Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H23N3O3 |
Molecular Weight | 341.4042 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C)C2=C(NC(=O)CN3CCCC3=O)C4=C(CCCC4)N=C2O1
InChI
InChIKey=PSPGQHXMUKWNDI-UHFFFAOYSA-N
InChI=1S/C19H23N3O3/c1-11-12(2)25-19-17(11)18(13-6-3-4-7-14(13)20-19)21-15(23)10-22-9-5-8-16(22)24/h3-10H2,1-2H3,(H,20,21,23)
DescriptionSources: http://www.braintropic.com/nootropics/coluracetam/Curator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800001490
https://examine.com/supplements/coluracetam/
http://www.studydrugs.net/Coluracetam-Review.html
Sources: http://www.braintropic.com/nootropics/coluracetam/
Curator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800001490
https://examine.com/supplements/coluracetam/
http://www.studydrugs.net/Coluracetam-Review.html
Coluracetam (code name BCI-540; formerly MKC-231) 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). Like most racetam compounds, Coluracetam increases choline uptake, but it also increases uptake in damaged neurons. Specifically, Coluracetam interacts with the HACU process, which is responsible for absorbing choline into the neurons. This increased uptake occurs during the Acetylcholine synthesis process. Since Coluracetam improves choline preservation during this process, a larger amount is converted into Acetylcholine. This results in increased memory, attention and alertness. It is important to note here, that these benefits were only seen in subjects with previously impaired neurons, not in subjects with normally functioning neurons. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness. Although Coluracetam interacts with choline transporters as well, there isn’t enough evidence to explain why or how this interaction occurs, or what occurs after the interaction. Coluracetam has been in phase II clinical trials for the treatment of major depression and anxiety. However, this research has been discontinued.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: High-affinity choline uptake |
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Target ID: CHEMBL5797 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18461273 |
2.0 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.braintropic.com/nootropics/coluracetam/
A dosage of 240mg (split into three daily doses of 80mg) was useful in treating major depression co-morbid with GAD (generalized anxiety disorder).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18461273
Incubation of synaptosomes with MKC-231 (Coluracetam) (10(-8) M) significantly increased Vmax without significant change in the Km of AF64A-treated rats
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C1509
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ACTIVE MOIETY