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Coluracetam

Well Researched

The only racetam that traffics the choline transporter itself (CHT1/SLC5A7 to the synaptic membrane) instead of modulating receptors.

Aliases (5)
BCI-540 · MKC-231 · Coluracetamum · N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide · COLURACETAM
TYPICAL DOSE
5-10 mg
1-2x
ROUTE
Oral (tablet)
Oral
CYCLE
PRN use only
As prescribed
STORAGE
Room temp; original container
Room temp

Overview

What is Coluracetam?

Coluracetam (BCI-540, MKC-231) is a racetam-class nootropic developed in Japan for Alzheimer's research. It is best known among nootropic users for choline modulation and reported visual / mood-enhancement effects.

Key Benefits

Anecdotal reports of enhanced color vibrancy and visual perception, mood lift, and improved memory consolidation. Some users report anxiolytic and antidepressant-like effects in major depression with comorbid anxiety.

Mechanism of Action

Selectively enhances high-affinity choline uptake (HACU) into cholinergic neurons, particularly in the hippocampus, even after the system is impaired. Distinct from typical racetams; effect persists after compound clearance, suggesting durable upregulation.

Pharmacokinetics

·
PeakHalf-life
Approximate curve — visual aid only, not data-precise PK
Brand options4 known
BCI-540MKC-231ColuracetamumCOLURACETAM

StatusUnscheduled (US) — research chemical, not approved for human consumption; not FDA-approved

Research Protocols

Disclaimer: These are commonly discussed research protocols and not medical advice.

Goal:PsychonautWiki dose tiers (oral):
Dose:1 mg - Light: 3-5 mg - Common: 5-10 mg - Strong: 10-20 mg - Heavy: 20+ mg
Frequency:
Solo:
Cycle:

Peptide Interactions

citicoline
Synergistic

*(already in the user's V stack at 500 mg/day)* — Citicoline raises systemic choline + provides cytidine for phospholipid synthesis. Coluracetam needs adequa…

alpha-gpc
Synergistic

Alternative choline donor; raises brain choline more aggressively than citicoline. Use this only if citicoline is not in the stack — don't double-stack alpha…

aniracetam
Synergistic

Mood-and-memory racetam with a different mechanism (AMPA receptor modulation + 5-HT2A modulation). Some users stack aniracetam 750 mg + coluracetam 10 mg for…

dha / fish oil
Synergistic

*(already in the user's V stack at 2 g/day)* — Substrate-level support for cholinergic neurons; phosphatidylcholine synthesis depends on DHA availability. No…

pramiracetam
Avoid

Both work via HACU enhancement (different binding profile but same downstream pathway). Stacking is mechanistically redundant and may push cholinergic tone t…

other HACU enhancers in development
Avoid

None on the gray market currently, but if any emerge (e.g., fresh CHT1 modulators in research), avoid stacking on the same principle.

strong AChE inhibitors (donepezil, high-dose huperzine A)
Avoid

Coluracetam raises ACh synthesis ceiling; AChE inhibitors slow ACh breakdown. Combining could produce cholinergic excess (sweating, GI cramping, fatigue). Lo…

anticholinergics (diphenhydramine, dicyclomine, scopolamine)
Avoid

Direct mechanistic opposition. No safety risk but defeats the purpose. Note that many sleep aids (Benadryl, doxylamine) are anticholinergic — separate by 6+ …

Quality Indicators

Pharmacy-dispensed, intact packaging

Prescription tablets in original sealed packaging from a licensed pharmacy.

!

Generic vs branded

Generics are usually fine but bioavailability can vary slightly; track if you switch.

Unbranded blister or counterfeit risk

Counterfeit pharmaceuticals are a known issue; verify pharmacy and lot if buying internationally.

What to Expect

  • Day 1
    PK-driven acute peak per administration. Verify dose tolerated.
  • Week 1
    Steady-state reached for most daily-dosed pharma.
  • Week 2-4
    Therapeutic effect established; titration window if needed.
  • Long-term
    Periodic monitoring per drug class (labs, BP, ECG as applicable).

Side Effects & Safety

  • Common (>10% users): Mild GI upset (nausea, indigestion) at higher doses (20 mg+) or on empty stomach. Mild headache — most often when choline cofactor is inadequate (same pattern as all racetams). Daytime sleepiness intermittently reported.

  • Less common (1-10%): Anxiety/nervousness (some users feel keyed-up rather than calmed — opposite of the typical anxiolytic report; suggests population variability in cholinergic response). Fatigue at very high doses. Mild irritability.

  • Rare-serious (<1% but worth knowing): None documented in the published literature. The Phase 2a trial at 240 mg/day for 6 weeks reported a placebo-comparable AE profile with no serious adverse events. Long-term safety data does not exist — no human use beyond the 6-week trial has been formally documented, so chronic-use safety is unknown.

  • Specific watch periods: First 1-2 doses for headache (resolve with adequate choline). First week for GI tolerance. No SJS/DRESS-type rash signals (this is not a typical concern for coluracetam).

  • Theoretical concerns: Sustained CHT1 up-regulation at the synaptic membrane is unstudied beyond 6 weeks. Whether continuous daily use causes adaptive down-regulation (coluracetam tachyphylaxis) or trafficking exhaustion is unknown. The PRN dosing pattern most users adopt likely circumvents this issue but it's not proven.

References

Coluracetam — Wikipedia

en.wikipedia.org

overview, development history, mechanism summary

View Study

Coluracetam — NCATS Inxight Drugs

drugs.ncats.io

chemical structure, CAS, NCT identifier (NCT00621270), CHT1 Kd ~2 nM, regulatory status

View Study

Coluracetam — AdisInsight

adisinsight.springer.com

clinical pipeline status, BrainCells program history

View Study

BrainCells Inc. Initiates Phase 2 Clinical Trial with BCI-540 — BioSpace

biospace.com

primary source for trial initiation; results reported subsequently with mixed primary endpoint and MDD+GAD subgroup signal

View Study

MKC-231 long-lasting cognitive improvement — Murai et al. via ResearchGate

researchgate.net

primary animal evidence for HACU mechanism and 24-hr functional duration

View Study
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