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Racetam Family of Nootropic– Coluracetam

Coluracetam (BCI-540, or MKC-231) is a fat-soluble nootropic in the racetam-class of compounds. Coluracetam is much more potent than the original racetam, Piracetam. Coluracetam was patented by Mitsubishi Tanabe Pharma of Japan in 2005. Making it one of the newest racetam-based nootropics.

The patent for Coluracetam was later sold to BrainCells, Inc. in San Diego, California. BrainCells is a small, privately-held biopharmaceutical company specializing in developing compounds for the treatment of major depressive disorder (MDD), treatment resistant depression (TRD), and Alzheimer’ s Disease.

Coluracetam is similar in structure to Piracetam. And like all racetam nootropics, has a pyrrolidone nucleus at its core. The latest clinical research indicates potential for treating depressive disorders, and retinal and optic nerve damage.

Coluracetam is a very strong choline targeting supplement. It boosts your brain’ s choline conversion to acetylcholine (ACh) through the high affinity choline uptake (HACU) process. Which increases alertness, attention to detail and memory.

Some research, and personal experience shows Coluracetam may affect AMPA receptors. Making it a potential ampakine nootropic. Which could explain the stimulant-like effects without the side effects of traditional stimulants. Coluracetam also shows some anxiolytic (anti-anxiety) qualities helping improve mood and quieting anxiety.


How Coluracetam Works(Mechanism of Action)

Like most racetam compounds, coluracetam(CAS:135463-81-9) works mainly by increasing levels of the neurotransmitter acetylcholine, which is strongly associated with learning, memory, and cognition.

However, the way that coluracetam modulates acetylcholine levels is unique. Typically, racetams trigger acetylcholine production by stimulating the appropriate receptors, but coluracetam does so by enhancing high-affinity choline uptake, or HACU. The HACU system determines the rate at which choline is drawn into neurons for conversion into acetylcholine.

By increasing the rate at which choline is drawn into nerve cells, coluracetam promotes acetylcholine production and causes brain levels of this crucial neurotransmitter to rise.‍ It has also been shown to create an increase in the high-affinity choline transporter molecule CHT1, which leads to the rapid availability of choline for uptake.

Together these actions lead to higher levels of acetylcholine, which are associated with enhanced cognition and memory.


Benefits And Effects Of Coluracetam

 Coluracetam Improves Memory and Learning

Coluracetam benefits proves to work in enforcing cognitive and memory function in rats and similar effects on humans. Brain Cells Inc. conducted a study which reveals an improvement of mind in rats after receiving AF64A for eight days. The development continued to last even beyond treatment. Alzheimer’s disease leads to lower levels of acetylcholine. By growing acetylcholine in the hippocampus, coluracetam will increase symptoms of Alzheimer’s disease such as learning disorders and poor memory.


 Coluracetam Reduces Treatment-Resistant Depression

In a study of 101 individuals with depression, who did not achieve result treatment with antidepressants, it had a constructive impact on the apparent improvement in the quality of life at 80 mg 3 times a day. However, this is the only study on humans. The capacity it holds to minimize glutamate noxiousness may be liable for its positive impacts in the depression treatment.


 Coluracetam Reduces Anxiety

In a rat study, dosing 21 days of coluracetam shows a 20% improvement in anxiety, which was higher than the 12% effect valium impact in a single dose in the same study.


 Coluracetam Promotes Neurogenesis

Some studies mention that it helps with neurogenesis. The primary mechanism is still not clear, but it relates to the administration of it for several weeks, which increase in acetylcholine in the hippocampus area.‘’Patents state that it promotes nerve cell growth (neurogenesis). The mechanism is unknown, yet is thought to be related to the increase in hippocampal acetylcholine when coluracetam is dosed daily for a few weeks.’’


 Coluracetam Helps with Schizophrenia

Coluracetam increases the activity of ChAT in rats with nerve cell damage. This increase suggests it may benefit patients with schizophrenia through this same enzyme. More research directly on people with schizophrenia is undergoing.


 Coluracetam Enhances Eyesight

Coluracetam has shown its optic strengths such as improved color recognition, vision, and vividness. Specifically, it promotes nerve growth for the degenerative retinal disease. Numerous studies mention better color vision and sharpening of the eyesight, but no scientific research has confirmed these effects.

AASraw is the professional manufacturer of Coluracetam.

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How does Coluracetam Work in the Brain?

Coluracetam boosts brain health and function in several ways. But two in particular stand out.

Coluracetam boosts your brains choline uptake by targeting and working with the high affinity choline uptake (HACU) process in the brain’s neurons.

Acetylcholine (ACh) is made up of choline and acetate. These must be available to the neuron terminal at all times. So that ACh can be synthesized whenever it is needed.

Free choline circulating in the blood crosses the blood-brain barrier. And is taken up by cholinergic neuron terminals. It gets taken into the neuron by the high affinity choline uptake (HACU) system. The synthesis of ACh takes place in the synaptic cleft. The space between neurons as it travels into the neuron.

The HACU system is temperature-, energy-, and sodium-dependent. This system is the primary means by which choline needed for the synthesis of ACh is transported into the neuron. And is the rate-limiting step in the production of this critical neurotransmitter.When this system breaks down or doesn’ t work as efficiently as it was designed, you experience problems with memory, learning, and brain fog.

Coluracetam effects this process and helps it work more efficiently. In fact, it seems to boost the HACU process. Even in damaged neurons. Increased acetylcholine in neurons helps improve memory, boosts cognition and provides better decision-making capabilities.

Coluracetam also seems to improve AMPA potentiation. AMPA receptors are affected by glutamate. Which works in the brain and central nervous system to improve alertness and cognition.

Coluracetam works with both AMPA potentiation and choline uptake enhancement. This combination seems to help improve mood disorders without affecting serotonin levels.

Serotonin Selective Reuptake Inhibitors (SSRIs) is the current preferred mainstream medical method for dealing with mood disorders and depression. They come with a list of detrimental side effects. And don’ t work for every depressed patient.

Researchers reported that Coluracetam was beneficial in treating major clinical depression and anxiety disorder. Without affecting serotonin levels in the brain. And without the side effects that go with disrupting serotonin.


Coluracetam Usage: Dosage And Stack For Reference Only

Coluracetam is a compound which isn’t found in any foods and our bodies cannot produce it. Hence, the only way to yield the benefits of this molecule is through supplementation.

Coluracetam is typically sold in powder or capsule form and can be taken orally. Doses can also be taken sublingually (under the tongue) for faster and more efficient absorption.

Since coluracetam is a particularly powerful agent, it’s advisable to start with the lowest effect dose. If you find you need to increase the dose to feel the benefits, this should be done so gradually and should not exceed 80mg.

Coluracetam is non-toxic and considered safe and well-tolerated.There are only a few rare side effects associated with the compound, such as anxiety, headache, fatigue and nausea. These side effects are rare and usually only occur when there is not a large enough precursor pool of choline to be used for acetylcholine synthesis. This is why we recommend start the synthesis-increase coluracetam with a choline level enhancer such as citicoline.

Coluracetam can interact with some drugs, especially those that interact with the NMDA receptor. This includes cough suppressants and anaesthetics. Other substances which interact with the cholinergic system, such as glaucoma medication and nicotine, may also interact with the effects of coluracetam. Coluracetam can counteract the effects of anti-cholinergic drugs (such as some Benadryl, some antipsychotics and Parkinson’s medications).

As with any supplement, if you’re on medication or have an underlying health condition, it is sensible that you speak to your doctor before starting any supplement regime.


 How To Stacks Well With Other Drugs

♦ Coluracetam is a fat-soluble molecule, so it’s best stacked with a healthy fat such as coconut or MCT oil.

♦ Coluracetam should also be stacked with a choline supplement such as citicoline. Citicoline increases the pool of available choline for synthesis. The stack can create powerful effects by increasing available choline (citicoline) and the ability to synthesise it into acetylcholine (coluracetam).


 Recommended Dose: 5-80mg per day

We recommend between 5-80mg of coluracetam per day.

The safe upper limit for coluracetam is 80mg per day. However, we recommend staying with 35mg per day as the consequences of higher doses have not yet been fully examined in humans.

It’s optimal to split these doses into a morning or afternoon dose. For example, a 20mg dose of 10mg in the morning and a further 10mg in the afternoon.

As previously mentioned, you should start at the lower end of the dosing scale. Beginning of the lowest effective dose will decrease the likelihood of experience any negative side effects.


Coluracetam Side Effects

Coluracetam is non-toxic. So is considered well-tolerated and safe. Many first-time users of Coluracetam report fatigue which is often the result of starting with too high a dose.

Remember, Coluracetam works by enhancing choline uptake in your brain. Choline is a precursor to the production of acetylcholine. If not enough choline is available in your system, you’ll feel the side effects.

Side effects are rare but can include anxiety, fatigue, headaches, nervousness and nausea. Again, side effects are often a result of unusually high doses of the nootropic.

Headaches from using Coluracetam typically happen when you forget to combine it with a good choline supplement. Headaches are often a symptom of a choline deficit in your brain.


Overview– Coluracetam

Coluracetam is one of the newer and less familiar members of the racetam class of nootropics, but it’s a favorite with many users.

It increases levels of the ‘’learning neurotransmitter’’ acetylcholine, which may boost cognition, and animal studies show that it can offset memory deficits without significant side effects. Though there’s little-documented human research on coluracetam, the studies that exist indicate that it may be a valuable treatment for anxiety and depression.

Many users count on it as a reliable mood lifter and memory enhancer that gives them better focus and concentration. Others say it gives them the equivalent of “HD vision”, making colors brighter, contrast more intense, and lights more radiant.

Coluracetam is a potent compound, so dosage amounts are low, and it’s known to be fast-acting. It’s sold as a dietary supplement in the US and can be legally imported into Canada and the UK in small amounts.

There’s still much to be learned about coluracetam, but it appears to be safe for most users when taken responsibly. If you’re interested in adding something new and different to your nootropic stack, coluracetam could be one to consider.

Coluracetam doesn’ t have extensive amount of research, the studies available do show a great potential for its use. It is one of the more recent-going-mainstream racetams, side by side with Fasoracetam. However, recently, the FDA has approved an “enhanced” form of Fasoracetam for the treatment of ADHD.

AASraw is the professional manufacturer of Coluracetam.

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[1] Brauser D. “Neurogenesis-Stimulating Compounds Show Promise in the Treatment of Major Depression” Medscape Medical News September 21, 2009

[2] Murai S., Saito H., Abe E., Masuda Y., Odashima J., Itoh T. “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 General Section. 1994;98(1):1-13.

[3] Takashina K., Bessho T., Mori R., Eguchi J., Saito K. “MKC-231, a choline uptake enhancer: (2) Effect on synthesis and release of acetylcholine in AF64A-treated rats.” Journal of Neural Transmission (Vienna). 2008 Jul;115(7):1027-35.

[4] Bessho T., Takashina K., Eguchi J., Komatsu T., Saito K. “MKC-231, a choline-uptake enhancer: (1) long-lasting cognitive improvement after repeated administration in AF64A-treated rats.” Journal of Neural Transmission (Vienna). 2008 Jul;115(7):1019-25.

[5] Akaike A., Maeda T., Kaneko S., Tamura Y. “Protective effect of MKC-231, a novel high affinity choline uptake enhancer, on glutamate cytotoxicity in cultured cortical neurons.” Japanese Journal of Pharmacology. 1998 Feb;76(2):219-22

[6] Shirayama Y, Yamamoto A, Nishimura T, Katayama S, Kawahara R (September 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): 616–26.

[7] Qualifying Therapeutic Discovery Project Grants for the State of California, IRS.gov.

[8] Malykh, A. G., & Sadaie, M. R. (2010). Piracetam and Piracetam-Like Drugs. Drugs, 70(3), 287–312.


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