Role of Cannabinoid Receptors in the Endocannabinoid System

The word cannabinoid has its roots in cannabis, and the end is short for endogenous. This means that the endocannabinoid system which comprises cannabinoid receptors is a line of cannabinoids produced naturally in the human body. Since its discovery in the early 1990s, the system has been the center of rigorous scientific debate. In modern times, it has garnered even more attention largely because of the loosening of legal restrictions surrounding several cannabis compounds, such as CBD and THC. 

In this article, we’ll review how the endocannabinoid system regulates various critical functions, from inflammation and mood to appetite and sleep with a vast network of receptors that stretch throughout the human body. 

The Endocannabinoid System: The Parts

The ECS has three parts. These include two very influential cannabinoid receptors. Here’s the breakdown:

• Endocannabinoids: natural chemicals produced by the ECS
• Enzymes: Involved in processing cannabinoids and endocannabinoids
• CB1 and CB2 receptors: CNS receptors that endocannabinoids and phytocannabinoids bind with.

Cannabinoid Receptors: Crucial for Homeostasis

To understand why CB1 and CB2 receptors are so crucial to the human body, you have to first understand the importance of homeostasis. 

Put simply, homeostasis is the internal environment of your body. Unless this environment is stable, meaning doesn’t have a high temperature, PH, or other abnormalities, your whole physiology is in disarray. It won’t matter if the world around you is sunshine and rainbows if your endocannabinoid receptors aren’t doing a good job at maintaining homeostasis. 

When something inside your body is out of place, the ECS activates cannabinoid receptors to bring it to equilibrium. The cannabinoid receptors are present in select tissues. CB1 receptors are present in the brain and spinal cord. On the other hand, CB2 receptors are present in the immune system, digestive system, and peripheral nervous system. 

Some researchers believe there are another set of receptors, but they are yet to pull the cover on their physiological role. With the help of these receptors, the ECS performs a whole host of functions, including but not limited to:

• Appetite
• Digestion
• Immune function
• Inflammation, including neuroinflammation
• Mood
• Sleep
• Reproduction/fertility
• Motor control
• Temperature regulation
• Memory
• Pain
• Pleasure/reward

Once endocannabinoids perform their jobs via cannabinoid receptors, certain enzymes pitch in and break down and slow things down to prevent progression into overdrive. This ensures that everything stays in balance, and the response is always precise. 

However, things are starkly different when someone consumes marijuana. Marijuana floods the system and widely impacts physiology. Some of the effects induced by marijuana may be beneficial, but some are extremely detrimental to human health. Especially, THC-rich marijuana can cause a serious threat to mental health. Some studies have shown that the compound can cause hallucinations and delirium and exacerbate underlying mental conditions. 

Because cannabis products can tap into the cannabinoid receptors of the ECC, they are touted as a purported remedy for various conditions, such as arthritis, insomnia, and cancer. We also have drugs based on cannabinoids, such as nabilone. 

The Role of Cannabinoid Receptors and Enzymes

When you take marijuana, cannabinoids from the plant enter your system and attach to the CB1 receptors in your brain and induce a high. This compound in question is THC, which mimics the activity of a natural human endocannabinoid called anandamide. 

While THC and anandamide share similarities, anandamide doesn’t alter consciousness. That said, anandamide does calm your brain.

The reason THC causes a high and anandamide doesn’t is because of the FAAH enzyme. FAAH metabolizes anandamide and other endocannabinoids. However, when it comes to THC, its response is relatively slow. In some cases, it doesn’t act on THC, to begin with. This allows THC to build in the system and pose a much greater effect. 

Neurotransmitters in the brain transmit messages from one cell to another. In human brains, phytocannabinoids and endocannabinoids play the same function as neurotransmitters. Like neurotransmitters, they interact with a lot of receptors and therefore have a hand in various functions. 

One cannabinoid, in particular, that has garnered a lot of scientific attention is cannabidiol or CBD. Unlike THC, CBD isn’t intoxicating and doesn’t cause any negative psychological symptoms. One surprising function of CBD is to inhibit FAAH activity so that more anandamide is available to the system. This is why CBD is often thought to have anxiety-relieving properties. 

Endocannabinoid Deficiency

As more and more research on the ECS has amassed, researchers are starting to believe that a lot of human disorders are because of the dysregulation of the endocannabinoid system. Endocannabinoid Clinical Deficiency is the term that has emerged from this debate and is referred to a host of conditions with roots in endocannabinoid deficiency. 

Conditions for which science suggests cannabinoid receptors can help with include:

• Fibromyalgia
• Migraine
• Irritable bowel syndrome
• Treatment Potential
• Cannabinoid receptors are being researched for their potential to treat neurodegenerative and many other conditions. These include:
• Alzheimer’s disease
• Parkinson’s
• Cardiovascular disease
• Neurological, neurodegenerative, neurodevelopmental, and psychiatric illnesses
• Acute and chronic kidney disease
• Autoimmune diseases
• Chronic inflammatory diseases
• Chronic pain conditions

Cannabidiol, a major external influencer Of CB1 and CB2 receptors, has already been given the greenlight to treat epilepsy. In 2018, the Food and Drug Administration approved the first CBD-based oral solution to treat pediatric epilepsy. More CBD-based drugs for the treatment of acne, asthma, pain, and chronic inflammation are undergoing trials.

Final Thoughts

Cannabinoid receptors open a new wave of possibilities for medicine. However, most of the compounds with the capacity to tap into these receptors are in no way close to ascertaining their therapeutic properties. Most of the studies we have on THC and CBD are based on animal-models, and shouldn’t be taken as a gold standard to gauge cannabis’s condition-treating qualities. 

One thing more you should keep in mind is that every treatment has side effects, even if it is derived from natural sources. Self-medication can put you at serious risk of side effects. 

Though CBD has an excellent safety profile and doesn’t have any reported side effects, it’s always best to practice caution and consult a holistic doctor before consuming the compound in any form. There are also legal implications you should be aware of. While CBD is legal in most states, laws vary from one state to another.