WELCOME TO THE CBD SCIENCE PAGE
From our ‘What is CBD’ page you may have dipped your toes into CBD and the Endocannabinoid system. In this page, we really go into details of the Endocannabinoid system, CBD, THC, other THC and the impact of Cannabinoids on the body.
The content here is pretty heavy in terms of CBD Science, but it is what we are passionate about. Anytime your stuck on terms mentioned in the page, head over to our CBD Glossary. We want to help alter the perception about CBD products and we are determined to publish content to make it as easy as possible in order to help you ‘educate yourself’ in the World of CBD.
CBD (Cannabidiol) and THC (delta-9-tetrahydrocannabinol) are compounds called Cannabinoids. Cannabinoids are compounds that interact with an unfamiliar system in the body called the Endocannabinoid system. As Cannabinoids such as CBD and THC come from a plant, they are known as Phytocannabinoids.
A CBD compound is made up of Carbon, Hydrogen and Oxygen atoms. The image over on the right shows the structure of the CBD compound.
You already have Cannabinoids in your body assisting your Endocannabinoid system, these are called Endocannabinoids. Phytocannabinoids such as CBD can optimise your Endocannabinoid system, by signalling to the body to use more of its OWN Cannabinoids.
It happens to be how CBD does NOT ‘fit’ with the Endocannabinoid system which owes to it’s function in the body. CBD indirectly influences the Endocannabinoid system, playing a critical role in a vital process in the body called Homeostasis.
HOMEOSTASIS REFERS TO STABILITY, BALANCE OR EQUILIBRIUM
Primarily, the Endocannabinoid system is so important because it works towards maintaining Homeostasis in the body. Homeostasis encompasses the brain, endocrine, and immune systems, to name a few and refers to balance, stability and equilibrium within the entire body.
The Endocannabinoid system utilises chemical signallers and cannabinoid receptors to maintain balance and homeostasis in nearly every system and tissue in the body.
Homeostasis is a Greek work; ‘homeo’ meaning similar and ‘stasis’ meaning stable.
AN EXAMPLE OF THE ENDOCANNABINOID SYSTEM POSITIVELY INFLUENCING HOMEOSTASIS IS INFLAMMATION IN THE BODY. LET’S TAKE A BROKEN TOE:
Immediately after damaging the toe, the immune system signals for blood cells to travel to the site of damage. Inflammation begins - Great! But, too many signals for blood cells to travel to the toe would continuously trigger inflammation in the toe, leading to further damage. The Endocannabinoid system recognises excessive signals and intervenes with nerve cells to prevent the signaling and stop blood cells travelling to the toe, reducing the need for an increase in inflammation and allowing the toe to recover.
The CBD (Cannabidiol) compound is made up of:
21 Carbon atoms
30 Hydrogen atoms
2 Oxygen atoms
YOU ALREADY HAVE CANNABINOIDS NATURALLY PRODUCED BY YOUR BODY. PHYTOCANNABINOIDS, SUCH AS CBD, CAN OPTIMISE YOUR ENDOCANNABINOID SYSTEM BY PROMOTING THE USE OF THE CANNABINOIDS ALREADY INSIDE YOUR BODY!
Other examples of homeostasis include:
Thermoregulation (regulation of body temperature)
Glucoregulation (regulation of blood sugar levels)
Osmoregulation (regulation of water and dissolved minerals)
Water pressure and blood pressure regulation
Blood pH regulation (quantities of Hydrogen molecules in the blood)
INTRODUCTION TO THE ENDOCANNABINOID SYSTEM
You have heard of the skeletal system, the respiratory system, the muscular system, the circulatory system, the digestive system, the nervous system, well here goes the Endocannabinoid System…
Long story short, the Endocannabinoid system is not well known about due to oppression of scientific research into cannabis plants. With acts such as the Marijuana tax act of 1937 in the USA, which essentially banned Cannabis use and sale, with ignorance towards Cannabidiol (CBD) and focus only on the psychoactive delta-9-Tetrahydrocannabinol (THC) portion of the Cannabis plant. It was not until the 1960s, when cannabis research really heightened and research on the Cannabis plant Cannabis sativa L. resulted in the discovery of the Endocannabinoid system (ECS).
The Endocannabinoid System (ECS) is a signaling pathway that occupies the:
i) Central Nervous System: Brain & Spinal Cord
ii) Peripheral tissue
iii) Immune pathways
The binding of Cannabinoids, such as CBD, to receptor sites within the Endocannabinoid system triggers physiological responses in the body. Check out the summarised distribution of Cannabinoid receptors, CB1 and CB2 on your man below:
A major component on the Endocannabinoid system are the Endocannabinoid receptors, CB1 & CB2, which are distributed throughout the body.
Signalling pathways: a pre-synaptic neurone and a post-synaptic neurone. Signalling between synapses in the body is vital for the functioning of processes in the entire body. Signalling demonstrated in the image above is vital for the functioning of all systems in the body.
WHY IS THE ENDOCANNABINOID SYSTEM SO IMPORTANT?
The Endocannabinoid system has a wide scope of influence due to the abundance of cannabinoid receptors located anywhere, from immune cells to neurones.
Basically, the Endocannabinoid system can be influenced throughout the entire human body.
CBD SCIENCE - THE ENDOCANNABINOID SYSTEM
Okay…so here is where we go into some serious CBD Science…
The Endocannabinoid system is found in all vertebrates. So yes, Cats and Dogs have an Endocannabinoid system! There is conflicting evidence in regards to whether invertebrates have an Endocannabinoid system. Studies have proposed that since the Endocannabinoid system worked so well, it was retained during evolution and that invertebrates can serve as a model to study endogenous cannabinoid singling. However, other research has shown the Endocannabinoid system does not exist in invertebrates.
WHY IS THE ENDOCANNABINOID SYSTEM SO IMPORTANT?
Sallaberry and Aster (2018) proposed three reasons why the Endocannabinoid system is so important:
1) the Endocannabinoid system is a retrograde system, referring to its potential to alter signals. It is the ‘master regulator’ in the human body
2) Endocannabinoid receptors are distributed abundantly and widely throughout the body
3) Cannabinoids (such as CBD) do not stay in the body for long in high amounts, they are rapidly processed and degraded in the body, potentially making them more tolerable and less addictive than alternative methods of therapy.
WHAT IS THE ENDOCANNABINOID SYSTEM MADE UP OF?
The Endocannabinoid System is comprised of the following:
1) Endocannabinoids – cannabinoids produced endogenously (within the body). Yes, your body already has and produces cannabinoids, referred to as Endocannabinoids, produced naturally.
2) Receptors sites – CB1 & CB2. Receptors and their sites are vital for all functions in the body. Therein, CB1 & CB2 receptors/sites are vita for processes of the Endocannabinoid system.
3) Enzymes – Enzymes are proteins that act as biological catalysts, meaning they speed up reactions without being used up.
Endocannabinoids are Cannabinoids developed naturally in the body. The body already produces compounds similar to CBD and these molecules are called Endocannabinoids.
Features of the Endocannabinoid system are seen in the earliest embryonal stages and throughout pre- and postnatal development and Endocannabinoids and the Endocannabinoid system play an essential role for development and survival.
THERE ARE 2 MAIN ENDOCANNABINOIDS (ENDOGENOUS CANNABINOIDS, PRODUCED IN THE BODY):
1) 2-AG (2-Archidonylglycerol)
2-AG is the most abundant Endocannabinoid in the human body. It was first discovered by Raphael Mechoulam and Shimon Ben-Shabat in 1995. 2-AG is an ester formed from omega-6-arachidonic acid and glycerol. It has a chemical structure similar to anandamide. 2-AG is prevalent in the CNS (Central Nervous System).
Due to its high prevalence in peripheral immune cells, it seems to have high anti-inflammatory properties. It also functions as a psychoactive endocannabinoid when it binds to CB1 receptors within brain cells.
The molecule 2-AG (2-Archidonyl Glycerol), the most prevalent endogenous endocannabinoid. A molecule of 2-AG has 23 Carbon atoms, 38 Hydrogen atoms and 4 Oxygen atom.
2-AG is considered a full agonist of the CB1 and CB2 receptors. We will touch on agonists and antagonists later on when we discuss the second component of the Endocannabinoid system; Receptor sites.
Anandamide, also known as N-arachidonoylethanolamine (AEA) is the second most prevalent Endocannabinoid in the human body. Anandamide was the first endogenous cannabinoid discovered in the body, discovered in 1992. Anandamide may be a very important cannabinoid to manipulate for controlling pain stimuli. This is due to an interesting quality of Anandamide in which the concentration of Anandamide dictates the type and number of receptors activated.
The molecule Anandamide, an endogenous cannabinoid. A molecule of Anandamide has 22 Carbon atoms, 37 Hydrogen atoms, 2 Oxygen atoms and 1 atom of Nitrogen.
Anandamide also has the ability to make or break short-term connections between nerve cells that directly affect memory. There is speculation whether Anandamide dulls and removes not only physical pain but psychological discomfort as well. If so, this could be utilized to help individuals with post-traumatic stress disorder (PTSD).
Anandamide has also been shown to bind with a strong affinity to the CB1 receptors, which may play a greater role in the analgesic effects (pain relieving effects) of the endocannabinoid.
Research has shown that the presence of CBD in the body increases Anandamide levels by preventing the breakdown of Anandamide and also the re-uptake of Anandamide for other uses. This is an example where CBD has the potential to help those with pain/discomfort issues.
WHY SO MUCH EMPHASIS ON ENDOCANNABINOIDS?
It is important to consider Endocannabinoids when considering CBD and the Endocannabinoid System. This is because CBD is believed to direct the body towards utilising greater quantities of Endocannabinoids. So it could be seen that it Is not the direct effect of CBD that influences your body, but the indirect effects caused by CBD encouraging the body to use more of its OWN naturally produced Cannabinoids (Endocannabinoids).
An example of the indirect effects of CBD on the Endocannabinoid System is in the prevention of the destruction of the Endocannabinoid Anandamide. CBD reduces the action of the enzyme responsible for degrading Anandamide, FAAH (Fatty Acid Amide Hydrolase). Without the action of CBD, the FAAH enzyme would reduce the processes Anandamide is responsible for and diminish the Endocannabinoid System. Remember, from focusing on Anandamide above: Anandamide also has the ability to make or break short-term connections between nerve cells that directly affect memory. There is speculation whether anandamide dulls and removes not only physical pain but psychological discomfort as well.
RECEPTOR SITES (CB1 & CB2)
Seeing as the Endocannabinoid System is believed to have more cellular receptors than any other receptor system in the body, the importance of receptor sites cannot be underestimated.
A QUICK INTRODUCTION TO RECEPTORS
Receptor are vital for singling in all systems throughout the entire human body. Without receptors, processes within the body simply would not occur. Signalling in the body for vital communication takes place via these receptors.
Receptors are proteins, that are located mainly within the cell membranes of all human cells. Receptors are responsible for:
i) the entry and exit of substances in and out of all cells in our body
ii) cell to cell communication via signalling
i) the entry and exit of substances in and out of all cells in our body:
A small number of molecules are small enough to pass through the cell membrane and enter/exit the cell freely. However, the majority of substances in the body are too large to simply fit through gaps in the cell membrane, therefore, they have to use receptors and their sites in order to pass through.
ii) cell to cell communication via signalling
The receptor sites are not just vital for the entry and exit of substances. The receptors assist signalling in the body. Receptor involvement in cell to cell communication is vital in the functioning of the Endocannabinoid system and is what we will focus on in the next section. As discussed above when we introduced the Endocannabinoid system, the Endocannabinoid system is a signalling pathway and it is important to understand receptors, receptor sites and signalling molecules (CBD, THC, Anandamide, 2-AG and many more) in order to understand how the Endocannabinoid system functions.
The cell membrane surrounds the entire cell and regulates the entry and exit of substances in and out of the cell.
WHEN DEALING WITH RECEPTORS OF THE ENDOCANNABINOID SYSTEM, WE ARE TALKING ABOUT CB1 & CB2 RECEPTORS
Check out of CBD History page to learn more about the discovery of CB1 & CB2 receptors. CB1 & CB2 receptors are the most known Endocannabinoid receptors. There is believed to be a third Endocannabinoid receptor, GPR55. Scientists believe that inhibiting the overexpression of the GPR55 receptor could be a potential target for cancer therapy. Research suggests that the GPR55 is activated by the illegal cannabinoid THC, so we’ll stay clear of the GPR55 for the time being!
THE LOCATION OF CB1 AND CB2 RECEPTORS
CB1 receptors - located in the Central Nervous System (CNS), including the brain
CB2 receptors - located mainly in the immune system and peripheral cells
CB1 receptors are also expressed by some non-neuronal cells, including immune cells, whereas CB2 has been recognised on some neuronal cells, either within or outside the brain, even if its role remains to be better clarified.
Both CB1 receptors and CB2 receptors are members of the seven-transmembrane G protein-coupled receptor superfamily. CB1 & CB2 receptors are G-protein coupled receptors. G-protein coupled receptors detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular response. Internal signal transduction pathways are vital of the functioning of the Endocannabinoid system.
Notice the CB1 and CB2 receptors of the Endocannabinoid system have a wide distribution throughout the body. The Endocannabinoid system has a wide scope of influence due to the abundance of cannabinoid receptors located anywhere, from immune cells to neurons (then photo of all the receptors in the body.
TIME TO TALK SHAPE…
CB1 and CB2 receptors are found embedded in the cell membrane of neurones, synapses and immune cells. The interaction of cannabinoids such as CBD and the CB1 and CB2 receptor sites is what regulates the Endocannabinoid system
THE ENDOCANNABINOID SYSTEM IS BELIEVED TO HAVE MORE CELLULAR RECEPTORS THAN ANY OTHER RECEPTOR SYSTEM IN THE BODY.
These receptors have receptor sites. For a chemical to enter the cell, it has to fit perfectly into this receptor site in order for a series of chemical reactions to occur in order for the chemical to finally enter.
The shape of the molecule attempting to enter the cell and the receptor site has to be complementary in order for a perfect fit and subsequent cascade of biochemical reactions which influence cell signalling.
The complementary shape of signalling molecules and receptor sites can be described best by thinking of a lock and key analogy.
Notice how the Endocannabinoid, Anandamide, has a complementary shape to the CB1 receptor site. Whereas, the CBD molecules is unable to ‘fit’ into the CB1 receptor site. We will go into more detail later how CBD does not ‘fit’ into the receptor site of the CB1 or CB2 receptor.
RECEPTOR SITES & CBD
It is the interaction of the CB1 and CB2 receptor sites with cannabinoids such as CBD that leads to a series of chemical reactions that creates an effect on the Endocannabinoid System.
Take a look at the image on the right. The vast distribution of CB1 and CB2 receptors throughout the body can be seen.
But, take a look at the different shapes of the CB1 and CB2 receptors sites in the cell membrane (the layer between the outside of the cell and the inside of the cell).
Cannabinoids (CBD, THC, Anandamide, 2-AG and more) also have a specific shape and their ‘fit’ with the CB1 & CB2 receptors will be different.
The cannabinoids Anandamide, 2-AG and THC are all able to bind with and active both CB1 receptors and CB2 receptors. Surprisingly, CBD does NOT fit into the receptor sites of CB1 or CB2 receptors. CBD is said to have a low affinity for CB1 and CB2 receptors. Instead CBD encourages other Cannabinoids to be used by the Endocannabinoid system for signalling and delay the uptake of Endocannabinoids.
The signalling molecule, known as a Ligand, has to fit perfectly into the receptor site of the receptor in order for a cascade of reactions that allow signalling to follow.
CBD AND MOOD: 5-HT1A
CBD may not interact with CB1 receptors or CB2 receptors, but CBD does interact and activate 5-HT (5-HT1A) receptors involved with Serotonin (5-HT), a mood hormone. The signalling of the Serotonin hormone is linked to anxiety and depression. A recent study by Shannon et al (2015) indicated that the activity of CBD at 5-HT1A receptors may drive its neuroprotective, antidepressive, and anxiolytic benefits, although the mechanism of action by which CBD decreases anxiety is still unclear.
As discussed above, the shape of the CBD molecule means it does not fit and does not activate the CB1 & CB2 receptors of the Endocannabinoid system. But, CBD does activate the 5-HT1A, Serotonin receptor. CBD is said to have a low affinity for CB1 and CB2 receptors.
CBD AND PAIN
CBD is believed to interact with inflammatory responses in the body. Inflammation refers to the painful swelling and redness of tissue caused as a result of infection or tissue damage. Despite inflammation being an important process carried out by the immune system, over activity by the immune system can lead to too much on an inflammatory response, which is where autoimmune issues, allergies and other symptoms occur.
CBD AS AN ANTI-INFLAMMATORY SUPPLEMENT
CBD is believed to aid in over-inflammatory instances by preventing a process known as chemotaxis. Chemotaxis is an immune response to injury or damage and causes immune cells to migrate to the site of damage. CBD interacts with the Endocannabinoid system to turn off chemotaxis, preventing too many cells to migrate to the site of damage, acting as an anti-inflammatory supplement.
CBD IS ALSO BELIEVED TO BIND CB2 RECEPTORS (NOT SPECIFICALLY TO THE CB2 RECEPTOR SITE) WHICH ARE ACTIVE IN THE IMMUNE SYSTEM, THUS FIGHTING INFLAMMATION AND REDUCING PAIN AT ITS SOURCE!
Last but not least, there are the Enzymes involved in the Endocannabinoid system. Enzymes are biological molecules that speed up the rate of reactions in the body. The enzymes in the Endocannabinoid system are responsible for creating and breaking down various Cannabinoids in an attempt to optimise the performance of the Endocannabinoid System.
The enzymes involved in Endocannabinoid metabolism are emerging as very important regulators of endocannabinoid function at peripheral and neuronal levels. Better understandings of these enzymes in pathophysiological conditions will largely contribute to develop selective inhibitors, which may be useful for the development of novel therapeutic drugs (Basavarajappa, 2007).
OKAY, LET’S CLEAR UP THE TOPIC THAT PERCEIVES CBD IN A NEGATIVE LIGHT. CBD IS CLOSELY ASSOCIATED WITH THE COMPOUND THC, AN ILLEGAL COMPOUND THAT MAKES USERS HIGH! CBD DOES NOT MAKE USERS HIGH, THE CONTENT BELOW GOES INTO MORE DETAIL ON CBD AND THC…
CBD & THC
>THC has a high affinity for CB1 and CB2 receptors
>CBD has a low affinity for CB1 and CB2 receptors.
Affinity refers to the strength of a molecule to bind to a receptor site. Therefore, THC directly binds to the receptor sites on CB1 and CB2 receptors and activates them, leading to a cascade of reactions resulting in changes in signalling. CBD does not directly bind to CB1 and CB2 receptors.
THC and marijuana are classified as class-B illegal drugs. CBD is not a drug.
CB1 receptors are responsible for most signalling in the Endocannabinoid system in the brain. When THC enters to the body, it binds with CB1 receptors in the brain due to it’s high affinity for CB1 receptors. The binding of THC with CB1 receptors causes activation of the CB1 receptors in the brain, decreasing the release of neurotransmitters in the brain and causing a psychoactive effect (a ‘high’).
Most importantly, CBD does not create a psychoactive effect (a ‘high’) as has a low affinity for CB1 receptors and therefore does not bind with CB1 receptors to activate them. Our CBD products contain less than 0.2% THC (we have certification to support this) and are classed as food supplements.
It is easy to mix up CBD and THC. We try and break it down for you.
Research has shown that the mechanism by which a ‘high’ is created occurs when THC is absorbed in the body and completes a complementary bind with CB1 receptors in the brain. This binding causes a cascade of biochemical reactions which decrease neurotransmitter release in the brain and leads to a ‘high’ effect. As discussed above, CBD is unable to bind to CB1 receptors, so it does not create a ‘high’.
Marijuana plants are usually cultivated to create buds with a rich THC content. Whereas Hemp plants are cultivated with a low THC content in mind. Additionally, CBD products are produced with a low THC content (broad-spectrum CBD should contain less than 0.2% THC). The CBD in our CBD products come from the Cannabis sativa L. plant, generally known as industrial Hemp. Industrial Hemp is cultivated to produce CBD-rich buds with a low THC content.
Furthermore, CBD has shown to neutralise the psychoactive effects of THC. When CBD is absorbed in the body, it interacts with the Endocannabinoid system, reducing the binding of THC to CB1 and CB2 receptors, disrupting the biochemical reaction that lead to a high. It is this interaction of CBD in the body which is why CBD is believed to be useful for individuals fighting substance abuse.
The similarities and differences between CBD and THC on a structural level can be seen below:
With the exact same number of Carbon, Hydrogen and Oxygen atoms, you would think CBD and THC would behave similarly in the body. However, it is the difference in structure (shown above) that differentiates their use in the body. Just the differences in the Cyclic ring in THC and the Hydroxyl group in CBD leads to a difference in structure and thus shape. With a difference in shape comes altering interactions with receptors sites, such as receptor site on CB1 and CB2 receptors. Image taken from:
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