Coluracetam powder, also known as BCI-540; MKC-231, is a AMPA receptor agonist potentially for the treatment of major depression and anxiety. MKC-231 antagonizes phencyclidine-induced behavioral deficits and reduction in septal cholinergic neurons in rats. MKC-231 ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice.
02 Coluracetam powder (135463-81-9) video
03 Coluracetam powder Base Information
|Chemical name||N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide |
|Synonyms||Coluracetam; BCI-540; MKC-231; BCI 540; MKC 231; BCI540; MKC231.|
|Molecular Weight||341.411 g/mol|
|Appearance||white crystalline powder|
|Solubility||Soluble in DMSO|
|Storage Condition||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years)|
|Application||Coluracetam (MKC-231) is a synthetic racetam drug purported to be a nootropic compound. It does not have a large body of evidence investigating it, but the mechanisms of action (as well as structute) appear to be very distinct from other racetam compounds like Piracetam or Aniracetam.|
04 Coluracetam powder General Description
Coluracetam powder, with CAS 135463-81-9, is also known as BCI-540 and MKC-231. Coluracetam was invented in Japan and only first registered in 2005 by the Mitsubishi Tanabe Pharmaceutical Corporation, and then its patent has been transfer to BrainCells Inc.
Coluracetam powder is a brain supplement for cognitive enhancer, memory improvement as well as also treats Major Depressive Disorder(MDD) and also anxiety problems.
05 Coluracetam powder (135463-81-9) History
Coluracetam (INN) (code name BCI-540; formerly MKC-231) powder is a nootropic agent of the racetam family. 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 MDD with generalized anxiety disorder (GAD). BrainCells Inc is currently[when?] out-licensing the drug for this purpose.[full citation needed] It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.[medical citation needed]
Coluracetam has been shown to reverse the loss of choline acetyltransferase production in the medial septal nucleus of rats exposed to phencyclidine (PCP), and is considered a potential therapeutic drug for schizophrenia.
06 Coluracetam (135463-81-9) Mechanism Of Action
Coluracetam enhances high-affinity choline uptake (HACU), which is the rate-limiting step of acetylcholine (ACh) synthesis. Studies have shown coluracetam to improve learning impairment on a single oral dose given to rats which have been exposed to cholinergic neurotoxins. Subsequent studies have shown that it may induce long-lasting procognitive effects in cholinergic neurotoxin-treated rats by changing the choline transporter regulation system.
07 Benefits of Coluracetam (135463-81-9)
Coluracetam is a nootropic compound in the racetam family, with a unique enhancing effect on high affinity choline uptake.
Coluracetam can improve memory, learning, anxiety, depression, and eyesight. It has potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury. It also can improve learning impairment on a single oral dose given to rats which have been exposed to cholinergic neurotoxins.
It may induce long-lasting procognitive effects in cholinergic neurotoxin-treated rats by changing the choline transporter regulation system. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness.
08 Coluracetam (135463-81-9) side effect
Additionally, standard racetam side effects also apply to users of Coluracetam. Some people struggle with a headache due to a lack of acetylcholine (remedied by alpha GPC or citicoline). Other people have Colurracetam side effects such as overstimulation or jitteriness, nausea, or irritability.
09 Coluracetam (135463-81-9) Document Download
10 Coluracetam (135463-81-9) Reference
- Takashina K, Bessho T, Mori R, Kawai K, Eguchi J, Saito K. MKC-231, a choline uptake enhancer: (3) Mode of action of MKC-231 in the enhancement of high-affinity choline uptake. J Neural Transm (Vienna). 2008 Jul;115(7):1037-46. doi: 10.1007/s00702-008-0049-0. PubMed PMID: 18461273.
- 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. J Neural Transm (Vienna). 2008 Jul;115(7):1019-25. doi: 10.1007/s00702-008-0053-4. PubMed PMID: 18461272.
- 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. J Neural Transm (Vienna). 2008 Jul;115(7):1027-35. doi: 10.1007/s00702-008-0048-1. PubMed PMID: 18446264.
- Shirayama Y, Yamamoto A, Nishimura T, Katayama S, Kawahara R. Subsequent exposure to the choline uptake enhancer MKC-231 antagonizes phencyclidine-induced behavioral deficits and reduction in septal cholinergic neurons in rats. Eur Neuropsychopharmacol. 2007 Sep;17(9):616-26. PubMed PMID: 17467960.
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- 01. Overview
- 02. Coluracetam powder (135463-81-9) video
- 03. Coluracetam powder Base Information
- 04. Coluracetam powder General Description
- 05. Coluracetam powder (135463-81-9) History
- 06. Coluracetam (135463-81-9) Mechanism Of Action
- 07. Benefits of Coluracetam (135463-81-9)
- 08. Coluracetam (135463-81-9) side effect
- 09. Coluracetam (135463-81-9) Document Download
- 10. Coluracetam (135463-81-9) Reference