Coluracetam

Overview

Coluracetam is a non-peptide small-molecule racetam-family nootropic (pyrrolidinone-substituted tetrahydrofuroquinoline) that enhances high-affinity choline uptake (HACU), the rate-limiting step in acetylcholine synthesis. Originally developed by Mitsubishi Tanabe Pharma as MKC-231 for Alzheimer's disease and later by BrainCells Inc. as BCI-540 for major depressive disorder, it is not FDA-approved for any indication and remains inactive in U.S. regulatory development. Sold only as an unregulated research chemical/nootropic powder with no validated human dose or safety profile.

Mechanism of Action

Coluracetam enhances high-affinity choline uptake (HACU), the rate-limiting step in acetylcholine synthesis, by acting on the choline transporter CHT1. In AF64A-lesioned rat hippocampal synaptosomes and COS cells, it increased the Vmax of HACU 1.6-fold and the Bmax of [³H]hemicholinium-3 binding 1.7-fold, consistent with increased CHT1 trafficking to the synaptic membrane (Takashina et al. 2008, PMID 18461273). This mechanism was observed in lesioned tissue only, with no effect in non-lesioned controls.

Research Summary

No peer-reviewed or regulatory-posted human efficacy or safety data exist. One Phase 2 randomized, double-blind, placebo-controlled trial (NCT00621270) tested BCI-540 (80 mg once daily or three times daily vs. placebo) in 115 participants with major depressive disorder and concomitant anxiety (Jan 2008–Oct 2009); the trial is listed as Completed but has no results posted (hasResults=false, confirmed via ClinicalTrials.gov). In rodent models, oral coluracetam (1–10 mg/kg) significantly improved Morris water-maze learning deficits in AF64A-lesioned rats without tremor, salivation, or hypothermia, and reversed working-memory deficits and hippocampal acetylcholine depletion in AF64A-treated mice (Bessho et al. 1996, PMID 8740080; Murai et al. 1994, PMID 7710736). Coluracetam is not FDA-approved for any indication; U.S. development for Alzheimer's disease is listed as Inactive.

Vendors selling Coluracetam

Scored vendors carrying Coluracetam, ranked by trust grade. Grades are computed from indexed Certificates of Analysis. Full $/mg pricing is on the comparison page.

Reported Side Effects

• No systematic human adverse-event data published or posted
• Rodent studies reported absence of cholinergic side effects (tremor, salivation, hypothermia) vs. tacrine
• Unregulated research chemical with no guaranteed purity or identity
• Anti-doping classification unclear/inconsistent across databases
• Not FDA-approved; no validated safety profile

Compare Coluracetam with Others

Research References

• Coluracetam, Compound Summary for CID 214346.
• Safety and Effectiveness Study of BCI-540 Versus Placebo in the Treatment of Major Depressive Disorder With Concomitant Anxiety (NCT00621270). 2008.
• MKC-231, a choline uptake enhancer: (3) Mode of action of MKC-231 in the enhancement of high-affinity choline uptake. 2008. PMID 18461273.
• Effect of the novel high affinity choline uptake enhancer ... on deficits of water maze learning in rats. 1996. PMID 8740080.

Frequently asked questions

Has Coluracetam been independently lab-tested?

Disclosed Labs has collected 2 Certificates of Analysis (COA) for Coluracetam from 2 independent testing labs. 1 vendor has submitted material for testing. Products average 99.7% tested purity across the corpus. Full testing data is available at https://www.disclosedlabs.com/peptides/coluracetam/testing.

Where can researchers source Coluracetam?

1 vendor with Disclosed Labs trust grades currently list Coluracetam, including Kimera Chems. Compare live prices and lab-verified COAs at https://www.disclosedlabs.com/prices/coluracetam.

How does Coluracetam work?

Coluracetam enhances high-affinity choline uptake (HACU), the rate-limiting step in acetylcholine synthesis, by acting on the choline transporter CHT1. In AF64A-lesioned rat hippocampal synaptosomes and COS cells, it increased the Vmax of HACU 1.6-fold and the Bmax of [³H]hemicholinium-3 binding 1.7-fold, consistent with increased CHT1 trafficking to the synaptic membrane (Takashina et al. 2008, PMID 18461273). This mechanism was observed in lesioned tissue only, with no effect in non-lesioned controls.

What does the research say about Coluracetam?

No peer-reviewed or regulatory-posted human efficacy or safety data exist. One Phase 2 randomized, double-blind, placebo-controlled trial (NCT00621270) tested BCI-540 (80 mg once daily or three times daily vs. placebo) in 115 participants with major depressive disorder and concomitant anxiety (Jan 2008–Oct 2009); the trial is listed as Completed but has no results posted (hasResults=false, confirmed via ClinicalTrials.gov). In rodent models, oral coluracetam (1–10 mg/kg) significantly improved Morris water-maze learning deficits in AF64A-lesioned rats without tremor, salivation, or hypothermia, and reversed working-memory deficits and hippocampal acetylcholine depletion in AF64A-treated mice (Bessho et al. 1996, PMID 8740080; Murai et al. 1994, PMID 7710736). Coluracetam is not FDA-approved for any indication; U.S. development for Alzheimer's disease is listed as Inactive.