Coluracetam (BCI-540, MKC-231) is an investigational racetam believed to exert procognitive effects by enhancing high-affinity choline uptake, boosting acetylcholine synthesis in the brain.

How does Coluracetam work?

Coluracetam enhances activity of the high-affinity choline uptake (HACU) system—the rate-limiting step for acetylcholine synthesis—potentially improving memory and learning.

Is Coluracetam legal and FDA approved?

Coluracetam is not FDA approved. In the US it has no legal medical status. In Australia it is Schedule 4 (prescription only).

What scientific evidence exists for Coluracetam?

Evidence for Coluracetam comes mainly from preclinical studies in rats and mice. One phase IIa trial found possible benefit in depression/anxiety, but no large human trials.

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Coluracetam

BCI-540 (MKC-231, INN: Coluracetam)

Coluracetam is a unique racetam-class compound investigated for neurocognitive and mood effects, acting as a high-affinity choline uptake enhancer. It has no FDA approval and only limited published clinical evidence.

Also known as:

ColuracetamMKC-231BCI-540

Formula

C₁₉H₂₃N₃O₃

Chemical Profile

IUPAC Name:No official IUPAC (INN: Coluracetam)

Molecular Formula:C19H23N3O3

Structure:Quinolone-pyrrolidinone scaffold, 9-amino-tetrahydroacridine bioisostere

Related Compounds:Piracetam, Aniracetam, Phenylpiracetam

PubChem CID:214346

Molar Mass:341.4 g/mol

Solubility/Dosage:Experimental only, not established

Origin:Mitsubishi (JP), BrainCells Inc.

Mechanism of Action

Coluracetam is unique among racetams in that it enhances the high-affinity choline uptake (HACU) process, which increases the biosynthetic rate of acetylcholine, a neurotransmitter central to learning and memory. This effect has been linked to improvement of working memory and learning deficits in multiple animal models.

Effect on HACU established in preclinical models (see Bessho 1996, Murai 1994).

Clinical & Preclinical Evidence

Memory & Learning Rescue in Rodents, Working Memory/Cholinergic Models

Coluracetam reverses learning and memory deficits induced by cholinergic neurotoxin exposure in animal models, with improvement shown after both single and repeated administration.

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.
Bessho T et al. Arzneimittelforschung. 1996;46(4):369-73.PMID 8740080

Choline Uptake Enhancement & Cognitive Effects

Coluracetam enhances high-affinity choline uptake (HACU) and raises acetylcholine levels in brain regions. In mice with induced cholinergic deficits, it improves working memory and hippocampal acetylcholine after both acute and chronic dosing.

MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice.
Murai S, Saito H, Abe E, et al. J Neural Transm Gen Sect. 1994;98(1):1-13.PMID 7710736

Long-lasting Cognitive Effects in Cholinergic Deficit Models

Studies indicate lasting cognitive improvement in rats following repeated administration, likely related to choline transporter regulation.

MKC-231, a choline-uptake enhancer: (1) long-lasting cognitive improvement after repeated administration in AF64A-treated rats.
Bessho T, Takashina K, Eguchi J, et al. J Neural Transm. 2008;115(7):1019–25.PMID 18461272

Protection of Cholinergic Neurons under Neurotoxic Stress

Coluracetam reverses phencyclidine-induced behavioral deficits and choline acetyltransferase neuron injury in rats, raising the possibility of future antipsychotic adjunct or neuroprotective uses.

Subsequent exposure to the choline uptake enhancer MKC-231 antagonizes phencyclidine-induced behavioral deficits and reduction in septal cholinergic neurons in rats.
Shirayama Y, Yamamoto A, Nishimura T, et al. Eur Neuropsychopharmacol. 2007;17(9):616–26.PMID 17467960

Phase IIa Trial: Comorbid Major Depressive Disorder & Generalized Anxiety

Small phase IIa exploratory trial by BrainCells, Inc. suggested potential benefit for patients with MDD/GAD, but data remain unpublished outside company releases.

BrainCells Inc. Announces Results From Exploratory Phase 2a Trial of BCI-540
Company Press Release, 2010

Safety & Side Effects

No formal clinical safety studies have been published. No major side effects reported in animal models at tested doses.

Safety profile in humans is not established.

Regulatory & Legal Status

United States

Not FDA approved for any use
Unscheduled, not lawful for sale as a supplement or medicine
Available only for research in some jurisdictions

Australia/International

Schedule 4 in Australia (Rx only)
No formal approval in EU, UK, Canada
Research chemical status elsewhere

Legal note: Coluracetam’s human use is not authorized in any country. Research use only where permitted.

Development History

Coluracetam was invented by Mitsubishi Tanabe in Japan for Alzheimer’s disease treatment, but development was discontinued after weak clinical efficacy. BrainCells Inc. briefly repurposed it for mood disorders. It remains a research compound with limited availability and no approved applications.

1994–1996

Discovery & Animal Study

2008

Long-term Effect Models

2010

MDD/GAD Phase IIa Trial Press Release

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Benefits

Enhances high-affinity choline uptake (unique among racetams)
Demonstrated procognitive effects in preclinical studies
Potential utility in mood and cognition research

Considerations

No clinical proof of efficacy
Not FDA approved/regulated
Research use only; not for human use

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Scientific References

Bessho T, Takashina K, Tabata R, Ohshima C, Chaki H, Yamabe H, et al. 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. Arzneimittelforschung. 1996;46(4):369-73.PMID: 8740080
Murai S, Saito H, Abe E, Masuda Y, Odashima J, Itoh T. MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice. J Neural Transm. 1994;98(1):1-13.PMID: 7710736
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. 2008;115(7):1019–25.PMID: 18461272
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;17(9):616-26.PMID: 17467960
BrainCells Inc. Announces Results From Exploratory Phase 2a Trial of BCI-540. 2010 Press Release.View Archived Press Release

Content above is for scientific and research purposes only. Not medical advice. Last updated: 4/12/2025.