There are many types of nootropics each with their own set of attributes… Some nootropics relax the mind and help us sleep, others are more stimulating to give us a boost in energy levels throughout the day. What are nootropic stimulants? What is it that they do inside our bodies to give us these stimulating effects? In order to answer this question we need to first have a quick look at how our minds regulate our energy levels to begin with.

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How Nootropics Act As Stimulants

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The brain is a careful orchestra of neurotransmitters, each working with each other to regulate the movement of signals throughout the brain. Neurotransmitters like glutamate cause the nerve cells to fire more often, making us feel alert and sharp. On the opposite spectrum we have compounds like GABA that make it harder for the nerve cells to fire electrical impulses, making us feel slower and sleepy.

The targets of the stimulating nootropics tends to be on neurotransmitters that promote nerve transmission rather than inhibit it.

The Stimulating Neurotransmitters

The main stimulating neurotransmitters in the brain are acetylcholine, glutamate, norepinephrine, and dopamine. These neurotransmitters work in unique ways to stimulate the firing of the nerves to transmit messages from one part of the brain to the other. Depending on the nootropic being used, it will have different effects on these neurotransmitters and the receptors associated with them.

For example, noopept and the racetam family of nootropics have an affinity for the glutamate receptors. When these receptors are activated it causes positively charged ions to enter the nerve cell and lowers the action potential. With a lower action potential in a nerve cell, it takes less effort for one region of the brain to send a signal to the other.

When nerve cells fire more easily we end up with a greater movement of information in the brain. This gives us the feeling of being alert and sharp. Memory, reaction times, and energy levels are all improved when the brain is able to activate neurons with greater ease.

This is just one example of ways nootropics can create stimulating effects. Others increase the release of acetylcholine, dopamine, or norepinephrine. Some will work instead by inhibiting the neurotransmitters and chemicals that cause us to feel relaxed such as adenosine, GABA, or serotonin.

There are literally hundreds of different ways a nootropic can interact with the brain to cause neurostimulation.

A List Of Stimulating Nootropics

  1. Piracetam

  • Piracetam was the first substance ever classified as a nootropic, and remains one of the most popular to this day. It serves as the most simple member of the racetam family of chemicals, which includes other such members as aniracetam, oxiracetam, phenylpiracetam, and pramiracetam.
  • Piracetam is considered a stimulating nootropic because it both binds to and increases the number of AMPA-glutamate receptors on the neurons. This allows for faster reaction times, better learning and cognition, and gives a feeling of being alert and awake. [1].
  • Additionally, piracetam promotes glucose metabolism and mitochondrial function which benefits energy levels throughout the day [2]. Although this mechanism isn’t directly stimulating, it optimises energy levels and allows for our neurons to fire at a higher rate for a longer period of time.
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  1. Noopept

  • Noopept is structurally similar to the racetam family of nootropics. It works through the glutamate receptors within the brain in a similar respect to piracetam [3].
  • Noopept is considered to be nearly 100 times stronger than piracetam, and has an effect on both the AMPA-glutamate receptors as well as the NMDA-glutamate receptors. This allows noopept to offer a more well-rounded neurostimulatory effect, making us feel more awake and alert.
  1. Adrafinil

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  • Adrafinil is similar in structure to the prescription nootropic modafinil. It’s used to promote a feeling of wakefulness and sharpens the mind. It works through the adrenergic receptors which regulate the sympathetic nervous system (fight or flight) [4].
  • The adrenergic receptors are regulated by norepinephrine and epinephrine within the body. These catecholamine neurotransmitters cause stimulation to various organs throughout the body, giving us a surge of energy, more mental focus and clarity, and speeds up our heart rate to provide more oxygen to our cells.
  • Adrafinil is considered a prodrug for modafinil. This means that once inside the body adrafinil is converted to modafinil which then activates the adrenergic receptors. The results of Adrafinil are very similar to Modafinil, but can be achieved without a prescription in most countries.
  1. Caffeine

  • Caffeine is by far the most well-known and popular stimulating nootropics available. Found mainly in coffee and tea, this substance has a unique ability to stimulate the mind and inhibit the feeling of sleepiness. People have been using caffeine for years as a preworkout before exercise, in the morning to give us a mental boost, and late at night during long and challenging projects at work or school.
  • Caffeine works by inhibiting a molecule known as adenosine. This compound builds up in the brain throughout the day as a byproduct of nerve function. As is builds in concentration it begins to bind to receptors located on the nerve cells causing a delay in the transmission of electrical impulses throughout the nerve. As more and more adenosine builds up, this delay becomes longer and more widespread. We begin to feel dull and slow, eventually leading us to feel tired. It works as a way for the body to remind us to go to sleep.
  • Caffeine works by inhibiting adenosine, helping us feel more alert and awake for longer. Additionally, caffeine has the ability to remove previously bound adenosine molecules, which can eliminate sleepiness and make us feel stimulated and awake. Our nerve cells begin firing faster, and information can travel throughout the brain more easily.

How To Use Stimulating Nootropics

Stimulating nootropics should not be used too much. It’s important to follow the directions on the box, and avoid taking stimulants multiple times throughout the day. Our bodies need sleep and although its useful to inhibit sleepiness while trying to finish a project or get through a shift at work, eventually the mind needs to shut down for the night to rest.

Stimulating nootropics can be used directly in the morning or before lunch. Some individuals are more sensitive to this class of nootropics so careful titration is recommended. If trying a new nootropic supplement for the first time start with a smaller dose one day, and slowly build up to the recommended dose over the course of a week or two. If you notice difficulty sleeping, simply take the nootropic earlier in the day, or reduce the dose.

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References:

  1. Copani, A., Genazzani, A. A., Aleppo, G., Casabona, G., Canonico, P. L., Scapagnini, U., & Nicoletti, F. (1992). Nootropic Drugs Positively Modulate α‐Amino‐3‐Hydroxy‐5‐Methyl‐4‐Isoxazolepropionic Acid‐Sensitive Glutamate Receptors in Neuronal Cultures. Journal of neurochemistry, 58(4), 1199-1204.
  2. Heiss, W. D., Hebold, I., Klinkhammer, P., Ziffling, P., Szelies, B., Pawlik, G., & Herholz, K. (1988). Effect of piracetam on cerebral glucose metabolism in Alzheimer’s disease as measured by positron emission tomography. Journal of Cerebral Blood Flow & Metabolism, 8(4), 613-617. Chicago.
  3. Vorobyov, V., Kaptsov, V., Kovalev, G., & Sengpiel, F. (2011). Effects of nootropics on the EEG in conscious rats and their modification by glutamatergic inhibitors. Brain research bulletin, 85(3-4), 123-132.
  4. Duteil, J., Rambert, F. A., Pessonnier, J., Gombert, R., & Assous, E. (1979). A possible α-adrenergic mechanism for drug (CRL 40028)-induced hyperactivity. European journal of pharmacology, 59(1-2), 121-123.