Coluracetam

Key Takeaways

1. Coluracetam is a fat-soluble nootropic, more potent than Piracetam, in the racetam class.
2. It boosts brain choline conversion to acetylcholine (ACh), improving learning, memory, alertness, and attention.
3. Coluracetam may act as an ampakine, producing stimulant-like effects without typical stimulant side effects.
4. It exhibits anxiolytic qualities and has potential in treating depressive disorders without affecting serotonin levels.
5. Benefits include restoring acetylcholine synthesis, improving memory, relieving severe depression and anxiety, repairing retinal and optic nerve damage, and enhancing mood and cognition.

Coluracetam (BCI-540, or MKC-231) is a fat-soluble nootropic in the racetam-class of compounds. Coluracetam is much more potent than the original racetam, Piracetam.

Coluracetam was patented by Mitsubishi Tanabe Pharma of Japan in 2005. Making it one of the newest racetam-based nootropics.

The patent for Coluracetam was later sold to BrainCells, Inc. in San Diego, California. BrainCells is a small, privately-held biopharmaceutical company specializing in developing compounds for the treatment of major depressive disorder (MDD), treatment resistant depression (TRD), and Alzheimer’s Disease.

Coluracetam is similar in structure to Piracetam. And like all racetam nootropics, has a pyrrolidone nucleus at its core. The latest clinical research indicates potential for treating depressive disorders, and retinal and optic nerve damage.

Coluracetam is a very strong choline targeting supplement. It boosts your brain’s choline conversion to acetylcholine (ACh) through the high affinity choline uptake (HACU) process. Which increases alertness, attention to detail and memory.

Some research, and personal experience shows Coluracetam may affect AMPA receptors. Making it a potential ampakine nootropic. Which could explain the stimulant-like effects without the side effects of traditional stimulants.

Coluracetam also shows some anxiolytic (anti-anxiety) qualities helping improve mood and quieting anxiety.

Coluracetam helps:

• Brain Optimization: Coluracetam is a choline uptake enhancer which boosts the effects of choline in your brain. It increases the production of acetylcholine (ACh) through HACU. Resulting in better learning and memory.[i]
• Neurotransmitters: Coluracetam reduces glutamate toxicity in your brain.[ii] Which boosts neural signaling by increasing the effectiveness of glutamate. Resulting in better focus and concentration.
• Mood & Anti-anxiety: Coluracetam is effective in treating anxiety and depression. Even in people suffering from major depression and who do not respond to SSRI’s.

Overview

Coluracetam is in the racetam-family of nootropic compounds. It is a fat-soluble nootropic. The racetam-class of nootropics share a pyrrolidone nucleus at their core.

Coluracetam is a High Affinity Choline Uptake Enhancer

Coluracetam is unique among the racetams in the way it targets choline in the brain. It boosts your brain’s choline conversion to acetylcholine (ACh) through the high affinity choline uptake (HACU) process.

Pramiracetam is the only other racetam that has a similar mechanism of action. By influencing the HACU process.

Coluracetam is one of the newest synthetic nootropic compounds. It is known for improving long-term memory and mood. And for enhancing sounds and color.

Coluracetam is considered to be much more potent than Piracetam. And suggested doses are much smaller – often in the 3 – 10 mg range.

Coluracetam helps increase attention span, alertness and boosts long-term memory.

Coluracetam acts like an ampakine nootropic although this hasn’t been verified in clinical trials. Ampakines tend to have a stimulant effect. But do not produce the same stimulant side effects as Ritalin or coffee.

Coluracetam vs. Piracetam: What’s the Difference?

Piracetam, the original racetam that started the nootropic movement, is a cyclic derivative of GABA. It affects the neurotransmitter acetylcholine (ACh) by helping ACh receptors accept, or be more sensitive to acetylcholine.

Coluracetam also boosts acetylcholine in the brain. But through a different mechanism of action. Rather than making the ACh receptors more sensitive to ACh, it actually increases the synthesis of acetylcholine from choline. By affecting the high affinity choline uptake (HACU) process.

How does Coluracetam Work in the Brain?

Coluracetam boosts brain health and function in several ways. But two in particular stand out.

1. Coluracetam boosts your brain’s choline uptake by targeting and working with the high affinity choline uptake (HACU) process in the brain’s neurons.

Acetylcholine (ACh) is made up of choline and acetate. These must be available to the neuron terminal at all times. So that ACh can be synthesized whenever it is needed.

Free choline circulating in the blood crosses the blood-brain barrier. And is taken up by cholinergic neuron terminals. It gets taken into the neuron by the high affinity choline uptake (HACU) system.[iii]

The synthesis of ACh takes place in the synaptic cleft. The space between neurons as it travels into the neuron. In animal experiments, Coluracetam has been shown to reverse decreased hippocampal acetylcholine induced by a reduction in high affinity choline uptake.

The HACU system is temperature-, energy-, and sodium-dependent. This system is the primary means by which choline needed for the synthesis of ACh is transported into the neuron. And is the rate-limiting step in the production of this critical neurotransmitter.[iv]

When this system breaks down or doesn’t work as efficiently as it was designed, you experience problems with memory, learning, and brain fog.

Coluracetam effects this process (ameliorates working memory deficits) and helps it work more efficiently. In fact, it seems to boost the HACU process. Even in damaged neurons.

Increased acetylcholine in neurons helps improve memory, boosts cognition and provides better decision-making capabilities.

2. Coluracetam also seems to improve AMPA potentiation. AMPA receptors are affected by glutamate. Which works in the brain and central nervous system to improve alertness and cognition.

Coluracetam works with both AMPA potentiation and choline uptake enhancement. This combination seems to help improve mood disorders without affecting serotonin levels.

Serotonin Selective Reuptake Inhibitors (SSRIs) is the current preferred mainstream medical method for dealing with mood disorders and depression. They come with a list of detrimental side effects. And don’t work for every depressed patient.

Researchers reported that Coluracetam was beneficial in treating major clinical depression and anxiety disorder.[v] Without affecting serotonin levels in the brain. And without the side effects that go with disrupting serotonin.

How things go bad:

As we get older, our brain chemistry and energy metabolism changes.

↓ Brain cell membranes degenerate

↓ Recall, reaction time and mood diminish

↓ Conversion of choline to acetylcholine breaks down

↓ Acetylcholine levels decline

All of these changes can happen at any age. And are a product of the food we eat, what we drink, lifestyle habits, the air we breathe and more.

So Coluracetam can help mood disorders and age-related cognitive decline. But it works as well for the student looking to do better in school. By boosting acetylcholine and controlling glutamate in the brain.

Coluracetam benefits

Research from a very limited number of studies have shown that Coluracetam will:

• Restore the synthesis of acetylcholine
• Restore long-term memory
• Improve working memory
• Relieve symptoms of severe depression
• Treat symptoms of generalized anxiety disorder
• Increase choline uptake even in damaged neurons
• Repair retinal and optic nerve damage

The benefits from supplementing with Coluracetam seem to be long-lasting. Even after supplementation has stopped.

How does Coluracetam feel?

Even with very small doses of Coluracetam you should experience a decrease in anxiety and improved mood. Overall energy levels should go up.

Unlike the effect commonly produced by stimulants, Coluracetam offers a more relaxed, calm and free-minded kind of thought-processing.

Coluracetam acts quickly to boost long-term and working memory and word-recall. And many nootropic-users report that colors are crisper, or enhanced. Sound and audio seems to wash through you.

Some even report that Coluracetam enhances meditation. There is an extremely pleasant sense of being at peace with the world.

Coluracetam Clinical Research

Coluracetam was first discovered the late 1990’s. And because it’s so new, very few clinical trials have been done with humans. Most of the clinical research available to us has been done on animals.

BrainCells, Inc., who acquired the patent from the company that first developed Coluracetam, have begun human trials. Here we have two examples of the clinical research done in the last 15 years on animals.

Coluracetam Provides Long-lasting Cognitive Improvement

Researchers in Japan worked with rats whose memory was chemically impaired. In this study, rats were dosed with Coluracetam (MKC-231) for 8 days.

The team studied the effects on the high affinity choline uptake (HACU) system of the rats after 8-days of repeated administration of Coluracetam treatment.

They reported an increase of HACU activity along with a boost in cognition. And concluded that Coluracetam “could induce long-lasting pro-cognitive effects by changing the choline transporter regulation system”.[vi]

Coluracetam Improves Working Memory

A study at Iwate Medical University in Japan was done on mice with working memory deficits.  In this study, scientists found that Coluracetam improved working memory at all doses tested.

They found it significantly reversed an acetylcholine deficit. And concluded that Coluracetam improved memory deficits by boosting high affinity choline uptake (HACU), and the release of acetylcholine.[vii]

Coluracetam Dosage

Recommended Coluracetam dosage is 20 – 80 mg per day. So 20 mg would be taken in two 10 mg doses. One Coluracetam dose in the morning, and one in the early afternoon.

Higher doses of Coluracetam are based on clinical trials mostly done on animals. When first adding Coluracetam to your stack, most neurohackers start out with a much smaller dose. And see how you react to it.

Coluracetam is typically sold in powder form. Smaller doses are often taken sublingually for faster and better absorption.

Since Coluracetam is a fat-soluble nootropic, you should take it with a meal containing healthy fats. Or with a tablespoon of unrefined coconut oil.

My preferred healthy fat is a tablespoon of the new organic, non-GMO Performance Lab^® MCT Oil.

Coluracetam Side Effects

Coluracetam is non-toxic. So is considered well-tolerated and safe.

Many first-time users of Coluracetam report fatigue which is often the result of starting with too high a dose.

Remember, Coluracetam works by enhancing choline uptake in your brain. Choline is a precursor to the production of acetylcholine. If not enough choline is available in your system, you’ll feel the side effects.

Side effects are rare but can include anxiety, fatigue, headaches, nervousness and nausea. Again, side effects are often a result of unusually high doses of the nootropic.

Headaches from using Coluracetam typically happen when you forget to combine it with a good choline supplement. Headaches are often a symptom of a choline deficit in your brain.

Where to buy Coluracetam

Coluracetam is usually sold in powder form. A couple of companies offer it in a liquid base making it easier to dose and take sublingually.

The best place to buy Coluracetam is: Science.bio – Coluracetam who sell Coluracetam as a “research” compound. It is sold to be used in an academic laboratory research setting. They go on to state “nothing we sell is intended for nor is it manufactured for diagnostic or therapeutic purposes in humans.”