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Coluracetam

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Other Names

N-(2,3-dimethyl-5,6,7,8- tetrahydrofuro[2,3-b] quinolin-4-yl)-2- (2-oxopyrrolidin-1-yl)acetamide, C19H23N3O3, (CAS Number) 135463-81-9, (PubChem) 214346, (ChemSpider) 185836, (ChEMBL) CHEMBL37935, MKC-231, BCI-540

Coluracetam Background

Being one of the newer entrants to the Racetam family of drugs, Coluracetam was first registered with PubChem in 2005 by the Mitsubishi Tanabe Pharma Corporation and later handed off to BrainCells Inc, who has done a majority of the testing on it, including the Phase 2A trials which were completed in 2010 [3,5].  Upon completion of the Phase 2A trials, BrainCells announced that Coluracetam showed promise as a treatment for Major Depressive Disorder co-morbid with Generalized Anxiety Disorder, but did not show significant results treating participants who only had one of those disorders [3].

Coluracetam’s Mechanism of Action

Coluracetam appears to have two well-defined mechanisms of action; the first being high-affinity choline uptake, and the other being AMPA potentiation [3].  As is the case with a few of the Racetams, Coluracetam has been show to facilitate AMPA potentiation which is known to increase alertness, memory, and learning capabilities.  What is more intriguing about Coluracetam are its high-affinity choline uptake properties; choline uptake plays a crucial role in the Acetylcholine synthesis process in the brain by acting as a rate-limiter.  This rate-limiting step allows the brain to convert choline into Acetylcholine in the neuron, and by increasing the high-affinity choline uptake the brain is more readily able to convert choline to Acetylcholine; by increasing the ability to convert choline to Acetylcholine, should in theory improve attention, memory, and wakefulness in humans.

Benefits of Coluracetam

The first noted benefit of Coluracetam is in ameliorating the effects of glutamate neurotoxicity; cortical cultures were taken from fetal rats that had been treated with a substance that causes glutamate toxicity and these cultures were treated with Coluracetam for 12 to 24 hours.  After this exposure period, it was found that Coluracetam ameliorated the effects of the exposure [1].

The second noted benefit of Coluracetam was in reducing the effects of learning deficits in rats, using the Morris Water Maze as a test.  Adult rats in the experimental group were treated with a cholinergic neuron-specific neurotoxin and the control group was a population of healthy rats.  In the experimental group, Coluracetam greatly reduced the learning deficits associated with the administration of the neurotoxin without causing any expected side effects such as tremor, hypothermia, or salivation. It would appear from this study that Coluracetam had less of an effect on the control group (the healthy rats) than it did on the experimental group [2].

During the Phase 2A trials of Coluracetam by BrainCells Inc, it was noted that 80mg of Coluracetam administered three times per day was somewhat effective in treating Major Depressive Disorder co-morbid with Generalized Anxiety Disorder in those who had no positive effects from at least two other anti-depressants in the past.  In the basic group (those administered Coluracetam at 80mg once per day), no significant effects were found compared to placebo; but at 80mg TID, 36% of participants saw a marked improvement in the test used to assess depression [3].

The final noted benefit of Coluracetam is long-term improvements in learning-impaired individuals; rats were given treated with the substance AF64A which is a cholinergic neuron-specific neurotoxin, and then given repeated doses of Coluracetam for 8-days at 3mg/kg/day.  The researchers found that even 72 hours after the final administration of Coluracetam, the learning impaired rats still showed improvements in their abilities in the Morris Water Maze.  During this experiment, the researchers also tested whether or not Coluracetam was found in the rats system at the time of Water Maze testing; they found that even though the rats were still exhibiting positive effects from the last administration, the concentrations of Coluracetam in their systems were negligible [4].

Coluracetam Dosing

Of the studies cited done on adult rats, the dosing schedule ranged anywhere from 1mg/kg up to 10mg/kg in (per day) [4].  At the high end of that range, the dosing (accounting for Allometric scaling) in an average adult human would be equivalent to 2.9mg/kg; this would work out to 203.5mg/day for someone of an average weight [2].

BrainCells Inc. also recently concluded Phase 2A trials of Coluracetam, under the name BCI-540, where they administered up to 80mg three times per day for Major Depressive Disorder in adult humans (or 1.14mg/kg in an average weight human); 36% of participants showed improvements in their scores on two tests for MDD [3].

Coluracetam Toxicity

Phase 2A trials conducted by BrainCells Inc. found that 80mg of Coluracetam administered three times per day yielded no negative side effects, so at the time of this writing that is the highest suggested dosing schedule for Coluracetam [3].

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References

[1] http://www.ncbi.nlm.nih.gov/pubmed/9541286

[2] http://www.ncbi.nlm.nih.gov/pubmed/8740080

[3] http://www.braincellsinc.com/wp-content/uploads/2010/06

[4] http://www.ncbi.nlm.nih.gov/pubmed/18461272

[5] http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=214346