Since its discovery in 1990 the CB1 receptor has continued to amaze researchers in all that it’s responsible for regulating. As studies continue with this receptor, its homeostatic benefits and importance are getting harder for pharmaceuticals and modern medicine to ignore.
CB1 Receptor: The Highlights
- The human body contains an endocannabinoid system that includes cannabinoid receptors, CB1 and CB2, and endocannabinoids.
- The CB1 receptors are expressed primarily in the brain.
- Because the CB1 receptors are located in the brain, they play a role in hormonal regulation impacting mood, sleep, and emotional stability.
- The CB1 receptor readily accepts the ligand anandamide or its agonist THC.
- Other locations of the CB1 receptor, such as the liver and endothelial cells, making it important in regulating appetite as well as pain perception.
What Are Cannabinoid Receptors?
In the late 1980s and into the early 1990s large amounts of research efforts on cannabis and the effects of cannabinoids on the human body were done.
The research soon led to the discovery of a system within the body that reacts to cannabinoids through receptors in the brain and throughout the body. This system is known as the endocannabinoid system and the two receptors are best known as the CB1 receptor and CB2 receptor.
These receptors are cell membrane receptors and are part of the G- Protein-coupled receptors (GPCRs) superfamily of receptors.
To achieve receptor activation one of three groups must be present:
- ligands (endogenous cannabinoids)
- cannabinoids (Cannabidiol from the cannabis plant)
- synthetic cannabinoids (agonists from pharmaceutical companies)
What is the Endocannabinoid System?
To best understand the cannabinoid receptors it is important to first have a working knowledge of the endocannabinoid system to which they belong.
The endocannabinoid system is an important communication system within the body and is responsible for a wide variety of functions. The functions primarily include a person’s feeling of physical and emotional well-being.
This system will react with the body’s natural cannabinoids, like anandamide, to produce associated effects.
However, when cannabinoids from outside the body, such as those from the cannabis plant, enter they compete for binding sites on these receptors and overwhelm them producing greater effects or bringing the unbalanced person back to homeostasis.
Cannabinoid Receptors in the Human Body
Within the human body, the GPCRS receptors (CB1 and CB2) play special and specific roles. They both have their own unique locations throughout the body and play a role in bringing about specific changes based on their signaling pathways and activation by cannabinoids.
The CB1 receptors are located and have expressions in the brain, lungs, kidneys, and liver located on the endothelial cells of these areas. The CB1 receptors carry with them some important responsibilities in the body.
They primarily govern sleep, pain sensations, and appetite. When they are exposed to ligands, endogenous cannabinoids naturally occurring in the body, these occurrences they govern are brought to a homeostatic state.
However, when external cannabinoids enter the body, higher levels of cannabinoids are present. When exposed to these additional cannabinoids from the cannabis plant the receptors become “over-reactive.”
This over-reaction created is not necessarily a bad thing, it leads to an increase in the already positive effects of cannabinoids.
Because they create a heightened response a person suffering from insomnia may benefit with improved sleep, chronic pain may be lessened, and a patient with a low appetite may suddenly feel hungry.
The CB2 receptors are located primarily in the peripheral tissues of the immune system and hematopoietic cells. They are also, notably, expressed on the T-Cells, Macrophages, and B-Cells which are all associated with the body’s immune system.
Because they are located on these particular cells they carry anti-inflammatory properties. The CB2 receptors are also located on the peripheral nerve terminals.
How Cannabinoid Receptors Work
The writers of PlantEdu explain the workings of the cannabinoid receptors through a lock and key analogy. The two primary components of the endocannabinoid system are the cannabinoid receptors and the cannabinoids.
The two exogenous cannabinoids that have been discovered to work with this system are THC and CBD from the cannabis plant.
THC and CBD are the keys and the locks are the cannabinoid receptors. When a person takes in THC or CBD it begins looking for “locks.”
When the keys (THC and CBD) find the locks (cannabinoid receptors) they attach and instantly begin signaling and sending messages through the body for certain responses to take place. Some of these include pain relief or reduced inflammation based on the specific receptor type and location.
Within the body exists two primary naturally occurring cannabinoids (ligands) which are fatty-acid amides, Anandamide (AEA) and 2-Arachindonoylglycerol (2-AG). An agonist will mimic the ligand and produce similar effects. The agonist of these cannabinoids is THC and CBD, the G-proteins from cannabis.
The endocannabinoid system can be suppressed and/or the body can also have low levels of naturally occurring cannabinoids which can create unwanted health effects. Being able to supplement them with CBD can bring the body back to homeostasis or greater.
A 1990 study conducted by Lisa Matsuda and her colleagues at the National Institute of Mental Health showed how THC triggers cannabinoid receptors in the brain and central nervous system, which is located in the brain and spinal cord.
In this study, mice were genetically altered through site-directed mutagenesis to not contain the THC binding site, CB1 receptor, and then observed the binding assay of THC through western blot analysis.
When the mice, nicknamed “knockout mice” were given THC the study showed that no psychoactive effects were produced because the THC had nowhere to bind. This showed that THC, and other cannabinoids, worked through activating receptors.
CB1 Receptor Effects
Because the CB1 Receptors are located in the brain and are closely tied to the central nervous system they have a notable effect on mood and emotional well-being. They are also located in the lungs, liver, and kidneys giving them secondary effects on the gastrointestinal system.
While there are two cannabinoid receptors, that are known at present, the CB1 receptor is most responsible for the psychoactive effects of THC and seems to produce the most note-worthy side effects when combined with exogenous cannabinoids.
Lowers Stress And Anxiety
Hormones GABA and serotonin impact the body’s emotional balance and the levels of stress and anxiety a person experiences.
CBD and THC can influence the neurotransmitter release and binding affinity of these hormones, thereby, reducing anxiety and the stress response. Studies show that mice without CB1 receptors had higher levels of anxiety.
Because CBD and THC can cross the blood-brain barrier and impact the neurons for emotional stability, they are able to produce a long-term persistent strengthening of the CB1 and CB2 receptors and the body’s ability to reach emotional homeostasis.
Helps With PTSD
When a person experiences psychological stress the natural cannabinoid AEA is negatively impacted. This can then lead to cortisol release and lowered binding ability to the CB1 receptor. Administering an exogenous cannabinoid-like THC and CBD has shown to influence the neurons.
The rates of depression and anxiety in the United States alone are staggering. Pharmaceutical companies seem to produce new drugs almost annually to treat the causes and symptoms of these conditions, but they often carry their own side-effects.
When CBD or THC binds to the CB1 receptor they aid in regulating the hormone GABA and the glutamatergic neurons which impact mood. A person with a suppressed cannabinoid system will have lower levels of GABA and these important hormones for mood regulation and stability.
By administering the agonists of natural cannabinoids the body can begin to repair itself and reach emotional homeostasis by reactivating the CB1 receptors and encouraging them to be more susceptible to cannabinoid attachment.
Lowers Intestinal Inflammation
Inflammation is a natural immune response. But, when the immune system is overstimulated, as with the poor quality of food intake, this inflammation can create negative health consequences.
The Standard American Diet has created diet-induced obesity and intestinal inflammation increases cardiometabolic risk factors and produces excess adipose tissue, and insulin resistance.
The mast cells are a group of cells that are important in the immune response of inflammation. These cells can become over-responsive and cause gastrointestinal issues.
Inflammation in the gut is painful and disrupts the quality of life of the sufferer. Research is showing that CBD may play a role in the inhibition of these cells and their impact on the inflammation of the mucous membranes of the intestines.
Helps With Sleep
Serotonin is the hormone most associated with sleep. When this is low in the body it can heavily impact a persons quality and quantity of sleep.
The CB1 receptors in the brain encourage the release of this hormone, but when it is under-active or has little cannabinoids to trigger its activation, sleeplessness and insomnia may ensue.
By taking in exogenous cannabinoids the sleep-deprived sufferer may find relief of their symptoms.
Cannabinoid Receptors And The Entourage Effect
When studies are conducted on the benefits of CBD most use synthetically produced CBD which is a single molecule. When CBD is extracted from the cannabis plant it contains THC and up to 400 other potentially beneficial compounds.
The cannabinoid system has been shown to respond more positively to CBD that has been extracted from the whole plant and this is due to the “entourage effect” that the other compounds produce.
CBD alone is beneficial, but when coupled with the plants’ other components, the cannabinoid receptors show how the individual parts of the plant have their own unique benefits.
The Importance Of The CB1 Receptor
The cannabinoid receptors are exceptional groups of receptors in the body and are still being further understood.
The CB1 receptor is proving to be a leader in the system in terms of therapeutic benefits it creates when working properly and receiving the maximum amount of cannabinoids it needs.
As studies show, without the CB1 receptor the body becomes unstable in just about every area:
While there is still more to learn about this incredible system and the CB1 receptor specifically, it is already understood that it is beneficial and a major part of the body’s overall health and homeostasis.
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