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Clr3.2

Coluracetam (BCI-540) Research

Mostly mechanism / observationalLimited safety

6 peer-reviewed studies

What the evidence says

Mostly mechanism / observational

Most Coluracetam (BCI-540) studies are mechanism or observational rather than RCTs that measure a clinical effect — keep findings provisional.

Most evidence is from mixed-quality studies published 1994–2015.

Based on 6 studies

Confidence

Low

By outcome

Memory & cognition (preclinical)
Mostly mechanism / observational5 studies
Neuroprotection & brain aging
Too few graded studies1 study
Depression & mood
Too few graded studies1 study
Anxiety & stress
Too few graded studies1 study

Older research base

Newest study from 2015

199420042015

1Animal1994

In chronic experiments, MKC-231 improved memory deficits induced by AF64A in mice.

Murai S, Saito H, Abe E · J Neural Transm Gen Sect (1994)

AF64A lesioning produced working-memory deficits and reduced hippocampal acetylcholine in mice
Chronic (but not acute) MKC-231 improved the AF64A-induced memory deficit across all doses tested (0.3-3.0 mg/kg)
Foundational rodent study linking MKC-231 to cholinergic memory rescue

2Animal1996

Oral administration of MKC-231 significantly improved the learning deficits in the Morris water maze of AF64A-treated rats.

Bessho T, Takashina K, Tabata R · Arzneimittelforschung (1996)

MKC-231 increased high-affinity choline uptake (HACU) in hippocampal synaptosomes of AF64A-treated rats but not normal rats
Oral MKC-231 (1-10 mg/kg) significantly improved Morris water-maze learning deficits in AF64A-treated rats
It did not inhibit acetylcholinesterase or muscarinic binding — a HACU-specific mechanism distinct from tacrine

3Animal2008

MKC-231 significantly reversed the reduction of high-affinity choline uptake and acetylcholine release in AF64A-treated rats.

Takashina K, Bessho T, Mori R · J Neural Transm (Vienna) (2008)

AF64A reduced HACU and high-K+-induced acetylcholine release in hippocampal synaptosomes
MKC-231 reversed the decreases in both HACU and acetylcholine release
In-vivo microdialysis confirmed MKC-231 (10 mg/kg p.o.) restored basal hippocampal acetylcholine

4In Vitro2008

MKC-231 directly affects trafficking of CHT1 and increases the number of transporters working for high-affinity choline uptake.

Takashina K, Bessho T, Mori R · J Neural Transm (Vienna) (2008)

MKC-231 increased the Vmax of HACU and Bmax of [3H]-HC-3 binding (1.6- and 1.7-fold)
[3H]-MKC-231 binding and Biacore analysis showed affinity for the cloned high-affinity choline transporter CHT1
Proposes MKC-231 enhances HACU by driving CHT1 trafficking to the synaptic membrane — the core mechanistic anchor

5Review2015

Response to ketamine is compared with other glutamate drugs including lamotrigine, amantadine, riluzole, memantine and Coluracetam.

Dutta A, McKie S, Deakin JFW · Psychiatry Res (2015)

Review of glutamate-system antidepressant candidates for major depressive disorder
Lists coluracetam among compounds investigated as potential glutamate-related antidepressants
Confirms coluracetam reached human depression research but reflects no published efficacy result

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6In Vitro1998

MKC-231 protects against glutamate neurotoxicity by suppressing the NO formation triggered by Ca2+ influx.

Akaike A, Maeda T, Kaneko S · Jpn J Pharmacol (1998)

Pre-exposure to MKC-231 ameliorated glutamate excitotoxicity in fetal-rat cortical cultures
It reduced ionomycin (calcium-ionophore) cytotoxicity but not nitric-oxide-donor cytotoxicity
Suggests a neuroprotective action via suppression of Ca2+-triggered nitric-oxide formation

View in Research Library

Coluracetam (BCI-540) Research

Mostly mechanism / observational

MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice.

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.

MKC-231, a choline uptake enhancer: (2) Effect on synthesis and release of acetylcholine in AF64A-treated rats.

MKC-231, a choline uptake enhancer: (3) Mode of action of MKC-231 in the enhancement of high-affinity choline uptake.

Ketamine and other potential glutamate antidepressants.

Protective effect of MKC-231, a novel high affinity choline uptake enhancer, on glutamate cytotoxicity in cultured cortical neurons.