As the research into CBD and its effects continues to grow, we’ve been able to understand more about how it interacts with our bodies. Although there’s still a lot we don’t understand, we’ve been able to learn some cool things about how it affects our physiology.

Cannabidiol (CBD) is a phytocannabinoid found within the flower of the cannabis plant. Not unlike THC, it contributes to the plant’s therapeutic properties. However, CBD is unique and doesn’t produce the same high that THC is known for.

So far, studies have suggested that CBD can help with everything from mental health disorders to autoimmune diseases, gut disorders, metabolic syndromes, and cardiovascular dysfunction.  Currently, however, there are only two approved CBD-derived drugs available on the market: Epidiolex, which is a treatment used to help mitigate epileptic seizures, and Sativex, a pain management prescription. .

That said, with so many individuals and companies making claims about the benefits of CBD, we think it’s important to understand what the science actually says. That’s why we’ve taken the time to break down some of the research in order to help establish an understanding of what we know so far.

The Endocannabinoid System

The endocannabinoid system (ECS) is a series of receptors and transmitters that help to keep our bodies in homeostasis, or balance. Put simply, when a neurotransmitter (a chemical produced by the body), locks into a receptor, our body is then able to feed off these chemicals and produce results. The ECS contributes to everything from our sleep cycles to managing pain, mood, appetite, memory, stress, and immune responses. When processes start acting up, the ECS works to return us back to our baseline.

There are two main receptor sites in the ECS, called CB1 and CB2. CB1 receptors are largely found in the brain and nervous system. They’re associated with promoting feelings of calm through a chemical called anandamide. CB1 receptors are also linked with decreasing pain, anxiety, and inflammation.

CB2 receptors are found primarily in organs associated with the immune system. These receptors also may be linked with inflammation.

CBD interacts with the ECS in a multitude of ways, some of which are listed below. Mainly, CBD can act as a binding agent, attaching itself to receptors. It also prevents the reuptake, or breakdown, of endocannabinoids like anandamide. Additionally, CBD is also an allosteric modulator, which means it changes the shape of receptors in order to make them more (or less) effective at sending signals and connecting with neurotransmitters.

Basically, when our body struggles to regulate itself, CBD may be able to interact with the receptors in the ECS in order to provide us with the boost we need to return to homeostasis.

5-HT1A – Serotonin Receptors

5-HT1A (hydroxytryptamine) are also referred to as ‘serotonin receptors’ because they’re normally triggered by the chemical serotonin. These receptors are associated with various processes, including anxiety, addiction, appetite, sleep, pain perception, nausea, memory, and mood.

In one study, it was found that CBD activates 5-HT1A receptors, possibly triggering anti-depressant effects. Additionally, CBD, in conjuncture with these receptors, has been shown to help decrease blood pressure and regulate body temperature. A study conducted with animals has also suggested that CBD and 5-HT1A receptors have the potential to help treat depression, anxiety, nausea, and neuroinflammation.

TRPV1 – Vanilloid Receptors

Activated TRPV1, also known as vanilloid receptors, are known for increasing body temperature, inflammation, and signalling pain. In one study conducted, CBD has been shown to inhibit or desensitize TRPV1 signalling, which could have therapeutic pain management applications.

GPR55—Orphan Receptors

GPR55, nicknamed the orphan receptor, also appears to be blocked by CBD. This isn’t a bad thing, however, as it seems that overactive GPR55 has been associated with osteoporosis (though bone reabsorption) and the generation of cancer cells. GPR55 receptors have also been associated with blood pressure and bone density. Through blocking these receptors, CBD might help prevent bone reabsorption and cancer cell proliferation.

However, there’s still a lot we don’t know about GPR55 receptors, including their physiological functions, as the research is both new and limited.

PPARS – Nuclear Receptors

PPARS (peroxisome proliferator activated receptors) sit on the surface of a cell’s nucleus and have been associated with gene expression. This means that they either promote or prevent the transcription of specific genes, generally ones involved in homeostasis, insulin sensitivity, and lipid uptake. CBD activates these particular receptors, and because of the association to metabolic functions, it’s possible that CBD can act as a treatment for diabetes.

More specifically, however, activated PPAR-gamma receptors have been linked to the breaking down and reducing of amyloid-beta plaque, which is connected to Alzheimer’s disease. Since this is the case, there’s a possibility that CBD may be useful as a treatment for Alzheimer’s.

Another specific receptor, named PPAR-alpha, works to prevent the breakdown of our body’s chemicals, specifically anandamide. When activated with CBD, PPAR-alpha can help ensure more of the endocannabinoid is available in our bodies. Additionally, since PPAR-alpha deficiency has been linked to schizophrenia, it’s possible CBD could also be used as a treatment for this disorder.

While there’s been some research to suggest that PPARS activation can help reduce tumours and treat cancer, current studies have shown contradictory results. More research is needed before we fully understand PPARS and the effect CBD has on them.

Reuptake Inhibitor

As a part of its lifespan, anandamide will attach itself to a fatty acid binding protein (FABP). Once connected, it’s free to make the journey passed the membrane and into the cells of the body. This is where it’s broken down by a chemical called fatty acid amide hydrolase (FAAH). This process, where a chemical produced by the body passes into a cell and is broken down, is referred to as ‘reuptake.’

CBD, in some cases, acts as a reuptake inhibitor. In the case of anandamide, CBD will attach itself to the FABPs, preventing anandamide (and other chemicals) from hitching a ride into the cell. Essentially, this means that more of the chemical is available in our bodies. In the case of anandamide, this helps to stimulate feelings of calm and reduces anxiety.

Aside from anandamide, CBD might also impact adenosine reuptake, which regulates activity in the A1A and A2A adenosine receptors. These receptors impact cardiovascular functioning, helping to regulate myocardial oxygen consumption and coronary blood flow. Additionally, these receptors are associated with anti-inflammatory effects. Through preventing adenosine reuptake, more of the chemical is available to help our body maintain balance.

Allosteric Modulator

An allosteric modulator is anything that has the ability to change the shape of a receptor, making it more or less effective at signaling and attaching. As an allosteric modulator, CBD may be able to both amplify different receptors’ binding abilities as well as inhibit them.

In one example, CBD is shown to enhance the GABA-A receptor in a way that allows for easier binding with a chemical called gamma-aminobutyric acid (GABA), which is known for its calming effects. In contrast, CBD appears to change the shape of CB1 receptors, preventing them from binding effectively with THC. In this way, CBD might have the ability to minimize any intoxicating effects. This means that CBD could potentially help treat issues associated with endocannabinoid over-activity, like obesity, cardiovascular issues, or liver disease.

TL;DR

Although we still have a lot to learn about CBD and its effect on the body, what we do know so far is that it works with the endocannabinoid system in order to help maintain our body’s homeostasis. It appears to enhance the beneficial effects of certain receptors (CB1 and 5-HT1A), while blocking other receptors (TRPV1 and GPR55) that are associated with health problems. CBD also seems to be able to change the shape of receptors, making them more or less effective. As the science continues to develop, we look forward to having a deeper understanding of the physiological impact of CBD.