Coluracetam

PRODUCT DESCRIPTION

Introduction

Coluracetam (INN; development code BCI-540; formerly MKC-231) is a nootropic agent belonging to the racetam family. Initially developed by Mitsubishi Tanabe Pharma Corporation for Alzheimer’s disease, it has since been studied for potential use in cognitive enhancement, major depressive disorder (MDD), and generalized anxiety disorder (GAD). Coluracetam acts by enhancing high-affinity choline uptake (HACU), the rate-limiting step in acetylcholine synthesis, thereby promoting memory and learning functions. It has shown promise in reversing cholinergic deficits and may have neuroprotective effects useful in neurological disorders like schizophrenia.

Chemical Properties and Specifications

2.1 Structural and Molecular Characteristics

• Chemical Formula: C19H23N3O3

• Molecular Weight: 341.4 g/mol

• CAS Number: 135463-81-9

• IUPAC Name: N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide

• Synonyms:

  • Coluracetam

  • BCI-540

  • MKC-231

2.2 Physical Properties and Purity Standards

• Appearance: White crystalline powder

• Purity: ≥98% pharmaceutical grade

• Solubility: Soluble in DMSO (~68 mg/mL), ethanol; preparation protocols recommend sonication for dissolution

• Storage Recommendations: Store at -20°C for powder; solutions stored at -80°C for maximal shelf life; protect from moisture and light

Pharmacological Profile and Mechanism of Action

3.1 Mechanism of Action

Coluracetam enhances high-affinity choline uptake by upregulating choline transporter function in cholinergic neurons, increasing acetylcholine synthesis, thereby improving cholinergic neurotransmission. This effect supports learning, memory, and cognitive function. It also demonstrates neuroprotective properties and can mitigate deficits induced by cholinergic neurotoxins.

3.2 Research Applications

Coluracetam is widely used in cognitive neuroscience, neurodegenerative disease research, and neuropharmacology to investigate cholinergic system enhancement, cognitive recovery, and potential treatments for depression and anxiety. It is also valuable for studying neuroprotective mechanisms in CNS injury and disease models.

Comparative Analysis with Related Compounds

4.1 Compared to Other Racetams

Coluracetam differs from piracetam and aniracetam by its unique mechanism enhancing high-affinity choline uptake and neurotrophic effects. It has higher potency and longer-lasting cognitive enhancement in animal models.

4.2 Advantages for Research

High purity and stability facilitate reproducible experimental outcomes. Multiple formulation options, including powders and solutions, support diverse dosing strategies and research methodologies.

Safety and Handling Guidelines

5.1 Laboratory Safety

Use gloves, lab coat, and goggles when handling powders or solutions. Employ proper ventilation or fume hoods to minimize exposure.

5.2 Disposal and Environmental Considerations

Dispose of unused materials following hazardous pharmaceutical waste protocols. Prevent environmental contamination.

5.3 Regulatory Status

Coluracetam is not approved for medical use in many countries and is classified as a research chemical. Verify local legal status before acquisition or use.

Frequently Asked Questions (FAQs)

1. What is Coluracetam used for?
   Cognitive enhancement, neuroprotection, and treatment evaluation for depression and anxiety.

2. How does Coluracetam work?
   Enhances high-affinity choline uptake, increasing acetylcholine synthesis.

3. What is the purity level?
   Typically ≥98% pharmaceutical grade.

4. Is Coluracetam water soluble?
   Mostly soluble in DMSO and ethanol, limited aqueous solubility.

5. Is Coluracetam legally approved for medical use?
   No, it is mainly used as a research chemical.

Conclusion

Coluracetam is a potent racetam nootropic that enhances cholinergic neurotransmission through increased high-affinity choline uptake. Its neuroprotective and cognitive-enhancing properties make it an important compound for neuroscience and pharmacological research. It requires careful handling in well-controlled research environments with compliance to local regulations.