Racetam

Coluracetam

Coluracetam (MKC-231)

Evidence TierDWADA NOT PROHIBITED

tuneTypical Dose

20-80 mg per day (sublingual or oral)

watchEffect Window

Acute effects within hours (anecdotal). Sustained HACU enhancement shown in repeated-dose animal studies.

check_circleCompliance

WADA NOT PROHIBITED

Overview

Clinical Summary

Coluracetam is an investigational nootropic linked to high-affinity choline uptake mechanisms. It is used for memory, attention, and mood-related cognitive symptoms, with limited clinical validation.

Human evidence is limited, with small studies suggesting possible effects on memory and mood in select groups. Preclinical research indicates neuroprotective and sensory-processing effects. Minority claims include reduced anxiety and improved visual perception, largely anecdotal. Overall support remains preliminary, with limited replication and uncertain long-term safety at common nonclinical exposures.

Enhances high-affinity choline uptake (HACU) via CHT1 transporter upregulation, increasing presynaptic acetylcholine synthesis. Distinct from other racetams which primarily modulate AMPA receptors.

Outcomes

What This Is Expected To Influence

Primary Outcomes

  • Reversed AF64A-induced learning deficits in rats via HACU enhancement
  • Phase 2a MDD/GAD trials conducted but results never published in peer-reviewed literature

Secondary Outcomes

  • Persistent HACU upregulation after washout in repeated-dose animal protocol
  • Anecdotal reports of color/vision enhancement lack scientific basis

Safety

Contraindications and Interactions

Contraindications

  • Pregnancy
  • Lactation
  • Severe renal impairment
  • Severe hepatic impairment

Side effects

  • Headache (anecdotal)
  • Nausea (anecdotal)
  • Fatigue (anecdotal)

Interactions

  • Anticholinergic medications (opposing mechanism)
  • Acetylcholinesterase inhibitors (additive cholinergic effect)

Avoid if

  • Cholinergic hypersensitivity
  • Epilepsy (no seizure safety data)
  • Concurrent multiple racetam use

Evidence

Study-level References

coluracetam-SRC-001Animal study
Sourceopen_in_new

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. doi:10.1007/s00702-008-0053-4. PMID:18461272.

Population: AF64A-treated male Wistar rats with cholinergic lesion-induced learning impairment

Dose protocol: MKC-231 (coluracetam) administered orally over 8 days to AF64A-treated rats. Water maze testing at 1, 24, 48, and 72 hours after the final dose.

Key findings: Significant cognitive improvement persisted for 24 hours after the last dose, even though MKC-231 was no longer detectable in the brain. High-affinity choline uptake remained elevated across the same timeframe, indicating lasting changes to choline transporter regulation rather than direct pharmacological action.

Notes: This is the primary published evidence for coluracetam. All human-facing claims trace back to this single animal study.

Paper content

Repeated oral administration of MKC-231 in AF64A-treated rats produced cognitive improvement lasting up to 24 hours after the last dose, even though the compound was no longer detectable in the brain. HACU was similarly elevated, suggesting MKC-231 may induce long-lasting procognitive effects by altering choline transporter regulation rather than through direct receptor occupancy.

coluracetam-SRC-002Unpublished phase 2a human trial

BrainCells Inc. phase 2a coluracetam trial in major depressive disorder with comorbid generalized anxiety disorder. Results referenced only in company communications; no peer-reviewed publication.

Population: Adults with major depressive disorder and comorbid generalized anxiety disorder.

Dose protocol: Oral coluracetam. Specific dose and duration not publicly disclosed in detail.

Key findings: Trial did not meet primary endpoints for MDD Some signal noted in comorbid anxiety subgroup per company communication

Notes: Results were never published in a peer-reviewed journal. BrainCells Inc. subsequently ceased operations. Data may be inaccessible for independent verification.

Paper content

This record exists only so the catalog can represent the unpublished human coluracetam trial transparently. The study was referenced in company communications, reportedly missed its primary depression endpoint, and never produced a peer-reviewed paper. It should be treated as an unverifiable historical note rather than affirmative efficacy evidence.

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