cas: 135463-81-9 Coluracetam

Coluracetam (INN; development code BCI-540; formerly MKC-231) is a purported nootropic agent of the racetam family.[1] It is contains a chemical group that is a bioisostere of the 9-amino-tetrahydroacridine family. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach 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.[2] Findings from phase IIa clinical trials have suggested that it would be a potential medication for comorbid MDD with generalized anxiety disorder (GAD).[3] BrainCells Inc is currently[when?] out-licensing the drug for this purpose.[4][full citation needed] It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.[medical citation needed]

Coluracetam has been shown to reverse the loss of choline acetyltransferase production in the medial septal nucleus of rats exposed to phencyclidine (PCP), and is considered a potential therapeutic drug for schizophrenia.[5]

Coluracetam (MKC-231) is a synthetic racetam drug purported to be a nootropic compound. It does not have a large body of evidence investigating it, but the mechanisms of action (as well as structure) appear to be very distinct from other racetam compounds like Piracetam or Aniracetam.

Coluracetam appears to interact with a process known as high affinity choline uptake (HACU for short), which is the rate-limiting step of drawing choline into a neuron for synthesis into the neurotransmitter acetylcholine. Increasing the HACU rate appears to increase the activity of cholinergic neurons, so it is a desired target for cognitive enhancement.

Interventions in rats (as there is no human evidence currently) support the usage of coluracetam at very low oral doses to preserve HACU that is otherwise impaired by the use of research drugs that are known to impair HACU. The limited evidence looking at the inherent effects of coluracetam on the HACU of normal neurons has failed to find any significant interaction.

Coluracetam has also been noted to associate with choline transporters physically, but it is not known exactly what it does once associated.

Overall, there is currently insufficient evidence to support the usage of coluracetam for cognitive enhancement. Further studies are needed to see if it has a therapeutic role in instances where HACU may be impaired (such as Alzheimer's disease).

What else is Coluracetam known as?

Note that Coluracetam is also known as:MKC-231

BCI-540

2-(2-oxypyrrolidin-1-yl)-N-(2 3-dimethyl-5 6 7 8-tetrahydrofuro(2 3-b)quinolin-4-yl)acetoamide