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'''Coluracetam''' ('''BCI-540'''), formerly ('''MKC-231''') is a [[psychoactive class::nootropic]] of the [[chemical class::racetam]] family<ref>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. | https://www.ncbi.nlm.nih.gov/pubmed/8740080</ref>. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach 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 potential medication for comorbid major depressive disorder (MDD) with generalized anxiety disorder (GAD).
It is readily available and sold through online vendors as a dietary supplement in the U.S. To supplement coluracetam, one should take 5 – 20 mg at once. Dosages range nearly half of that of [[noopept]], making it twice as potent while offering comparable benefit. Due to it's short acting and acute nature, the preferred ROA is generally [[insufflation]], [[sublingual]], or [[vaporising]], though it is still active orally.
'''Coluracetam''' ('''BCI-540'''; formerly '''MKC-231''') is a [[psychoactive class::nootropic]] belonging to the [[chemical class::racetam]] family of drugs.<ref>{{cite journal | vauthors=((Bessho, T.)), ((Takashina, K.)), ((Tabata, R.)), ((Ohshima, C.)), ((Chaki, H.)), ((Yamabe, H.)), ((Egawa, M.)), ((Tobe, A.)), ((Saito, K.)) | journal=Arzneimittel-Forschung | title=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 | volume=46 | issue=4 | pages=369–373 | date= April 1996 | issn=0004-4172}}</ref> 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 [[Routes_of_administration|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.
This compound's active dose range is between 5 and 20 mg. This is much smaller than the comparative doses of the racetam class of drugs ([[piracetam]], [[oxiracetam]], [[phenylpiracetam]], etc.) Dosages higher than 20mg do not appear to offer any additional benefit.
==Chemistry==
==Chemistry==
Coluracetam, or 2-(2-oxopyrrolidin-1-yl)-N-(2, 3-dimethyl-5, 6, 7, 8-tetrahydrofuro2, 3-b quinolin-4-yl)acetoamide, is a synthetic [[racetam]]. A known metabolite is hydroxylated coluracetam on the 2-carbon of the pyrrolidinone backbone, it is sometimes referred to as M-MKC-231. It appears inactive on the main mechanism of action coluracetam is known for (increasing HACU).
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 R<sub>2</sub>.<ref>{{cite journal | vauthors=((Malykh, A. G.)), ((Sadaie, M. R.)) | journal=Drugs | title=Piracetam and Piracetam-Like Drugs: From Basic Science to Novel Clinical Applications to CNS Disorders | volume=70 | issue=3 | pages=287–312 | date= February 2010 | url=http://link.springer.com/10.2165/11319230-000000000-00000 | issn=0012-6667 | doi=10.2165/11319230-000000000-00000}}</ref> 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 R<sub>N</sub> 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 R<sub>2</sub> and R<sub>3</sub> of the structure on the furan ring. Coluracetam is structurally analogous to [[piracetam]] with an added fluoroquinolone group.
==Pharmacology==
==Pharmacology==
Coluracetam enhances high-affinity choline uptake (HACU),<ref>MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice | http://link.springer.com/article/10.1007%2FBF01277590</ref> which is the rate-limiting step of acetylcholine (ACh) synthesis.
Coluracetam enhances high-affinity [[choline]] uptake (HACU),<ref>{{cite journal | vauthors=((Murai, S.)), ((Saito, H.)), ((Abe, E.)), ((Masuda, Y.)), ((Odashima, J.)), ((Itoh, T.)) | journal=Journal of Neural Transmission | title=MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice | volume=98 | issue=1 | pages=1–13 | date= February 1994 | url=http://link.springer.com/10.1007/BF01277590 | issn=0300-9564 | doi=10.1007/BF01277590}}</ref> 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.
However, the role of these interactions and how they result in the compound's effects continues to remain elusive.
==Subjective effects==
==Subjective effects==
The effects listed below are based upon the [[subjective effects index]] and personal experiences of [[PsychonautWiki]] [[Special:TopUsers|contributors]]. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of 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.
====Sensory effects====
{{Preamble/SubjectiveEffects}}
A prominent experience amongst Coluracetam's effects is it's ability to enhance the immediate five senses.
{{effects/base
*'''[[Effect::Acuity enhancement]]''' - Most prominent for most users is coluracetam's visual effects, users describing it as "widescreen HD vision."
*'''[[Effect::Colour enhancement]]''' - Coluracetam has been described to make colours appear more vibrant.
*'''[[Effect::Auditory enhancement]]''' - Some users describe a better and crisper perception of sounds.
*'''[[Effect::Mindfulness]]''' - Coluracetam can invoke the first component of mindfulness, or an enhanced perception of immediate environment, while being remaining absent of mindfulness's second component.
*'''[[Effect::Tactile enhancement]]''' - Coluracetam may promote a heightened awareness of textures of objects as well as the sensations of the body.
*'''[[Effect::Brightness alteration]]''' - Secondary to color enhancement, users may feel an enhanced sense of brightness of scenery.
====Physical effects====
|{{effects/physical|
*'''[[Effect::Stimulation]]''' - The stimulation which Coluracetam presents can be considered as primarily subtle and short lasting, comparable to that of [[caffeine]].
*'''[[Effect::Stimulation]]''' - The stimulation which coluracetam presents can be considered as primarily subtle and short lasting, comparable to that of [[caffeine]].
}}
====Cognitive effect====
{{effects/sensory|
*'''[[Effect::Cognitive euphoria]]'''
A prominent experience amongst coluracetam's effects is its ability to enhance the immediate five senses.
*'''[[Effect::Acuity enhancement]]'''
*'''[[Effect::Colour enhancement]]'''
*'''[[Effect::Auditory enhancement]]'''
*'''[[Effect::Mindfulness]]'''
*'''[[Effect::Tactile enhancement]]'''
}}
|{{effects/cognitive|
*'''[[Effect::Wakefulness]]'''
*'''[[Effect::Wakefulness]]'''
*'''[[Effect::Anxiety suppression]]'''<ref> 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</ref>
*'''[[Effect::Thought connectivity]]'''
*'''[[Effect::Thought connectivity]]'''
*'''[[Effect::Focus enhancement]]'''
*'''[[Effect::Focus enhancement]]'''
*'''[[Effect::Immersion enhancement]]'''
*'''[[Effect::Motivation enhancement]]'''
*'''[[Effect::Motivation enhancement]]'''
*'''[[Effect::Memory enhancement]]'''
*'''[[Effect::Memory enhancement]]'''
*'''[[Effect::Rejuvenation]]'''
*'''[[Effect::Dream potentiation]]'''
*'''[[Effect::Anxiety suppression]]'''
}}
*'''[[Effect::Irritability]]'''
}}
===Experience reports===
There are currently no anecdotal reports which describe the effects of this compound within our [[experience index]]. Additional experience reports can be found here:
There are no known long-term dangers or health safety issues. However, there are a small number of people who suffer from nausea, depression, and the inability to sleep. It is recommended to cease usage immediately if these side effects are experienced.
The toxicity and long-term health effects of recreational coluracetam use do not seem to have been studied in any scientific context and the [[Toxicity::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).
===Lethal dosage===
The median lethal dosage (LD50) of coluracetam has not been officially published as it has low abuse potential, but the recommended dosage is 10mg once to three times a day. Anecdotal evidence from people within the community who have tried coluracetam suggests that there are no negative health effects attributed to simply trying the drug by itself at low to moderate doses and using it very sparingly (but, as per most substances, nothing can be completely guaranteed). [https://www.google.com/ Independent research] should always be done to ensure that a combination of two or more substances is safe before consumption.
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this substance.
It is strongly recommended that one use [[responsible use|harm reduction practices]] when using this drug.
===Tolerance and addiction potential===
===Tolerance and addiction potential===
There is a slight tolerance with coluracetam which builds up with repeated usage, though preliminary reports may demonstrate a lasting promotion of efficient Cholinergic Neurotransmission, promoting a downregulation of a rate-limiting step of acetylcholine synthesis. There does not seem to be any addictive potential.
The chronic use of Coluracetam can be considered as [[Addiction potential::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 [[Time to full tolerance::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 [[Time to half tolerance::3 - 7 days]] for the tolerance to be reduced to half and [[Time to zero tolerance::1 - 2 weeks]] to be back at baseline (in the absence of further consumption). Coluracetam may presents cross-tolerance with [[Cross-tolerance::all [[racetam]] [[nootropic]]s]], meaning that after the consumption of Coluracetam certain [[nootropics]] such as [[aniracetam]] and [[piracetam]] may have a reduced effect.
===Dangerous Interactions===
{{DangerousInteractions/Intro}}
{{DangerousInteractions/Depressants}}
==Legal issues==
==Legal status==
{{legalStub}}
{{legalStub}}
Coluractam, being a member of the [[racetam]] family, currently is legally available to buy and sell in most countries, but may still vary by region.
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.
==Literature==
* 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
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Coluracetam (BCI-540; formerly MKC-231) is a nootropic belonging to the racetam family of drugs.[1] 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.[2] 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.
Pharmacology
Coluracetam enhances high-affinity choline uptake (HACU),[3] 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.
Subjective 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), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also 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 increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects
Stimulation - The stimulation which coluracetam presents can be considered as primarily subtle and short lasting, comparable to that of caffeine.
Sensory effects
A prominent experience amongst coluracetam's effects is its ability to enhance the immediate five senses.
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
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).
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 [[Cross-tolerance::all racetamnootropics]], meaning that after the consumption of Coluracetam certain nootropics such as aniracetam and piracetam may have a reduced effect.
Dangerous Interactions
Warning:Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).
Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
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.
Stimulants - 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.
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.
Literature
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
↑Bessho, T., Takashina, K., Tabata, R., Ohshima, C., Chaki, H., Yamabe, H., Egawa, M., Tobe, A., Saito, K. (April 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. ISSN0004-4172.
