|Summary sheet: Coluracetam|
|Routes of Administration|
Coluracetam (BCI-540; formerly MKC-231) is a nootropic belonging to the racetam family of drugs. It was originally developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug had failed to reach the endpoints in its clinical trials, it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD), which was preceded by being awarded a "Qualifying Therapeutic Discovery Program Grant" by the state of California. Findings from phase IIa clinical trials have suggested that it would be a possible medication for a comorbid major depressive disorder (MDD) with generalized anxiety disorder (GAD).
Colouracetam is easily available and sold through online vendors as a dietary supplement in the United States. Dose for dose colouracetam's potency is nearly twice that of noopept, making it require lower amounts while offering many similar effects. Due to its short acting and acute nature, the preferred ROAs are generally insufflation, sublingual, or vaporisation, though it is still active orally.
The active dose range of this compound is between 5 and 20mg. This is much smaller than comparable doses of the racetam class of drugs (piracetam, oxiracetam, phenylpiracetam, etc.). Dosages higher than 20mg do not seem to offer any additional benefit.
Coluracetam, or N-(2,3-Dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxo-1-pyrrolidinyl)acetamide, is a synthetic compound of the racetam family. Racetams share a pyrrolidine nucleus, a five-member nitrogenous ring with a ketone bonded oxygen at R2. This 2-pyrrolidone ring is bound to the terminal carbon of an acetamide group, an ethyl amide chain with a ketone bond (C=O) at the alpha carbon.
Coluracetam features an additional three-ring substituted fluoroquinolone component bonded to RN of the acetamide group. The fluoroquinolone group is comprised of a central nitrogenous pyridine ring fused to a benzyl and furan ring on either side. Two methyl groups are bonded to R2 and R3 of the structure on the furan ring. Coluracetam is structurally analogous to piracetam with an added fluoroquinolone group.
Coluracetam enhances high-affinity choline uptake (HACU), which is the rate-limiting step of acetylcholine (ACh) synthesis. This process essentially allows acetylcholine to accumulate at higher levels than normal. As acetylcholine is involved in the function of memory, this could potentially account for its nootropic effects.
In comparison to the effects of other nootropics such as noopept, this compound can be described as focusing primarily on physical stimulation over that of cognitive stimulation. Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a research literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be regarded with a healthy degree of skepticism. It is worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become much more likely with higher doses and may include addiction, serious injury, or death.
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and harm potential
The toxicity and long-term health effects of recreational coluracetam use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because coluracetam has very little history of human use. Anecdotal evidence from people who have tried coluracetam within the community suggests that there do not seem to be any negative health effects attributed to simply trying this drug at low to moderate doses by itself and using it sparingly (but nothing can be completely guaranteed).
It is strongly recommended that one use harm reduction practices when using this substance.
Tolerance and addiction potential
The chronic use of Coluracetam can be considered as not addictive with a low potential for abuse. It does not appear to be capable of causing psychological dependence among certain users.
Tolerance to many of the effects of Coluracetam develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Coluracetam may presents cross-tolerance with all racetam nootropics, meaning that after the consumption of Coluracetam certain nootropics such as aniracetam and piracetam may have a reduced effect.
Although many psychoactive substances are reasonably safe to use on their own, they can suddenly become dangerous or even life-threatening when combined with other substances. The following list includes some known dangerous combinations (although it is not guaranteed to include all of them). Independent research (e.g. Google, DuckDuckGo) should always be conducted to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
- Depressants (1,4-Butanediol, 2M2B, alcohol, benzodiazepines, barbiturates, GHB/GBL, methaqualone, opioids) - This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration. There is also an increased risk of suffocating on one's vomit while unconscious. If nausea or vomiting occurs before a loss of consciousness, users should attempt to fall asleep in the recovery position or have a friend move them into it.
- Stimulants - It can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.
- Dissociatives - This combination can unpredictably potentiate the amnesia, sedation, motor control loss and delusions that can be caused by each other. It may also result in a sudden loss of consciousness accompanied by a dangerous degree of respiratory depression. If nausea or vomiting occurs before consciousness is lost, users should attempt to fall asleep in the recovery position or have a friend move them into it.
This legality section is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
Coluracetam, being a member of the racetam family, currently is legally available to buy and sell in most countries, but may still vary by region.
- United Kingdom - Coluracetam and other racetams are prescription-only drugs; however, there is no penalty for possession or importing them.
- 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. https://doi.org/10.1007/BF01277590
- Akaike, A., Maeda, T., Kaneko, S., & Tamura, Y. (1998). Protective Effect of MKC-231, a Novel High Affinity Choline Uptake Enhancer, on Glutamate Cytotoxicity in Cultured Cortical Neurons. The Japanese Journal of Pharmacology, 76(2), 219–222. https://doi.org/10.1254/jjp.76.219
- 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
- Bessho, T., Takashina, K., Eguchi, J., Komatsu, T., & Saito, K. I. (2008). MKC-231, a choline-uptake enhancer: (1) Long-lasting cognitive improvement after repeated administration in AF64A-treated rats. Journal of Neural Transmission, 115(7), 1019–1025. https://doi.org/10.1007/s00702-008-0053-4
- Takashina, K., Bessho, T., Mori, R., Eguchi, J., & Saito, K. I. (2008). MKC-231, a choline uptake enhancer: (2) Effect on synthesis and release of acetylcholine in AF64A-treated rats. Journal of Neural Transmission, 115(7), 1027–1035. https://doi.org/10.1007/s00702-008-0048-1
- Takashina, K., Bessho, T., Mori, R., Kawai, K., Eguchi, J., & Saito, K. I. (2008). MKC-231, a choline uptake enhancer: (3) Mode of action of MKC-231 in the enhancement of high-affinity choline uptake. Journal of Neural Transmission, 115(7), 1037–1046. https://doi.org/10.1007/s00702-008-0049-0
- Malykh, A. G., & Sadaie, M. R. (2010). Piracetam and Piracetam-Like Drugs. Drugs, 70(3), 287–312. https://doi.org/10.2165/11319230-000000000-00000
- 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)acetamide on deficits of water maze learning in rats. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/8740080
- Malykh, A. G., & Sadaie, M. R. (2010). Piracetam and piracetam-like drugs: From basic science to novel clinical applications to CNS disorders. Drugs, 70(3), 287–312. https://doi.org/10.2165/11319230-000000000-00000
- 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 - General Section, 98(1), 1–13. https://doi.org/10.1007/BF01277590
- RESULTS FROM EXPLORATORY PHASE 2A TRIAL OF BCI-540 IN DEPRESSION WITH ANXIETY | https://web.archive.org/web/20111121081645/http://www.braincellsinc.com/wp-content/uploads/2010/06/BCI-PR-06142010.pdf