|Synonyms:||BCI-540, MKC-231, N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide|
|Molecular Weight:||341.411 g/mol|
|Appearance:||White to off-white powder|
|Storage:||Store in a dry, dark, sealed container at room temperature.|
|Stability:||Stable at least for 2 years when stored probably.|
Coluracetam is a compound belonging to the racetam family. It was originally developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer’s disease. After the drug had failed to reach the endpoints in its clinical trials, it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD), which was preceded by being awarded a “Qualifying Therapeutic Discovery Program Grant” by the state of California. Findings from phase IIa clinical trials have suggested that it would be a possible medication for a comorbid major depressive disorder (MDD) with generalized anxiety disorder (GAD).
Coluracetam is a synthetic compound of the racetam family. Racetams share a pyrrolidine nucleus, a five-member nitrogenous ring with a ketone bonded oxygen at R2. This 2-pyrrolidone ring is bound to the terminal carbon of an acetamide group, an ethyl amide chain with a ketone bond (C=O) at the alpha carbon. Coluracetam features an additional three-ring substituted fluoroquinolone component bonded to RN of the acetamide group. The fluoroquinolone group is comprised of a central nitrogenous pyridine ring fused to a benzyl and furan ring on either side. Two methyl groups are bonded to R2 and R3 of the structure on the furan ring.
Coluracetam enhances high-affinity choline uptake (HACU), which is the rate-limiting step of acetylcholine (ACh) synthesis. Studies have shown coluracetam to improve learning impairment on a single oral dose given to rats which have been exposed to cholinergic neurotoxins. Subsequent studies have shown that it may induce long-lasting procognitive effects in cholinergic neurotoxin-treated rats by changing the choline transporter regulation system.