How Cannabinoid Receptors Unlock Pain Relief & More

Cannabinoid Receptors

You’ve heard the well-worn narrative, “Cannabis and cannabinoids are bad for you, and stimulating your cannabinoid receptors will buy you a one-way ticket to Addiction Land.” That’s not exactly accurate. In this article, you’ll learn exactly how cannabinoid receptors work and how stimulating these receptors can be a safe way to help you alleviate pain.

What are cannabinoids?

Before you learn what cannabinoid receptors are (and how they work), it’s important to understand what cannabinoids are. In a nutshell, these are chemicals found in the cannabis plant; they interact with the receptors in your body to produce different effects. Over 113 different cannabinoids have been isolated from cannabis, with three of the most prolific being tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN).

Let’s delve into CBD first. CBD is generally acknowledged as the second most popular cannabinoid (coming in behind THC). This cannabinoid has numerous benefits and is often used for pain or stress relief. Consuming CBD is both legal and safe; CBD is not psychoactive, so it’s impossible to get “high” from ingesting CBD products.

Compared to CBD, CBN is definitely less well-known, but researchers have been paying this cannabinoid more attention as of late. Among other benefits, studies have shown that CBN helps with pain relief. (1) CBN has also been shown to be antibacterial and particularly useful for those with sleep disturbances. (2) (3)

Last but not least, THC is what you need to be wary of if you want to avoid a “high.” This particular cannabinoid has an intoxicating effect when consumed indiscriminately, and it has the potential to cause paranoia and lethargy. However, THC does bring with it plenty of benefits, including pain relief, heightened senses, and relaxation.

What are cannabinoid receptors?

As for cannabinoid receptors, think of these as “landing locations” on our cells with which cannabinoids can engage. These receptors make up our endocannabinoid system, which in turn keeps our bodily mechanisms in check.

Cannabinoid receptors are involved in a wide range of processes and functions, including cognition, memory, glucose metabolism, and insulin resistance. They also control our vomiting reflex, nausea and appetite control, as well as the “high” that we get from exercising. (Contrary to popular belief, the latter is not caused by endorphins!) (4)

How scientists discovered cannabinoid receptors

After learning about THC, CBD, and the other cannabinoids, scientists started searching for compounds that produced the same effects, but were naturally occuring in our bodies. They found and isolated the neurotransmitter called anandamide, a pain reliever which is often hailed as a “bliss molecule.” (5)

This got scientists thinking: there must be a corresponding receptor which responds to anandamide. Before long, they discovered cannabinoid receptors.  

CB1 vs. CB2 cannabinoid receptors

Your CB receptors can be categorized into two classes: CB1 and CB2. First and foremost, your CB1 receptors are predominantly found on nerve cells in the brain and spinal cord. The CB1 receptors in your hypothalamus affect your appetite, and the CB1 receptors in the hippocampus influence memory processing.

While the vast majority of CB1 receptors are located within the brain and spinal cord, you’ll still find a smattering of these receptors in other organs and tissues, including the spleen and endocrine glands.

CB2 receptors are mostly found in your peripheral nervous system, including white blood cells. Your CB2 receptors’ main role is keeping your immune system healthy. They achieve this by regulating the release of cell-signaling molecules (cytokines); these promote cell-to-cell communication and expedite the movement of cells towards areas of inflammation.

The function of your endocannabinoid system

Together with other endocannabinoids, anandamide taps into the endocannabinoid system (ECS) to maintain optimal balance in your body.

Your ECS coordinates messages between your brain and body; it also helps both the brain and body respond appropriately to stimuli. Essentially, the ECS is crucial to functions such as sleep, pain, pleasure, cognition, memory, appetite, and more. When you get sleepy around midnight, that’s the ECS at work. When you get hungry during mealtimes, that’s also the ECS doing its job.

Why are cannabinoid receptors so important?

Simply put, if our receptors don’t function properly, it messes with the processes and functions of the endocannabinoid system. If your CB1 receptors are suppressed, for example, this might bring about heightened sensitivity to pain and discomfort. (6)

Pain tolerance aside, your cannabinoid receptors also impact your appetite and food consumption. In 2006, pharmaceutical companies created a “smart diet pill” which blocked cannabinoid receptors. The hope was that by consuming these pills, you’d no longer have to deal with an excessive appetite (which correlated with the stimulation of these receptors).

Unfortunately, things went south with this drug (called Rimonabant, or Acomplia in some circles). Those who consumed it reported plenty of side effects, including depression, anxiety, insomnia, and even seizures and suicide. (7) The drug was off the market before long.

The benefits of cannabinoids

While dozens of active cannabinoids have been identified in cannabis, only a handful have been studied so far. Research has indicated that, by stimulating cannabinoid receptors, many cannabinoids are capable of reducing pain and inflammation, stimulating appetite, and promoting rest and relaxation, among many other potential benefits.

THC has been shown to inhibit the buildup of amyloid plaque, which is the primary pathological marker for Alzheimer’s disease. (8)

CBD has been shown to be beneficial where your cardiovascular system is concerned—it may protect against the vascular damage caused by various factors, including high-glucose environments. (9)

CBN is particularly helpful for assisting in better sleep. According to cannabis science and technology company Steep Hill Labs, CBN is as effective as pharmaceutical sedatives, without the potentially negative side effects. (10) Say goodbye to all those sleepless nights!

A final word on cannabinoid receptors

Researchers estimate that cannabis is one of the world’s oldest domestic plants and that it’s been used by humans for at least 10,000 years. (11) Taking into account the fact that our bodies contain cannabinoid receptors, cannabis advocates are now saying that consuming cannabis is a natural way of life.

We won’t jump to the conclusion that humans are “designed” to consume cannabis, but it’s clear that cannabis is an important and irreplaceable plant in the health and wellness space. There’s no cause to shy away from stimulating those receptors!

Frequently Asked Questions


How do cannabinoid receptors work?

Think of cannabinoid receptors as a lock, and cannabinoids as a key. When someone inhales or ingests cannabinoids, these cannabinoids “flood” the receptors and activate them. The receptors then perform their various functions, such as assisting with stress relief and pain.


How many cannabinoid receptors are in the human body?

As of now, it’s unclear how many receptors we have in our bodies. What we do know is that they’re distributed all over!


What is the endocannabinoid system?

The ECS consists of receptors (CB1 and CB2) that respond to certain chemical molecules (cannabinoids). When a cannabinoid binds to a receptor, it “instructs” the receptor to carry out certain functions (e.g., indicating to your body that it’s time to eat or sleep).


Where are cannabinoids found?

Cannabinoids are found in both plants and our bodies, and they can also be synthesized in the lab. Those produced by plants are termed phytocannabinoids, while those produced by our own bodies are called endocannabinoids. Lab-synthesized cannabinoids are referred to as synthetic cannabinoids.


What other plants have cannabinoids?

Radula marginata (also known as New Zealand Liverwort) produces perrottetinenic acid. This is a form of cannabinoid that appears to be extremely similar to THC. (12) Other plants that produce cannabinoid-like compounds include flax fiber and rhododendron. (13) (14)


What foods contain cannabinoids?

Good news for the chocolate lovers out there: as it turns out, dark chocolate contains anandamide and other cannabinoids. Feeling stressed and need to relax, pronto? Simply pop a few squares of dark chocolate in your mouth!

Don’t write black truffles off as just another trendy food, either—they actually produce anandamide and help with stress and pain relief. Researchers believe that the anandamide in these truffles act as “bait” to lure animals into consuming them; this allows them to spread their spores widely, providing a better chance at reproduction. (15)

Last but not least: black pepper. Unlike dark chocolate and black truffles, black pepper doesn’t contain anandamide. Instead, it produces an organic compound, beta-caryophyllene, which functions as a cannabinoid. This binds to CB2 receptors and is said to help with reducing inflammation.