Coluracetam - 0.3 Grams, ≥99%

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Chemical Name:     N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide
CAS Number:    135463-81-9
Purity:    ≥99%
Form:    White or off-white powder
Molecular Weight:    341.40 g/mol
Melting Point:    128-131°C
Molecular Formula:    C19H23N3O3
Synonyms:     BCI-540, MKC-231

Coluracetam is a nootropic compound in the racetam family, with a unique enhancing effect on high affinity choline uptake.

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Coluracetam (BCI-540) 0.3 Grams, ≥99%

Chemical Information:

CAS Number: 135463-81-9
Purity: ≥99%
Molecular Weight: 341.40 g/mol
Melting Point: 128-131°C
Molecular Formula: C19H23N3O3
Synonyms: N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide, MKC-231
PubChem CID: 214346

Technical Information:

Application: Coluracetam (BCI-540) is a nootropic compound of the racetam family.
Appearance: White or off-white powder
Physical State: Solid
Solubility: Soluble to 50 mM in Ethanol, insoluble in Water.
Storage: Store at room temperature or cooler, in a sealed airtight container, protected from heat, light and humidity.
Stability: Stable for at least two years when stored as above.


Biochemical Activity:

Coluracetam (BCI-540, MKC-231) is a nootropic drug in the racetam family1,2.  Like other racetams, Coluracetam has AMPA potentiating activity3 but has an additional, unique mechanism of action that sets it apart from canonical racetam compounds such as Piracetam2,3.  Coluracetam is currently used in neuroscience research related to the choline transporter system, protection against cognitive impairment, and neurochemical pathways for development of novel antidepressants.

Coluracetam is unique as a normalizer and enhancer of high afinity choline uptake (HACU), and is thus far the only known compound possessing this property.  Choline uptake is the process by which choline is transported from the synapse into the presynaptic neuron, allowing fresh acetylcholine to be synthesized for subsequent release. Agents which impair high afinity choline uptake (HACU) disrupt learning and neurological function.

Coluracetam was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation as a treatment for Alzheimer's disease1, and was later in-licensed by BrainCells Inc. for development as a treatment of Major Depressive Disorder3.

In randomized, double-blind and placebo-controlled human clinical trials with 101 evaluable patients conducted by BrainCells Inc., for the treatment of major depressive disorder (MDD) with anxiety, coluracetam was dosed orally at 80 mg total daily, and was well tolerated at this dose.  Patients with comorbid depression (MDD) and anxiety (GAD) who were dosed in three divided doses daily showed a greater rate of beneficial response vs. placebo at week six, as measured by the Hamilton Rating Scales for Anxiety (HAM-A) and Depression (HAM-D).3

Coluracetam has shown nootropic and neuroprotective effects in a number of animal studies, particularly those in which the cholinergic system has been impaired.  In a series of studies, Coluracetam was administered to mice and rats who had been treated with ethylcholine mustard aziridinium ion (AF64A), a neurotoxin which produces a long-lasting reduction in the activity of choline acetyltransferase and high-affinity choline transport.  In AF64A-treated mice, Coluracetam had no significant effect on memory deficits after an acute dose, but after daily administration for 11 days, Coluracetam improved memory deficit at all doses tested (0.3, 1.0, or 3.0 mg/kg p.o.), and significantly reversed hippocampal ACh depletion.4 

In AF64A-treated rats, Coluracetam was also shown to significantly repair the reduction of acetylcholine (ACh) release and basal ACh concentrations at 10 mg/kg p.o.5  In the same model, Coluracetam produced long lasting improvement in HACU and cognitive performance after chronic administration (1 and 3 mg/kg, p.o., for 8 days), with both effects significant up to 2 days after the last dose (when Coluracetam was no longer detectable in the brain).6  Coluracetam significantly increased HACU in the hippocampal synaptosomes of AF64A treated rats, but not normal rats, and oral administration of Coluracetam (1-10 mg/kg) to such rats significantly improved learning deficits in the Morris' water maze, without the side effects of acetylcholinesterase inhibitors.7



Precautions and Disclaimer:
This Material is Sold For Laboratory and Research Use Only.  Not for Diagnostic or Therapeutic, Drug, or Other Household Uses.

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