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|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.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
A prominent experience amongst coluracetam's effects is its ability to enhance the immediate five senses.
- Stimulation - The stimulation which coluracetam presents can be considered as primarily subtle and short lasting, comparable to that of caffeine.
- Anxiety suppression
- Thought connectivity
- Focus enhancement
- Immersion enhancement
- Motivation enhancement
- Memory enhancement
- Dream potentiation
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 noopept and piracetam may have a reduced effect.
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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