The Function of Cholinergic Receptors in the Brain

Cholinergic receptors in your brain are being highlighted more and more for their role in memory storage, conscious thought, and neurological disorders like Alzheimer’s disease and dementia.

Cholinergic receptors’ function is intricately involved in many of the most important processes that our brains carry out every second.

The cholinergic system in the brain uses the Acetylcholine neurotransmitter to communicate. Acetylcholine is an important neurotransmitter acting on a wide range of functions and tissues throughout the body.

Cholinergic receptors are a certain type of neuron whose molecular structure responds specifically to Acetylcholine.

In the brain, Acetylcholine is especially important because of the role it plays in memory formation and learning ability.

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Neurotransmitters and Receptors

In the brain, messages are carried between the nerve cells, or neurons, via chemical impulses. These chemical messengers are called neurotransmitters.

Scientists don’t know exactly how many types of neurotransmitters there are, but they have been able to identify over 100 types so far. These chemical messengers can be excitatory or inhibitory meaning they can boost or inhibit the continuation of messages along a neural pathway.

Some neurotransmitters, such as Acetylcholine, are capable of being both excitatory and inhibitory, depending on the type of receptors which are present. Cholinergic receptors respond to the neurotransmitter Acetylcholine specifically.

Although Acetylcholine is found in large quantities throughout the body, in the brain, Acetylcholine is a key neurotransmitter involved in cognitive function, making it one of main focuses of nootropic supplements. It also plays a role in decision-making capacity.

Our body gets Acetylcholine through foods we eat. We ingest foods and supplements which are precursors to Acetylcholine. For example, egg yolks are high in Choline which is a precursor to Acetylcholine.

Our body absorbs the Choline from the egg yolks and it is converted, in the brain, into a usable form of the neurotransmitter Acetylcholine.

Cholinergic Receptors System

There are two main types of cholinergic receptors (Acetylcholine sensitive receptors), prompting scientists to break down the cholinergic receptors even further into two subgroups, namely nicotinic and muscarinic.

Nicotine and muscarine are direct agonists of the cholinergic receptors. However, the muscarinic cholinergic receptors respond specifically to muscarine are not affected by nicotine. Conversely, nicotinic cholinergic receptors that respond to nicotine are unaffected by muscarine.

While the specific roles for both of these types of cholinergic receptors are not fully understood, we do know that greater levels of activity at these receptors leads to improvements in memory, attention, learning, reasoning, and a number of other cognitive functions.

As such, researchers have found that you may improve brain function by supplying the brain with more precursors of the Acetylcholine neurotransmitter or using other methods to increase activity at these receptors.

Supplements that are able to improve mental performance are referred to as nootropics and there are a number of ways that they can be used to positively affect cholinergic receptor sites.

Nootropic users deliberately provide their brains with the precursors to acetylcholine, or with inhibitors for the enzyme which breaks it down (acetylcholinesterase).

Cholinergic agonists, like nicotine, work to stimulate the system and to multiply the available Acetylcholine present in the brain at any given time. Other nootropic supplements like Galantamine and Huperzine A work to inhibit Acetylcholinesterase from breaking down Acetylcholine, thereby increasing the amount present in the brain for use.

What Are the Cholinergic Nootropics?

Cholinergic nootropics include Acetylcholine precursors and cofactors, and Acetylcholinesterase inhibitors.

Precursors to Acetylcholine are (in order of bioavailability):

• Alpha GPC
• Citicoline
• DMAE

Alpha GPC is able to cross the blood-brain barrier most easily and thus, is more bio-available for Acetylcholine production. Citicoline is a good Choline source, though not as bioavailable as Alpha GPC. DMAE is a good source of Choline, but the least bioavailable of the three.

Two necessary cofactors to the production of Acetylcholine are:

• Vitamin B5
• Acetylcarnitine

Vitamin B5 is a needed component in the process of Acetylcholine production, as is Acetyl L-Carnitine which is an amino acid responsible for donating the acetyl portion to the Acetylcholine molecule.

Agonists to Acetylcholinesterase:

• Huperzine A
• Galantamine
• Rosemary
• Cannabis

Huperzine A not only works to inhibit Acetylcholinesterase, but was also seen to increase nerve growth factor in rodent studies. Galantamine, Rosemary and Cannabis all work to inhibit Acetylcholinesterase, with Cannabis also working as a possible neuroprotective agent.

All of the above mentioned Nootropic compounds are available as dietary supplements only, and the FDA has not approved any of them as drugs to prevent or treat any conditions.

Common Stacks Targeting the Cholinergic Receptors

Many nootropic users opt to combine supplements which work together synergistically to boost cognitive function beyond what each component might be able to do on its own. The most common stack targeting the cholinergic system is a combination of racetams stacked with a Choline supplement.

Racetams, like Piracetam, Oxiracetam, Pramiracetam and Aniracetam are Acetylcholine receptor agonists. This means your Acetylcholine precursor, such as Alpha GPC or Citicoline, provides the brain with additional material for conversion to Acetylcholine, while at the same time the racetam works to stimulate the Acetylcholine receptors. When cholinergic receptors are stimulated, there may be a beneficial boost in learning ability, memory, and, usually, focus and concentration.

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