Anti-depressant MKC-231 Coluracetam Nootropic Raw Material Drug
|Solubility:||soluble in DMSO and Ethanol|
|1||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
structute) appear to be very distinct from other racetam compounds
like Piracetam or Aniracetam.|
|2||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.|
Coluracetam is a nootropic agent of the racetam family. It would be
a potential medication for comorbid major depressive disorder (MDD)
with generalized anxiety disorder (GAD). It may also have potential
use in prevention and treatment of ischemic retinopathy and retinal
and optic nerve injury.
Coluracetam is also considered a potential therapeutic drug for
Of the studies cited done on adult rats, the dosing schedule ranged
anywhere from 1mg/kg up to 10mg/kg in (per day) . 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.
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
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.
- 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.
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 . 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.
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|NSI-189/NSI-189 phosphate||cas 1270138-40-3|
|Beta nicotinamide mononucletide|