Acetylcholinesterase Inhibitors and their Effects on Memory, Cognition & Alzheimer’s Disease

Acetylcholinesterase Inhibitors are a class of compounds that prevent the breakdown of the neurotransmitter Acetylcholine and influence brain function.

They work by inhibiting the enzyme Acetylcholinesterase which is present in regions around your neurons to control levels of Acetylcholine in your brain.

Research into these compounds is being pursued vigorously in the hopes that they may be able to alleviate neurodegenerative disorders such as Alzheimer’s, dementia, and other forms of cognitive impairment.

Acetylcholinesterase inhibitors are also being looked at as potential nootropic supplements or smart drugs for use by healthy individuals who want to augment their intelligence and brain power.

Acetylcholinesterase Inhibitors

Cholinergic Supplement

Memory

Brain Health

Cognition

How It Works:

• Supports memory and synaptic plasticity
• Raises acetylcholine activity
• Promotes brain health and focus

Dosage:

Varies Depending on Supplement

Safety:

Varies Depending on Supplement

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Introduction to Acetylcholinesterase Inhibitors

There are many different types of Acetylcholinesterase inhibitors (also known as Cholinesterase inhibitors or AChEIs) described as either reversible, irreversible, or somewhere in between.

At one end of the spectrum, these compounds can act as memory enhancers, treatments for Alzheimer’s, and lucid dreaming supplements.

On the other hand, Acetylcholinesterase inhibitors are also used as insecticides, damaging nerve agents, and are components of some lethal venoms or poisons.

This disparity might surprise you, but it is another sign of just how complex the human brain is: too much inhibition of Acetylcholinesterase can produce damaging side effects, but at much smaller doses it may actually help you develop better memory capacity, improve the plasticity of your brain and enhance your intellect.

Acetylcholine and the Role of Acetylcholinesterase

Acetylcholine is one of the neurotransmitters most intricately involved in functions of memory storage, consolidation, and recall. It is a key chemical messenger used by your neurons to transmit signals to each other that underwrite our cognitive processing as well as our basic thoughts.

Optimal levels of Acetylcholine can contribute to better working or short-term memory capacity, greater fluid intelligence, reasoning, logical thinking skills, creative thought, executive function, attention control, as well as more vivid dreams at night.

Low levels of Acetylcholine are associated with memory disorders like Alzheimer’s as well as other forms of mental impairments.

We can think of the brain as a network of approximately 100 billion neurons that connect to each other via an interweaving map of synapses.

Neurons communicate to each other by way of these synapses which are essentially interfaces for exchanging neurotransmitters. A single neuron may be connected to thousands of other neurons which it then either sends signals to or receives signals from.

When one neuron “fires” and releases a neurotransmitter like Acetylcholine, it excites the neurons around it and may lead to them firing as well.

Too little excitement and you may suffer from low brain activity. But too much excitement is equally bad, potentially leading to over-stimulation and something called excitotoxicity.

The job of Acetylcholinesterase is to control how much Cholinergic excitement occurs in the brain by breaking down excess Acetylcholine in the area between neural synapses known as the synaptic cleft. Once Acetylcholine has been released by one of your neurons, it can bind to receptors on another neuron to create what is known as an action potential.

But after this action potential has been generated, the Acetylcholine needs to be removed from the synaptic cleft. It can either be taken up again by the neuron that fired it or it can be broken down by an enzyme such as Acetylcholinesterase. This prevents your neural receptors from becoming over-excited and ensures they remain sensitive to the presence of Acetylcholine in the future.

How Do Acetylcholinesterase Inhibitors Work?

If Acetylcholinesterase has an important role to play in regulation nervous system communication, why would you want to inhibit its activity? In some cases, a small amount of alteration of the activity of Acetylcholinesterase can have a positive effect on mental performance and specifically memory.

Acetylcholinesterase Inhibitors can both increase levels of the Acetylcholine neurotransmitter in your brain as well as increase the duration of its stimulatory effects. This means that when one neuron fires, it creates a greater action potential in the receptive neuron (known as the post-synaptic neuron).

You can kind of think of it like its turning up the volume on some of your brain signals. In healthy adults who exhibit normal cognitive function, this may lead to even better memory retention, improved reasoning, and what may seem like a higher rate of cognitive activity.

In patients with Alzheimer’s or elderly individuals, the benefits of Acetylcholinesterase Inhibitors are even more profound. As we age, levels of Acetylcholine start to naturally decline leading to a loss of brain plasticity and difficulty learning. Acetylcholine neurons are known to die off at accelerated rates among patients with Alzheimer’s which is now estimated to affect over 50% of individuals who live to the age of 85.

Using Acetylcholinesterase Inhibitors is shown to boost memory capacity in these individuals by compensating for the naturally lower Cholinergic activity. While they may not be a cure for memory loss and dementia, they are a viable treatment option with a solid history of positive research findings.

The Best Supplements to Use

Two of the most popular natural Acetylcholinesterase inhibitors that you can purchase as nutritional supplements are Huperzine A and Galantamine. Of the two, Huperzine A is more popular in the supplement world and may be safer.

Galantamine is considered to be stronger, but it is typically reserved for more intensive treatment of individuals who have already been diagnosed with Alzheimer’s.

Huperzine A is a natural extract from the Chinese Huperzia Serrata tree. You need an incredibly small amount of Huperzine A to experience the benefits of Acetylcholinesterase inhibition. Studies have found that it has powerful brain boosting effects even at a dosage of 200 micrograms per day. A microgram is one thousand times smaller than a milligram which should give you some appreciation of scale.

Huperzine A is sold as an independent memory supplement, but it is best to combine it with other supplements in a cognitive enhancement stack. A good example would be the Alpha Brain supplement by Onnit Labs which contains a high quality source of Huperzine A.

Neither Huperzine A or Galantamine have been approved by the FDA as drugs to prevent or treat any conditions, including Alzheimer’s disease.

Other Acetylcholine Supplements

There are few other ways that you can increase Acetylcholine activity in your brain. One strategy to use alongside with Huperzine A is to take a source of Choline which the body needs in order to make Acetylcholine.

Some good examples of choline supplements include Citicoline, Centrophenoxine and Alpha GPC which is also found in Alpha Brain. Many will also take ALCAR or Acetyl L-Carnitine with Huperzine since this also increases the rate of Acetylcholine synthesis.

A final option is to look into a class of Cholinergic supplements known as Racetams. These nootropics work by modulating your Acetylcholine brain receptors so they exhibit greater sensitivity. Piracetam, Aniracetam and Noopept fall into this category and are viewed as highly safe while offering incredible benefits for memory capacity.

Using a stack of several different Acetylcholine supplements alongside Acetylcholinesterase inhibitors may significantly improve your cognitive function and help you to retain a sharp memory even as you age.

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