Introduction to the Cholinergics

June 16, 2015

Introduction to the Cholinergics

Introduction to the cholinergic class of nootropics
  • Classes of cholinergics
  • Acetylcholine sources and production
  • Acetylcholinesterase and the Acetylcholinesterase inhibitors

For those interested in supplementing with nootropics, a basic understanding of how the compounds work in conjunction with your natural brain chemistry is necessary to get the most out of them. One of the most basic and widespread classes of nootropics available are the cholinergics, which can be subdivided into three sub-sets: choline precursors and intermediates, choline agonists and acetylcholinesterase inhibitors.

Our brain is the control center of our body and as a result uses an enormous amount of energy. If you’re going to be attempting to use cholinergics, its important to make sure you’re eating a choline rich diet. Choline is found naturally in dairy, fish, meat and soy but cheap choline sources are available in the form of choline citrate and bitartate or the more bio-available forms citicoline and Alpha GPC .

Choline is a necessary component during the brain’s synthesis of acetylcholine, a neurotransmitter involved in learning, memory and movement. The choline agonists, like members of the racetam family such as the classic nootropic Piracetam, work by up-modulating production of acetylcholine, however without a good base of choline to synthesize from some people experience headaches or brain fog.

 

Members of the racetam family are the most typical cholinergics and work by upmodulating acetylcholine production via an enzyme called acetyltranserase. Related to but performing a diametrically opposed job to acetyltransferase is acetylcholinesterase, an enzyme that degrades Acetylcholine into choline and acetic acid. This is a necessary reaction which allows the cholinergic neuron to rebound to it’s original resting state. Acetylcholinesterase, in addition to terminating acetylcholine transmissions allows muscles to relax as well, as a result powerful irreversible acetylcholinesterase inhibitors exist as naturally occurring poisons and some were used as early nerve agents due to their ability to induce paralysis or convulsions. Reversible acetylcholinesterase inhibitors have been used as treatment for Alzheimer's owing to their ability to block the breakdown of ACh in the synaptic gap. As we age, our ACh levels degrade. ACh is vital in learning and memory formation and recall in the brain so a correlated degradation in movement and memory accompanies the depletion of our cholinergic system.

 

As a result, there are a class of drugs that have been used to treat Alzheimer’s and other forms of age related cognitive decline known as acetylcholinesterase inhibitors. Drugs in this class include the naturally occuring alkaloid galantamine, in the Indian plant Celastrus Paniculatus (known as the “Intellect Tree” in Ayurvedic medicine), Huperzine-A, the extract of the Chinese fir moss Boswellia Serratta and the drug Cymserine.

Another popular Nootropic is Centrophenoxine.

Galanthus Caucasicus, Snowdrop flower

It’s not generally recommended to take ACh agonists at the same time as potent Acetylcholinesterase inhibitors due to their conflicting mechanism of action. Using both will result in the brain receiving signals to upmodulate acetylcholine production and acetylcholinesterase which can lead to dangerous excitotoxicity.

Always remember that despite the safety profile of these compounds, minimum effective dosing and understanding the mechanism of action of the chemicals and how they work with your neurochemistry are vital to getting the most out of the substances with the minimal amount of negative peripheral effects. Always consult with your physician before beginning any supplementation regimen, especially if you’re already taking prescriptions for any preexisting health conditions.




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