Coluracetam also known as BCI-540 or 2-(2-oxopyrrolidin-1-yl)-N-(2, 3-dimethyl-5, 6, 7, 8-tetrahydrofuro2, 3-b quinolin-4-yl) acetoamide was formerly known as MKC-231. Coluracetam is a new synthetic nootropic from the racetam family however, it a strong nootropic compound in enhancing memory and general cognitive functioning.
Coluracetam is essentially, a dietary supplement obtained from piracetam. Coluracetam was first developed by Mitsubishi Tanabe Pharma Corporation in 2005. They developed it as a potential treatment for Alzheimer’s disease. Although the preliminary results demonstrated some potential, they failed to reach the endpoints.
Later the license was transferred to BrainCells Inc. which developed it for treatment of major depressive disorder (MDD) and general anxiety disorder (GAD). They reached phase 2a clinical studies that reported some potential in relieving patients from major depressive disorder as well as from anxiety.
Unfortunately, Brain Cells Inc. did not develop it fully and also the company closed down in 2014. Coluracetam has hence been available for licensing since 2012.
Despite all these, coluracetam is regarded a very potent nootropic compound. It is usually fast-acting as it can reach very high levels in the blood within 30 minutes of consumption. However, the levels decrease within three hours of consumption which means one would get maximum benefits within three hours of use.
Just like other racetams, coluracetam increases the acetylcholine levels, however its mechanism of action stands out. Coluracetam primarily enhances the high affinity choline uptake (HACU) process thus increases the conversion of choline to acetylcholine. The neurotransmitter, acetylcholine, is associated with cognitive function and memory, hence the coluracetam ability as a nootropic compound.
The other benefits associated with coluracetam include improving vision, enhance comprehension and free recall, boosting mood, relieving from anxiety and depression as well as an element for bodybuilding.
Coluracetam is found in from f tablets, capsules or liquid. It can be taken orally or sublingually. Coluracetam is a fat-soluble nootropic and so for fast absorption it should be used along a healthy oil/fat such as virgin olive oil.
What is Coluracetam?
Coluracetam is a synthetic and fat-soluble nootropic compound in the racetam family. Coluracetam also known as BCI-540 was formerly referred to as MKC-231.
Although it is a fairly new compound, the coluracetam nootropic benefits are promising. It is believed to offer profound benefits in enhancing memory, learning, relieving anxiety, major depressive disorder as well as improving vision.
Coluracetam mechanism of action
How does coluracetam work in the brain?
Just like other racetams, coluracetam benefits the brain by affecting the choline and subsequently the acetylcholine in different ways. The research so far conducted suggest that the coluracetam effects in the brain are through three main mechanisms. These coluracetam mechanisms of action are elaborated below;
(1) Supporting high-affinity choline uptake
Nootropics in the racetam class are known to induce the production of acetylcholine by stimulating the responsible receptors. However, the coluracetam mechanism of action is unique in that it enhances production of acetylcholine by enhancing the high affinity choline uptake (HACU).
The HACU system is the central mode by which choline is transported to the brain. It is basically the rate-limiting step in the process of acetylcholine production. Acetylcholine is the neurotransmitter associated with memory, learning and general cognitive functioning.
Coluracetam supplements increases the rate at which choline is transported into the brain resulting to more production of acetylcholine. It specifically increases the CHT1, a high-affinity choline transporter, hence lead to high availability of choline for uptake.
In case of HACU breakdown, one experiences what is described as brain fog effect and issues with memory and learning. Coluracetam interestingly increases the choline levels in the blood plasma that helps the HACU system work more efficiently, even when some neurons are damaged.
The increased acetylcholine production in the neurons helps boost short and long-term memory, learning, as well as better decision-making ability.
(2) Improving AMPA potentiation
Research has revealed that coluracetam can enhance alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) potentiation. AMPA receptors are influenced by glutamate which in turn affects the long-term potentiation (LTP) which forms the basis for learning and memory.
Currently, Serotonin Selective Reuptake Inhibitors (SSRIs) are the drugs used in treatment of mood disorders and depression. These SSRIs, however, affect he serotonin levels in the brain which cause many adverse side effects.
Coluracetam comes in handy as treatment for depressive disorders and anxiety by enhancing glutamate activity hence does not cause any serotonin-related adverse reactions.
(3) Protecting the NMDA receptors from the harmfulness of glutamate toxicity
Another probable coluracetam mechanism of action is the ability to protect the N-Methyl-D-aspartate (NMDA) receptors from glutamate toxicity. The NMDA receptor is a glutamate receptor and also an ion channel protein occurring in the nerve cells. NMDA receptor plays a vital role in the control of synaptic plasticity and memory activities.
Damage to the NMDA receptors is linked to key brain disorders such as stroke, traumatic brain injury, Alzheimer’s disease among other brain diseases.
The Benefits of Coluracetam
Coluracetam research recognizes it as a powerful nootropic agent coupled with the positive coluracetam experiences by its users’. Coluracetam is an exciting cognitive enhancer due to its outstanding mechanism of action. However, since it is a new compound more studies in human are needed to confirm the coluracetam benefits insinuated.
Below are the coluracetam benefits that one can experience from consistent and proper use of coluracetam;
(1) Improve Memory and Learning
Coluracetam increases the production of the neurotransmitter, acetylcholine associated with learning and memory.
A number of studies indicate that coluracetam can boost the memory and cognitive function in rats. However, the studies have not yet been conducted with human subjects but the results might be similar.
For instance, in a study of rats with induced memory deficits, the oral administration of coluracetam at 1-10mg/kg was found to improve memory without causing any adverse side effects.
(2) Improve Reading Comprehension and Free Recall
Coluracetam supplements can improve short-term memory, enhance focus as well as free recall. These properties enable learners and anyone in a competitive environment to improve their performance.
Several coluracetam experiences by individual users demonstrate the ability of coluracetam to boost performance through better comprehension reading as well as free recall of studied materials.
(3) Long-term Cognition Improvement
Coluracetam is said to influence the choline uptake regulation system thereby enhancing the cognitive function long after the administration of even low coluracetam dosage.
(4) Reduce Treatment-Resistant Depression
Research shows that coluracetam supplements are a potential treatment for people resistant to anti-depressants.
A phase 2a trial was conducted by BrainCells Inc., on patients’ resistant to anti-depressants to test the efficacy of coluracetam against major depressive disorder (MDD) and general anxiety disorder (GAD). The preliminary results indicated that coluracetam at 240mg/day was effect against MDD and GAD.
(5) Potential Neurogenesis promotion
Neurogenesis is basically the process by which new brain cells are created. This process is vital for both cognitive function and general brain heath.
Coluracetam is able to promote neurogenesis but the underlying mode of action is unclear. Research suggests that it could be related to the ability of coluracetam to increase the acetylcholine levels and especially in the hippocampus.
(6) Can improve Mental Disability
Coluracetam increases acetylcholine activity which could help people suffering Schizophrenia in which the enzyme involved in acetylcholine synthesis is usually impaired.
It could also improve learning for people ailing from other metal disabilities such as Alzheimer’s disease.
(7) May Improve Vision
Coluracetam is an interesting nootropic compound that not only enhances cognition but can also boost your vision through improved color vision, better shape recognition and improved eyesight. It can encourage the growth of nerves in people affected by the degenerative disease of the retina.
Users of coluracetam experience different coluracetam effects including brighter colors, intense contrast, sharp focus on shapes and lights becoming more radiant.
(8) Irritable Bowel Syndrome symptom improvement
Irritable bowel syndrome (IBS) is a prevalent large intestine disease that occur due poor regulation of the choline transporter 1 (CHT1).
A 2018 study shows that coluracetam is able to regulate the CHT 1 molecule hence relieving the symptoms if the irritable bowel syndrome.
(9) Coluracetam recreational use
Coluracetam is a good mood enhancer and provides a relaxing feel gradually. It has been implicated to activate the growth hormones hence good for bodybuilding. However, it is not indicated as an energy booster and hence should be used with a stimulant for best results.
Coluracetam Vs aniracetam, fasoracetam, pramiracetam and Piracetam. What is the difference?
(1). Coluracetam vs Aniracetam
Both coluracetam and aniracetam belong to the racetam family. They are both strong nootropic supplements. Aniracetam was first discovered in the early 1970s. Aniracetam is known to enhance memory and mood, reduce anxiety and symptoms of depression as well as improving focus.
While both coluracetam and aniracetam affects acetylcholine levels in your brain, they differ in the way they affect it. Aniracetam directly leads to release of more acetylcholine while the main coluracetam mechanism of action is through regulation of the high affinity choline uptake process leading to more choline uptake and conversion into acetylcholine.
Additionally, coluracetam has been seen to lead to intense contrast and enhances details while Aniracetam leads to more colour saturation.
Although aniracetam and coluracetam nootropics are mood enhancers, Coluracetam is a better mood enhancer than aniracetam.
Furthermore, some aniracetam users report improved creativity. Coluracetam on other hand improves vision.
(2). Coluracetam vs Fasoracetam
Fasoracetam is the newest nootropic in the racetam family. It is being developed as a potential treatment or Attention Deficit Hyperactivity Disorder (ADHD) in children.
Just like coluracetam, Fasoracetam is a potential brain health nootropic that improves memory and general cognitive function. They both increase choline uptake which is used in the synthesis of acetylcholine.
One of the outstanding fasoracetam mechanism of action is its ability to upregulate GABAb receptors. The GABA receptors are associated with learning, calming effects that aid in relieving anxiety and depression as well as improve sleep.
These two nootropics might have very similar effects. However, a distinguishing characteristic is that, coluracetam produces acetylcholine at a higher rate than fasoracetam. Additionally, coluracetam ability in enhancing mood is well proven while that of fasoracetam is not fully proven.
Like other racetams, Fasoracetam requires to be used along with a good choline source such as Alpha GPC. However, it is difficult to stack it with other supplements. Interestingly, coluracetam fasoracetam stack is the only recommended stack.
(3). Coluracetam vs. Pramiracetam
Pramiracetam is one of the most powerful nootropics from the racetam family. It has very strong memory enhancing capability. Unlike other racetams, which are not mostly used on healthy subjects, pramiracetam can be used on healthy persons as well.
Like coluracetam, pramiracetam increases neurotransmitter in the brain. However, unlike coluracetam or other racetams that affects specific neuron receptors, pramiracetam can affect them all as well as influence the hippocampus.
While they can both improve memory, pramiracetam also offers the benefits of being a stimulant. However, coluracetam also offer additional benefit from pramiracetam of relieving anxiety and boosting mood.
(4). Coluracetam vs. Piracetam
Piracetam is the first nootropic to be synthesized and the strongest among other nootropics in the racetam class. Piracetam is an effective cognitive enhancer mostly for the elderly and people with cognitive deficiency. However, it might not be of help to healthy persons.
While both piracetam and coluracetam boost the level of acetylcholine in the brain their mode of action differs. Piracetam makes acetylcholine receptors to be more sensitive to acetylcholine, while, coluracetam increases the conversion of choline to acetylcholine by influencing the high affinity choline uptake process.
Coluracetam Dosage, Stack, Supplementation
(1) Coluracetam Dosage
The food and drug administration (FDA) regards coluracetam and other racetam nootropics as new unapproved drugs and hence there is no standard coluracetam dosage is defined. In this case the recommended coluracetam dosage would be derived from human clinical studies but unfortunately only limited research has been conducted with human subjects.
Well, all is not lost as many coluracetam reviews from individual users assist in getting an appropriate coluracetam dosage. The effective dosage lies between 5-20 mg per day, however, comparing coluracetam oral vs sublingual administration then the dose can be adjusted accordingly.
On choosing coluracetam oral vs sublingual dosage, the sublingual dosage should be lower. Sublingual administration basically involves placing coluracetam under the tongue and allowing it to dissolve via the skin. This allows coluracetam nootropic to flow directly to the bloodstream which enhances coluracetam effects.
Most users report a coluracetam dosage of 20-80 mg daily taken in two doses, one early in the morning and the other in the afternoon.
However, a high coluracetam dosage of about 100 mg daily taken thrice would be required to treat major depressive disorder as well as general anxiety disorders. A dosage of up to 240 mg daily administered thrice have been used in test without any adverse side effects.
As with any drug or dietary supplement, always start at the lowest effective dose and increase gradually as your body may require. Coluracetam should be taken with a good choline source to cater for choline deficiencies that could result to headaches.
(2) Coluracetam Stack
Racetams and other nootropic supplements yield better results when they are stacked with other supplements. Racetams particularly requires to be taken along with a good choline source to avoid the effects associated with insufficient choline in the brain such as headaches. Coluracetam is not an exception.
If you consider the coluracetam alpha GPC nootropic stack, a dosage of 300-600 mg daily would be appropriate otherwise 250-750 mg per day of CDP choline would yield better results take with 10-20 mg of the coluracetam daily.
Since stacking can be very wide as coluracetam provides room for experimentation, consider a stack that will significantly increase your cognitive functioning while stimulating great mental and physical energy as well as counteract choline deficiency. Such as stack include a coluracetam oxiracetam stack, coluracetam fasoracetam stack among others.
An example of a complete coluracetam oxiracetam stack is
- 20 mg coluracetam -the primary cognitive enhancer
- 200 mg oxiracetam -provides synergetic benefits with coluracetam
- 200 mg caffeine- to act as the stimulant
- 400 mg L-Theanine-to promote relaxation
- 300 mg of a choline source such as Alpha GPC supplement
(3) Coluracetam Supplementation
Coluracetam supplement can be found inn form of coluracetam powder, liquid usually easily taken sublingually and also as coluracetam capsules.
There are main ways of how coluracetam can be taken i.e. coluracetam oral vs sublingual administration. Sublingual administration is more effective than oral. When the supplement is placed under the tongue it penetrates directly into the bloodstream hence a faster and easier absorption.
Coluracetam is popular for its primary function in enhancing memory and learning along with other benefits such as improving vision, relieving anxiety and major depressive disorder as well as treating irritable bowel syndrome.
Coluracetam works mainly by increasing acetylcholine levels in the brain. Another alternative to coluracetam supplementation is taking choline-rich foods such as eggs, liver, beef and chicken meat, broccoli among others.
Most users of coluracetam stack it with a good choline source such as CDP-Choline or Alpha-GPC to boost coluracetam’s effects and lower possible side effects.
Coluracetam is a fat-soluble nootropic hence requires to be taken with a healthy oil such as unprocessed coconut oil, or extra virgin olive oil for better absorption.
Side Effects& Interaction
Coluracetam side effects
Coluracetam is a safe and well tolerated nootropic compound that has been used without causing adverse side effects. However, some mild to moderate side effects have been reported. The coluracetam effects usually occur when there is an overdose.
These possible coluracetam side effects include;
Headaches: This is very common with all racetams due to the fact that the increase choline conversion to acetylcholine. Inadequate choline in the brain usually results to headache in parts of the brain. Some coluracetam users have reported headaches. This is corrected by stacking with a good choline source and also lowering the dosage.
Brain fog: this simply means lack of focus and confusion. Some users of coluracetam have reported the feeling of disorientation as well as lack of focus. However, this usually disappears with consistent use of coluracetam at the right dosage.
A decline in mood: This is a contradiction of the supplements benefits. While it is known as a mood enhancer some users of coluracetam experience low mood at the start and more so with higher doses. Fortunately, lowering the dose could possibly help in improving the mood as well as using it along a better mood enhancer.
Nausea: when coluracetam is taken in overdose one is likely to experience nausea.
Daytime sleepiness: An overdose could decrease your level of alertness even during the day.
Other coluracetam side effects noted are irritability, anxiety, suicidal thoughts, and some night sleep disturbance.
The good news is that all these coluracetam effects are avoidable by;
- Using it with a choline source,
- Using the recommended dosage,
- Taking the supplement in the morning and afternoon,
- Taking adequate water.
Some coluracetam interactions have been reported and hence one should be very careful when considering this supplement. Talking to your doctor is highly advised to keep you informed on any drug interactions and also in the choices of your dietary supplementation.
Below are some of the interactions;
Coluracetam may hinder the effectiveness of anticholinergic drugs, including Parkinson’s medications, Benadryl, and some antipsychotics.
Coluracetam is a cholinergic supplement and may therefore increase the effects of cholinergic drugs, such as Alzheimer’s and glaucoma drugs.
It may also influence the NMDA receptor drugs, such as cough medicine and anesthetics.
Clinical research& User Experience
Coluracetam clinical research
Human clinical trials regarding coluracetam are limited to one trial conducted by Brain Cells Inc. the study involved over 100 people suffering from major depressive disorder and generalized anxiety. The preliminary results suggest that coluracetam had some potential however, they did not develop the supplement.
Despite coluracetam being a fairly new nootropic compound with limited human studies some individual users report some benefits as well as side effects. Some of the coluracetam experiences reported are;
- Brighter colors
- Improved eyesight
- Boosted mood
- Enhanced memory
- Relieved from anxiety
- Improved focus
- More energy
- Improved visual imagination
- Enhanced reading comprehension and free recall
However, some coluracetam reviews reveal some side effects:
- Brain fog
- Suicidal thoughts
- Inconsistent results
- Disrupted night sleep
- Day sleepiness
Due to lack of scientific back-up of the above coluracetam effects, we advise you to consult your medical care provider before taking the supplements.
Who can use coluracetam?
Coluracetam powder or solution is good for everyone who would like to reap its various benefits. However, people with some medical issues such as Parkinson’s disease, and also pregnant women are advised not to use this supplement.
People suffering from memory deficiency due to reasons such as age and illnesses like Schizophrenia and Alzheimer’s disorders among other memory-deficiency causing factors, can benefit from coluracetam supplement.
Coluracetam powder is fit for people suffering from anxiety and depression as it is able to boost mood and ability to reason. This coluracetam increases acetylcholine in the brain, which enhances memory and focus. Coluracetam for anxiety is a good option.
Coluracetam is also a good supplement for people intending to improve vision. This supplement helps one see clearly by enhancing vision, intensified contrast and lights become brighter. It has further been seen to enhance repair of damaged retinal and optical nerves.
Coluracetam powder or its liquid form is an excellent supplement for students. It is able to boost comprehension and free call hence can potentially improve performance.
Bodybuilders are not left out since this supplement can help in recreational activity that enhance relaxation and bodybuilding.
Where to Buy Coluracetam?
Coluracetam for sale is readily available online. If you consider buying coluracetam for sale or for personal use, carefully check for reputable vendors online. Since this is a fairly new supplement not many companies are offering coluracetam for sale and hence can easily choose from the alternatives available.
Coluracetam is a new member of the racetam family and has gained popularity due to its ability to improve cognitive function, as well as improve eyesight.
The main coluracetam mechanism of action is through influencing the high affinity choline uptake (HACU) process. This makes it unique and outstanding among the other racetam as only phenylpiracetam has the similar mechanism.
The fact of the matter is that our bodies do not make Coluracetam naturally. Hence, if one has to experience the coluracetam benefits then it has to come from the supplements.
Although only limited human trials are documented in regards to the benefits, a good number of people already tried it and reported some benefits.
Coluracetam for depression and anxiety has been reported in a clinical trial and this makes it a good candidate for further studies to confirm the said benefits.
Due to the limited human studies with this supplement, the possible side effects are not clearly defined, however, headache is a common issue with racetams.
Stacking coluracetam with a choline source is advised to offset the effects that occur due to choline deficits such as headaches. Such stack includes coluracetam alpha GPC stack and coluracetam CDC choline stack.
Coluracetam is a fat-soluble compound so for easier absorption into cells it should be taken with a healthy fat/oil like unprocessed coconut oil, or extra virgin olive oil.
Coluracetam stacks well with other racetam and also other supplements. Examples of such coluracetam stacks are coluracetam oxiracetam stack and coluracetam fasoracetam stack. This provide an opportunity for further research in coluracetam and other products. Coluracetam with noopept could be a possible synergistic combination for enhancing memory and cognitive function.
Additionally, coluracetam as with other racetam increases acetylcholine levels while a decline choline is experienced. This makes stacking coluracetam with a good choline source such as coluracetam Alpha GPC stack.
Limited clinical trials exist to confirm the coluracetam benefits furthermore many personal coluracetam experiences suggest the potential benefits. This shows that more research is required to confirm these benefits.
BrainCells Inc. has closed down hence coluracetam is open for licensing for further clinical trials.
Coluracetam interactions with other drugs is also an area that requires further studies.
- Akaike A, et al. (1998). Protective effect of MKC-231, a novel high affinity choline uptake enhancer, on glutamate cytotoxicity in cultured cortical neurons. Jpn J Pharmacol.
- Bessho, T., Takashina, K., Tabata, R., Ohshima, C., Chaki, H., Yamabe, H., Egawa, M., Tobe, A., & Saito, K. (1996). Effect of the novel high affinity choline uptake enhancer 2-(2-oxopyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b] quinolin-4-yl) acetoamide on deficits of water maze learning in rats. Arzneimittel-Forschung, 46(4), 369–373.
- Murai, S., Saito, H., Abe, E., Masuda, Y., Odashima, J., & Itoh, T. (1994). MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice. Journal of Neural Transmission, 98(1), 1–13.doi:10.1007/bf01277590.
- Shirayama, Y., Yamamoto, A., Nishimura, T., Katayama, S., & Kawahara, R. (2007). Subsequent exposure to the choline uptake enhancer MKC-231 antagonizes phencyclidine-induced behavioral deficits and reduction in septal cholinergic neurons in rats. European Neuropsychopharmacology, 17(9), 616–626. https://doi.org/10.1016/j.euroneuro.2007.02.011.
- BrainCells Inc. Announces Results from Exploratory Phase 2a Trial of BCI-540Archived November 21, 2011, at the Wayback Machine.
- RAW COLURACETAM POWDER (135463-81-9)