RESEARCH MONOGRAPH · KDC-MN-030
Coluracetam
Coluracetam is a quinoline-fused racetam developed by BrainCells Inc. for major depressive disorder. It enhances high-affinity choline uptake. Phase 2 trials were inconclusive. Not stocked by Kodiac. This monograph is provided for research and educational reference.
Intrigue 0–100 blends mechanism novelty, evidence strength, and translational potential. Kodiac editorial, not peer-reviewed.
Quinoline-fused pyrrolidinone racetam
A quinoline-fused racetam developed by Mitsubishi Tanabe and licensed to BrainCells for major depressive disorder, characterized by selective high-affinity choline uptake enhancement.
Abstract
Coluracetam (BCI-540, MKC-231; N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide; CAS 135463-81-9; molecular formula C19H23N3O3; molecular weight 341.41) is a fused-ring racetam developed by Mitsubishi Tanabe Pharma and subsequently licensed to BrainCells Inc for clinical evaluation in major depressive disorder and generalized anxiety disorder. The structural innovation is the fusion of a tetrahydrofuro-quinoline scaffold to the pyrrolidinone-acetamide racetam core, which produces a substantially different pharmacology relative to the open-chain racetams. The principal mechanism is selective enhancement of high-affinity choline uptake into cortical synaptosomes; the compound increases choline transport Vmax through a sustained mechanism that produces persistent elevation of extracellular acetylcholine in regions of high cholinergic demand. Notably, the choline uptake enhancement persists for hours to days after a single dose in animal models, distinguishing the compound from short-acting cholinergic enhancers. BrainCells advanced the compound through Phase 2 in major depressive disorder; results were modest and the program did not advance to Phase 3. The compound is not approved by any regulatory authority and is sold as a research chemical in jurisdictions where it is not specifically scheduled. Pharmacokinetics: plasma half-life of the parent compound is short (1 to 3 hours) but the choline uptake enhancement effect persists substantially longer due to the mechanism of action. The research-grade literature reports dose ranges of approximately 3 to 20 mg. Visual perceptual changes (color enhancement, increased visual contrast) are reported anecdotally and may relate to retinal cholinergic effects; the mechanism for these reports is not formally established.
Mechanism of action
Selective enhancement of high-affinity choline uptake; increases choline transport Vmax with persistent effect (hours to days after a single dose).
Reported research dose ranges
Research-grade literature reports a range of approximately 3 to 20 mg.
References
- Murai S, et al. MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium in rats. J Neural Transm 1994.
- Bessho T, et al. MKC-231, a choline-uptake enhancer: long-lasting effects on transmitters and receptors in scopolamine-induced cognitive impairment. J Neural Transm 2008.
- BrainCells Inc. Phase 2 study of BCI-540 in major depressive disorder. Clinical trial archive.
Read the full monograph
The full reference document covers compound identification, discovery and developmental history, mechanism of action, pharmacokinetics, reported research dose ranges, sourcing and quality verification, reconstitution and handling, stack interaction considerations, and a curated reference list. Available as a research-use-only PDF download.
The full reference document is provided strictly for research use only. It reports research dose ranges from the published literature, not instructions for use in humans or animals.
FOR RESEARCH USE ONLY. Not for medical, diagnostic, or therapeutic purposes. Not for human consumption. All information is provided for research and educational purposes only.