Neuroreceptor Resensitization

What causes neuroreceptor desensitization and why is it important?


Neuroreceptor desensitization occurs when usually a chemical that has a higher than normal affinity for the receptor is introduced in too high of quantities for the body to maintain physiological equilibrium. Because of the imbalance, the body will adapt by either reducing the number of receptors or by downregulating their effect. For the purpose that the receptor was serving, its functionality will be diminished through this process.

An Example

Let’s take an easy example; caffeine. Caffeine is an adenosine receptor A1/A2A antagonist. Adenosine receptors are like switches that help various areas of the body know when to conserve energy, or in other words slow metabolism. The effect of antagonizing (or blocking) this would be removing the limitations of your cellular metabolism, making it so that your body will consume more energy faster, with more caloric output. This can be great especially for the brain and muscles when in a situation where you need to perform your best such as a sport. 

 However, by consuming caffeine regularly through such things as coffee or energy drinks without allowing the body time to reset, the receptors will become desensitized, making it so that more caffeine is needed for the same effect. Keep in mind that caffeine has a very low rate of causing neuroreceptor desensitization compared to many other drugs and chemicals such as THC, amphetamines, psychedelics, and many pharmaceuticals. It only takes a month or so of abstinence from caffeine to reset the receptors. For this reason, and it having a rather high LD50, it is generally considered as safe by the FDA.

An analogy

This is a brutal analogy, but the brutality is similar to the situation of neuroreceptor desensitization, so let’s go with riding a horse. In the beginning you kick the horse in the side and the horse gallops with great speed and great results. By the end of the day, the horse hasn’t eaten or drinken anything and is rather tired. The rider sees the sun is starting to go down and is looking at the horse trotting along slowly. The rider naturally will want to go faster so they can make it to their destination before dark. So the rider proceeds to kick the horse more. The horse goes a little faster for a bit, but slows down again. Then the horse rider keeps kicking the horse as hard as he can, but with every kick the horse becomes weaker and slower and eventually doesn’t go anywhere. This is kind of what it’s like to constantly use a chemical such as caffeine on our brain. Horrible isn’t it?

The main point is not that we shouldn’t kick the horse, as a bump from the leg under normal circumstances is proper riding edicate. However, not taking care of the horse, not letting the horse take a break, and obsessively beating on the horse will lead to very bad results. This analogy isn’t even as bad as the situation we are describing, because you can always get a new horse, but you cannot get a new brain.

So in this article we are going to talk about neuroreceptors and why it is important to take care of them.

What are neuroreceptors?

Neuroreceptors are proteins on the outside of (mostly nervous system) cells that are meant to receive specific chemicals released by the nervous system for the purpose of signaling specific metabolic actions. They are like the switches on a dashboard of an airplane cockpit. Each switch has a critical function that the pilot needs to safely operate the plane. Our cells use neuroreceptors in the same way.

Every cell can perform many functions, but in having to co-exist with another 10,000,000,000 or so other roommates, it must be in complete coordination with the living organism. The nervous system is the system for coordinating cellular function so that it works with the rest of the body. In a single human being there are about 100,000 miles of nerves innervating the rest of the tissues in the body. That is enough to wrap the entire planet 4 times. So this coordination aspect of the human being is vitally important as it is the main controller of every tissue in the body and a huge determining factor of one’s ability to think clearly and stay healthy.

Why would neuroreceptors become desensitized?

Neurorecptors become desensitized when they are consistently pushed out of their equilibrium. The human body and all biology operates on balance. So when we introduce a new chemical such as a drug into one’s biological system, it will cause the balance to become upset. It sounds bad, but it can be very helpful in specific situations such as using anesthesia to remove consciousness of a person during surgery, or using an antidepressant drug to keep a person from suicidal tendencies. However, it can be a double-edged sword because if the drug is used too much for too long (which is only a matter of weeks before the body adapts), then the body will now have two problems. In the case of using antidepressants for depression, after months of use, one would not only have to solve how to get off the dependency of the drug, but will also still be left with what was causing the depression or emotional imbalances to begin with. This is not a good situation.

What side effects come with desensitization?

Again, we are going to stick with the example of depression. When the receptors for something like serotonin (the neurotransmitter associated with happiness) becomes desensitized, it will make it very difficult for the body to produce enough serotonin to maintain a basic level of well-being for that person. Or in other words, feeling happy will become near impossible without the help of a drug. Now at this point, we took a situation, and made it much worse. There are many accounts of people accidentally desensitizing their receptors all across the internet. It can be a very tedious, agonizing, and even traumatic experience. People can begin hallucinating, developing mental disorders such as schizophrenia and paranoia, along with a multitude of other things that will make life very difficult.

How do you fix desensitization currently?

Luckily, the human body is amazingly adaptive, healing, and responsive. So neuroreceptor desensitization can be fixed or prevented in a few ways.

The first way is through cycling usage of any psychoactive substance or drug. The cycling periods for various chemicals can range widely, but for most things that people consume regularly such as caffeine, cannabis, nootropics, or the Nootripure products, the cycle rate is about a week. For something like birth control or a tricyclic antidepressant it could be 6 months. But if you regularly allow a period for your body to reestablish equilibrium it will help prevent neuroreceptor desensitization.

The second way is just to abstain from using the drug for a long period of time. This is often very harsh and is the method that is most frequently used in drug rehabilitation clinics. The process can cause the person to develop severe mental illnesses such as uncontrollable shaking, seizures, hallucinations, and can cause permanent damage to the mind. It is a rather traditional way of resensitizing, but comes with a cost.

The third way which is most commonly practiced in the medical system is to slowly reduce the dosage of the drug, or to replace the drug with something similar that is safer and has a different mechanism of action. This will keep the body from having an adverse reaction while giving time to the desensitized neuroreceptors to rebuild.

How do the nootripure products solve the issue?

Here at Nootripure, we get a lot of inquiries from people about why they feel a certain way, or if they really need a certain medication, or how to stop abusing a particular drug. At a certain point, people will realize they have neuroreceptor desensitization, but just don’t know the words to use or how the physiology behind it works. But they know they don’t feel well and they know it has something to do with the chemical balance in their brain. So we like to offer solutions to help people move through this situation with ease and fulfillment.

One way we help people is by creating more holistic solutions to their needs. Most often we see neuroreceptor desensitization from over using antidepressants, opioids, and amphetamines. These work mostly on the serotonin and dopamine receptors. These two receptor groups are the main two that allow us to feel joyful and positive. So when people stop feeling joyful naturally, they often will seek chemicals that will help them get their positivity back. Unfortunately, these are the most dangerous to change because 90% or more of the time people will use too much and will make the problem worse. For this reason, the Food and Drug Administration created a list of banned and controlled substances. The controlled substances list is not defined by whether the drug is dangerous or harmful, it is defined by abuse potential. Meaning, that people, left to their own judgement will most likely consume the drug in amounts that will accidently cause more harm than good. For this reason, we strongly support the FDA’s decision to make these substances illegal to distribute and consume. As it takes a lot of refinement to be able to accurately use such powerful tools to heal the body and mind.

The unfortunate side is that the FDA placed research and medical restrictions on these substances too, which has limited progress in the medical and pharmaceutical fields, but organizations such as MAPS and the Nootripure Foundation are doing what we can to reestablish a balance legally that allows for medical progress.

We are currently developing pharmaceutical patents that reduce the likelihood of neuroreceptor desensitization as well as other side effects for various mental illness related drugs. To do this we created a subsidiary company called Nootripure Laboratories that produces a number of products that people can use to ensure that their mind performs well while it feels well and heals well. Already thousands of people have given up their coffee, energy drinks, focus pills, and other harmful substances for something much safer, and even offers more benefits. Our goal was to create something more effective and usable than the alternatives while making it safer and with a multitude of long term mental health benefits. Each of the products comes with a safety instruction booklet that let’s the person know how to leverage the product to maximize their results and their mental health. You can check out the products here.


Constantly consuming any chemical will cause neuroreceptor desensitization which will lead one to feel bad and become mentally unstable. So it is best to avoid with cycling or by using a safe and healthy alternative such as the Nootripure products. Taking a drug over and over hoping that one feels better is like beating a dead horse. Or an alive horse. Either way, one should ask themselves why the heck in the world would they be beating a horse at all? Or even worse, beating on neuroreceptors in their brain. If you wouldn’t beat a horse, then don’t beat on yourself either. Cycle coffee usage. Ask your doctor about cycling usage of your medications. Seek healthier alternatives with low risk of side effects. Take at least a couple days a week to just relax and care for your mind and body. It only takes a little awareness with a few minutes a day dedicated to self care to make a big shift in your well-being. If you want to live a life where mental health is inevitable and mental illness is optional, then welcome to the Nootripure life. Nootripure’s mission is to make mental illness completely optional for anyone. All of our research, educational tools and product development is focused on this one goal. And we are on track to hitting that goal in the next decade with products already on the market.

If this resonates with you we recommend joining our community of people who believe in a mentally healthier world. You can download the ebook and how to become an advocate for mental health here, or you can consider making a donation to support the research and educational efforts of the Nootripure Foundation here.

We will be with you on your journey to superior health and wealth.