLACEBO CONTROLLED, and hence some or all of the POSITIVE EFFECTS that I have listed could very well be due to the PLACEBO EFFECT.
2) Furthermore, I should add that I am recovering from CNS LYME DISEASE, BABESIOSIS and BARTONELLOSIS, and hence do not fall within the categorization of HEALTHY INDIVIDUAL; wherein it is possible that some of the benefits that I have experienced may not occur in HEALTHY INDIVIDUALS
3) I am not a vendor; I do not sell anything and that includes COLURACETAM.
4) I am not affiliated in any way with any custom synthesis laboratories.
UPDATE [19th September 2012]:
- POSITIVE EFFECTS:
I have added INCREASED / IMPROVED SOCIABILITY to my list of POSITIVE EFFECTS experienced. This effect is consistent.
I have been experimenting with various DOSAGES of COLURACETAM and have settled on a dosage that I consider, as far I am personally concerned, to be my ideal dosage; and this is 10mg TID (taken SUBLINGUALLY)
I experience all the POSITIVE EFFECTS that I have listed at this dosage.
- DURATION OF EFFECT:
I personally find that COLURACETAM's primary effects last the strongest for circa 4 - 5 hours, which is why I dose it TID with individual doses taken about 4 hours apart. The memory improvement is 24/7.
- STACKING COLURACETAM WITH OTHER NOOTROPICS:
OK this is predominently what I am currently experimenting with; wherein I have now fixed my dosage of COLURACETAM at 10mg TID, to which I have been stacking other NOOTROPICS one at a time individually at various dosages to establish how I react.
Here is my feedback regarding my experiences with regards to this so far (N.B. Please note that this is my own personal experience and does not mean that you will experience the same):
-- COLURACETAM, as far as I am concerned, does NOT stack well with PRAMIRACETAM at any dosage; wherein even at 50mg PRAMIRACETAM I experience manifestation of undesirable ADVERSE EFFECTS, which included: IRRITABILITY, IMPAIRED MOOD / DEPRESSION, ANXIETY, RESTLESSNESS, AGITATION and SLEEP DISTURBANCE.
-- COLURACETAM does stack exceedingly well with OXIRACETAM, wherein it appears to exert a potentiation of OXIRACETAM's effects, and as such I am finding individual dosages of OXIRACETAM of just 100mg to be highly efficacious.
-- It also stacks exceedingly well with very low dosages of HYDERGINE, wherein I have found a dosage of 0.1mg TID of HYDERGINE to be optimal, which is circa 1/10 the typical dosage for HYDERGINE.
I find that if I take HYDERGINE at a total daily dosage of 1mg+ then I experience persistent NAUSEA, which vanishes entirely when the dose is reduced.
-- I am currently in process of testing out a stack comprising COLURACETAM 10mg + OXIRACETAM 100mg + HYDERGINE 0.1mg, all taken TID; and so far the effects are pretty damn amazing... my working capacity is through the roof; and my energy levels incredible, which given my history of CFS is IMO particularly noteworthy
UPDATE [26th September 2012]:
- POSITIVE EFFECTS:
I have continued to take COLURACETAM every day without any breaks whatsoever and the all the POSITIVE effects are still occurring consistently and to the same magnitude.
I have increased my daily dosage of COLURACETAM to 10mg QID (taken SUBLINGUALLY) with circa 3-4 hours between doses.
I still experience all the POSITIVE EFFECTS that I have listed at the 10mg dosage. The reason why I have commenced taking four doses daily as opposed to three is somewhat due to the crazy work hours that I am doing at the moment, wherein I am usually pulling 18+ hour work days, and starting the day at all sorts of silly hours, such as 4:00AM
I am finding that my 10mg dose of COLURACETAM (taken SUBLINGUALLY) upon waking is highly effective in shaking off any and all sleepiness / grogginess within a matter of minutes, even when arising in the middle of the night with only a few hours of sleep... I am finding that COLURACETAM provides consistent results in this regard when other substances that I have tried in the past for the same purpose have failed miserably to yield consistent efficacy with repeated use; this includes ARMODAFINIL and PHENYLPIRACETAM, both of which I found to be a huge disappointment
- DURATION OF EFFECT:
Further to what I stated previously in my last update, I am finding that with the 10mg dosage COLURACETAM's primary effects in fact appear to last for circa 3 - 4 hours, wherein I this is applicable most notably to the ENERGY boosting effect. I should add that I am stacking the COLUTACETAM with CAFFEINE, taken as COFFEE and BLACK TEA, however prior to commencing the COLURACETAM I was very much suffering CAFFEINE TOLERANCE. I find that the COLURACETAM itself seems to have a STIMULATING / ENERGY ENHANCING effect as well as most certainly, for me at least, either POTENTIATING the effects of CAFFEINE or partially reversing TOLERANCE to CAFFEINE through some mechanism... I will be very interested to hear whether others also experience this same effect
- STACKING COLURACETAM WITH OTHER NOOTROPICS:
I have been continuing to experiment with stacking COLURACETAM with other NOOTROPICS and can now confirm the following further to the information outlined in my previous update:
-- COLURACETAM, as far as I am concerned, does NOT stack well with PIRACETAM at any dosage; wherein even at 800mg OD I experience manifestation of undesirable ADVERSE EFFECTS, which includes: FATIGUE, LETHARGY, IMPAIRED COGNITION / BRAIN FOG, IRRITABILITY.
I will reiterate that personally, as far as I am concerned, I find that COLURACETAM does stack exceedingly well with both OXIRACETAM and HYDERGINE; wherein (possibly due to SYNERGY) only a very low dosage of each is required to induce quite profound POSITIVE EFFECTS. Specifically, I find that OXIRACETAM at a dosage of just 100mg taken 1 - 3 times daily is, for me, the ideal dosage; and with regards to HYDERGINE I have found that taking it AT BEDTIME has eliminated, for me, any potential for inducing NAUSEA, and hence I am currently taking 1mg OD at BEDTIME.
BTW the issue of CARDIAC FIBROSIS and HYDERGINE is bound to come up at some point, so let me pre-empt this by offering what is my personal opinion on the subject. In short, with anything I consider it is all about weighing up RISK versus REWARD; and the possible concerns relating to CARDIAC FIBROSIS is in fact associated with a select number of studies on ERGOT DERIVATIVES in general, as opposed to HYDERGINE specifically, so it is unknown whether or not these possible risks are in fact applicable to HYDERGINE. Furthermore, any such risk would almost certainly be DOSAGE DEPENDANT and hence why I personal advise taking the MINIMUM DOSAGE at which the desired POSITIVE EFFECTS are experienced, which given this would be much lower than the 'NORMAL' dosage of HYDERGINE would reduce any such possible risk. This is of course just my personal opinion, and I would advise others to pass their own judgement on the subject.
- STACKING COLURACETAM WITH CHOLINE:
There has been quite a bit of focus on the subject of COLURACETAM and CHOLINE, specifically relating to the fact that it reportedly functions as a CHOLINE UPTAKE ENHANCER.
Well, here is a conundrum for you... I have stopped taking supplemental CHOLINE, and I am so far finding that I experience no lessening of POSITIVE EFFECTS whatsoever.
In fact, I find that if I combine any dosage of supplemental CHOLINE with COLURACETAM my mood takes a dive distinctly downwards; however, without any supplemental CHOLINE the COLURACETAM has a profound POSITIVE effect on my mood.
I am taking the 10mg QID dosage of COLURACETAM every day without any supplemental CHOLINE and have yet to experience any of the CHOLINE DEFICIENCY type adverse effects associated with RACETAM usage, such as HEADACHE, BRAIN FOG etc...
I should add that I do not consume any EGGS either via my diet.
So, despite the spiel about COLURACETAM being a CHOLINE UPTAKE ENHANCER I would urge others taking COLURACETAM to do so with an open mind and not assume that one needs to supplement with CHOLINE. I recommend that you experiment with taking COLURACETAM both with and without supplemental CHOLINE and see how you personally respond... I would be very interested in hearing how others respond in this regard
-- So, my current stack comprises:
- COLURACETAM 10mg QID
- OXIRACETAM 100mg OD - TID
- HYDERGINE 1mg OD at BEDTIME
and NO SUPPLEMENTAL CHOLINE
UPDATE [7th October 2012]:
BLOOD TESTS results following my first few months' consistent uninterrupted usage of COLURACETAM now in.
In short, I am pleased to report that blood tests for LIVER and RENAL FUNCTION as well as TESTOSTERONE, DHT, and ESTRADIOL are all NORMAL and there are no significant changes versus baseline blood test results.
Edited by ScienceGuy, 07 October 2012 - 03:31 PM.