Cholinesterase inhibitors are a new class of supplements and drugs that have been found to offer serious benefits for the way your brain works and stores memories.
They are a mainstay of popular brain supplements like the Alpha Brain formula from Onnit Labs. There are several different supplements that fall into the Cholinesterase inhibitors list like Huperzine A and Galantamine. These compound work to increase levels of one of the neurotransmitters that is necessary for memory function.
This class of compounds may be able to slow down the progression of memory loss in elderly individuals, while keeping memory performance sharp in younger people. Cholinesterase inhibitiors work to increase the plasticity of the brain’s synapses and have been shown to boost learning skills while affecting the fluid intelligence of the brain.



- Supports memory and synaptic plasticity
- Raises acetylcholine activity
- Promotes brain health and focus
How do Cholinesterase Inhibitors Work?
Related Topics
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- What is Acetylcholine?
- Cholinergic Receptors
- Choline's Role in the Brain
- Using Choline Supplements
- Cholinesterase Inhibitors
- Effects and Benefits
- Recommended Dosages
- Dietary Sources
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- Possible Side Effects
- Buy Choline
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The brain processes affecting memory are diverse and not understood completely, however we do know some of the chemical systems which have an effect on promoting better memory, and those which inhibit proper memory function.
Acetylcholine (ACh) is an important neurotransmitter involved in some of the most important signaling in the brain related to memory, cognition and attention. Certain supplements work to boost acetylcholine levels in the brain, contributing to better mental performance and cognition.
As we get older, levels of acetylcholine decline. People with Alzheimer’s and other forms of dementia often show particularly low levels of this key neurotransmitter.
Cholinesterase (Also known as Acetylcholinesterase or AChE) is the enzyme by which Acetylcholine is hydrolyzed, or broken down. It essentially works to control levels of Acetylcholine in the brain and make sure there is not too much of this neurotransmitter interacting with receptors. But sometimes by interfering with this enzyme, we can increase Acetylcholine levels to cause improvements in memory formation, retention and recall.
Cholinesterase inhibitors do exactly that; they inhibit the ability of this enzyme to break down this important neurochemical. Inhibition of this enzyme allows for the production of Acetylcholine to increase in the brain. Subsequently, more Acetylcholine is available to the cholinergic receptors.
Increased activity at cholinergic receptors may lead to increased memory function and enhanced learning ability. The end result is heightened memory and learning abilities, along with increased focus for both health young adults and older people experiencing memory deficits.
Cholinesterase’s Effect on Acetylcholine
Acetylcholine is the most common excitatory neurotransmitter and is present in vast amounts throughout the body. It acts on the central nervous system, the peripheral nervous system, and the somatic nervous system.
Depending on the receptors it encounters, Acetylcholine can work in the capacity of an excitatory neurotransmitter (in the brain and neuromuscular junctions) or as an inhibitory one (in cardiac tissue). For nootropic purposes, we are interested primarily in its function in the brain.
Nootropics work to boost memory, learning, and focus. Having an adequate amount of Acetylcholine available in the brain is necessary for normal cognitive function. Enhancing the amount of materials available for conversion into Acetylcholine, while at the same time stimulating the Acetylcholine receptor sites are standard brain supplement target goals.
Because Cholinesterase, or AChE, targets Acetylcholine in order to break it down, it causes less to be available at any given time. This makes the inhibition of Cholinesterase an obvious target for enhancing one’s cognitive abilities. It is thought that using Cholinesterase inhibitors may be a straightforward and simple way to improve short-term mental abilities.
Acetylcholinesterase Inhibitors
Acetylcholine (Ach) is released as a chemical signal (a neurotransmitter). It goes from the nerve into a synaptic cleft and binds itself to the receptors on the post-synaptic membrane in order to deliver the signal sent from the nerve. Once Acetylcholine has been released into the synapse, Cholinesterase is there to break it down.
This is a necessary cycle because if Acetylcholine remains in the synapse for an extended period of time it can impair the brain’s health. Cholinesterase works as a kind of recycling agent. It is present at the receptor site where it terminates the signal transmission by hydrolyzing Acetylcholine. However, high levels of Cholinesterase can cause too much Acetylcholine to be broken down too quickly, which may negatively impact memory and learning.
How to Inhibit AChE
Two of the most commonly used Cholinesterase inhibitors are Galantamine and Huperzine A. Both of these nootropics are derived from plants and are considered herbals.
Galantamine is an alkaloid originally extracted from the flowers of a plant called Galanthus Caucasius. In the late 1950s, it was synthesized and since that time has been used in many European countries to treat certain types of sensory or motor dysfunctions.
Currently, Galantamine is approved by the FDA for the treatment of Alzheimer’s disease and thus, it is available as both a prescription drug and an over-the-counter supplement. There is no known difference between the prescribed drug and the OTC supplement except that the prescribed drug has been altered to provide a time-release option.
Huperzine A comes from the Huperzia Serrata plant. Huperzine A also works in other capacities besides AChE inhibition. Scientists are interested in it because it may counteract one of the primary signs of cognitive decline which occurs in Alzheimer’s patients. It also improves neuroplasticity.
This means it makes it easier for the brain to form new connections between neurons enabling us learn faster and to remember more of what we learn. Long-term use of Huperzine A results in better brain health overall because of this herb’s neuroprotective properties.
Acetylcholine & Enhancing Memory
There are other ways to raise Acetylcholine levels as opposed to simply using Cholinesterase inhibitors. Many users seek to increase Acetylcholine availability in their brain while, at the same time, inhibiting its breakdown. This is accomplished by stacking several nootropic brain supplements together at once.
Increasing Acetylcholine availability can be accomplished by taking a good Choline supplement which has high bioavailability. Alpha GPC or Citicoline are both good options. Then, add a Cholinesterase inhibitor like Huperzine A (such as in the Alpha Brain stack) for a synergistic benefit. This combination improves both memory function and learning ability and may promote better brain health overall.
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Article last updated on: July 6th, 2018 by Nootriment