Coluracetam

Product Name: Coluracetam Synonyms: MKC-231; BCI-540; N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide12

General Description: Coluracetam is formally described as N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide.1 It is a synthetic, centrally acting small molecule belonging to the racetam family of nootropic (cognitive-enhancing) compounds.1 Originally synthesized in Japan in the 1990s by Mitsubishi Tanabe Pharma (under the developmental code MKC-231) and later investigated by BrainCells Inc. (as BCI-540), it has been clinically explored as a potential therapeutic for Alzheimer’s disease, ischemic neuropathy, and major depressive disorder (MDD) with comorbid generalized anxiety disorder (GAD).1

In analytical, clinical, and academic toxicology, coluracetam is utilized as a fundamental reference standard.1 It is essential for the calibration of analytical instrumentation (such as LC-MS/MS, GC-MS, and HPLC) and the development of screening methodologies to identify and quantify the substance in grey-market dietary supplements, experimental nootropic blends, or biological matrices.1

Technical Information:

• CAS Number: 135463-81-913
• Molecular Formula: C₁₉H₂₃N₃O₃1
• Formula Weight: 341.4 g/mol13
• SMILES: CC1=C(OC2=NC3=C(CCCC3)C(=C12)NC(=O)CN4CCCC4=O)C
• InChI Key: PSPGQHXMUKWNDI-UHFFFAOYSA-N1
• Formulation: Typically supplied as a neat white-to-off-white crystalline solid or as a certified reference material solution (e.g., 1 mg/mL in methanol or acetonitrile).1

Biological Action: While sharing structural similarities with classical racetams (such as piracetam), coluracetam possesses a distinct and highly specific primary mechanism of action: it acts as a potent enhancer of high-affinity choline uptake (HACU).1 HACU represents the rate-limiting step in the neuronal synthesis of the neurotransmitter acetylcholine.1 By directly enhancing this cellular uptake process—particularly in the hippocampus and cortex—coluracetam rapidly upregulates central cholinergic neurotransmission, which heavily mediates its memory-enhancing, learning, and potential neuroprotective properties.1 Furthermore, preclinical models suggest it may exhibit neurogenic properties and offer protection against glutamatergic excitotoxicity.1

Regulatory and Safety Information:

• Intended Use: This product is intended strictly for use as an analytical reference standard for forensic, toxicological, and academic research purposes.1
• Warning: This product is an unapproved investigational compound in many jurisdictions.1 It is not for human or veterinary use outside of approved clinical applications.1
• Legal Status: The regulatory status of coluracetam varies globally.1 In the United States, coluracetam is an unscheduled substance and is not controlled under the Controlled Substances Act (CSA).1 However, the Food and Drug Administration (FDA) does not recognize coluracetam as a legitimate dietary ingredient, classifying it instead as an unapproved new drug.1 The FDA has actively issued warning letters to vendors attempting to market coluracetam for human consumption or within dietary supplements.1 Procurement of the bulk material for analytical research requires no special DEA licenses, but handling must occur strictly within professional laboratory environments using appropriate Personal Protective Equipment (PPE) such as safety glasses, chemical-resistant gloves, and a laboratory coat.1