Human CBD Receptors Have Been Found!

Christine Colbert March 4, 2020 0 comments

How does CBD work inside the human body?

As cannabis research progresses, there is a lot to know about cannabidiol (CBD). And with the legalization of hemp in the United States, it might be edging out THC as the most popular cannabinoid among consumers.

CBD has been lauded as a helpful tool in fighting pain, inflammation, anxiety, and addiction. And for people who aren’t interested in the intoxicating qualities of THC, the best part about CBD is that it doesn’t make you high. That’s because THC and CBD affect the body in different ways.

It all comes down to the endocannabinoid system (ECS), and how CBD interacts with cannabinoid receptors in the body. These receptors reside on the surfaces of cells, and convey messages coming from endocannabinoids, like anandamide and 2-arachidonoylglycerol (2-AG). Depending on the type of cell, these messages initiate various responses.

Cannabinoid receptors exist throughout our bodies, and the two main types are CB1 and CB2 receptors. CB1 receptors are mainly found in the nervous system, in the brain, neurons and spinal cord. These are also found in the digestive tract. CB2 receptors are largely found in peripheral organs and are associated with the immune system.

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How CBD Interacts with Encocannabinoids

Unlike THC, CBD has a low affinity for binding with cannabinoid receptors. That may be why it doesn’t produce the same intoxicating high as THC. CBD modulates the receptors, affecting how they respond to certain cannabinoids. It also modulates receptors that aren’t cannabinoids, and it can enhance the effects of endocannabinoids, like anandamide.

For instance, CBD interacts with fatty acid binding proteins (FABP), which transport endocannabinoids. By preventing the breakdown of anandamide, CBD raises the levels of this endocannabinoid in the brain. That’s one reason why CBD has the potential to be effective in treating seizures.

It’s in this same way that CBD can also increase levels of adenosine in the brain. By allowing the accumulation of adenosine, CBD can help induce sleep, ease anxiety and lower inflammation. But interacting with FABPs isn’t the only way CBD affects the body. CBD also inhibits fatty acid (FAAH) enzymes, increasing levels of anandamide and 2-AG — which also ease anxiety and calm the mind.

human cbd receptors helping young white girl to relax and smile

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Human CBD Receptors

CBD doesn’t just interact with endocannabinoids. It has an effect on a variety of other signal mechanisms in the body, including non-cannabinoid receptors.

By activating the 5-HT1A (hydroxytryptamine) receptor, it can work to further ease anxiety. The 5-HT1A is part of a matrix of receptors that respond to serotonin — a neurotransmitter involved with anxiety, pain, digestion, mood, blood clotting and appetite. By activating 5-HT1A, CBD can ease anxiety, and according to this study — published in the journal Pain (2009) — possibly alleviate pain as well.

But that’s not the only receptor CBD interacts with to calm anxiety. In this study, published in Pharmacological Research (2017), scientists discovered that CBD and 2-AG were both modulators of the GABA-A receptor. In this way, CBD enhances GABA — which creates an anti-anxiety effect.

And what about those cancer-fighting properties of CBD we’ve heard so much about? They come from CBD’s ability to activate peroxisome proliferator activated receptors (PPAR). By serving as an agonist of the PPAR-gamma receptor, it can prevent the progression of cancer. Science has suggested that activating this receptor also promotes a neuroprotective effect.

Pathways to Killing Pain and Inflammation

Through various interactions with receptors, CBD also confers its famed anti-inflammatory and pain management effects. CBD binds to TRPV1 receptors, which play a role in fighting cancer. TRPV is short for “transient receptor potential cation channel subfamily V,” the “v” stands for vanilloid. These receptors are protein complexes that control the flow of ions. Through binding with this receptor, CBD can also affect the perception of pain by reducing sensitivity.

CBD also works to fight pain and inflammation by serving as an antagonist of GPR55. Through working to block the signaling of this G-protein coupled receptor, CBD can relieve inflammation and pain. Inhibiting this receptor also decreases the spread of cancer cells.

Seeing a trend? Much of what CBD does in the body overlaps among receptors and signal pathways. CBD’s activation of PPARg receptors also reduces gene expression in inflammation resulting from oxidative stress. It might also help with treating Alzheimer’s disease.

jhuman cbd receptors helping older adults stretching in a yoga class

Science is Still learning About CBD and Receptors

Right now, scientists are still learning about the ECS and human CBD receptors. But what we know so far is that the ECS is sensitive to stimuli. You can feed your ECS for more balanced health by exercising, consuming plenty of omega-3 fatty acids and reducing stress. Cannabinoids like CBD and THC can also help in treating conditions that affect this system.

The ongoing research into cannabis is exciting due to its remarkable potential to rebalance the ECS. As science continues examining the clues, we may see an emergence of treatments that target specific receptors, in order to battle disease and illness caused by a malfunctioning ECS. This much is clear, CBD conveys a multitude of therapeutic effects through an array of receptors that we’re only just beginning to understand.

References

De Gregorio, Danilo, et al. “Cannabidiol Modulates Serotonergic Transmission and Reverses Both Allodynia and Anxiety-like Behavior in a Model of Neuropathic Pain.” Insights.ovid.com, insights.ovid.com/crossref?an=00006396-201901000-00016.
Bakas, T, et al. “The Direct Actions of Cannabidiol and 2-Arachidonoyl Glycerol at GABAA Receptors.” Pharmacological Research, U.S. National Library of Medicine, May 2017, www.ncbi.nlm.nih.gov/pubmed/28249817.
Stahel, Philip F, et al. “Peroxisome Proliferator-Activated Receptors: ‘Key’ Regulators of Neuroinflammation after Traumatic Brain Injury.” PPAR Research, Hindawi Publishing Corporation, 2008, www.ncbi.nlm.nih.gov/pmc/articles/PMC2276625/.
Lauckner, Jane E, et al. “GPR55 Is a Cannabinoid Receptor That Increases Intracellular Calcium and Inhibits M Current.” Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 19 Feb. 2008, www.ncbi.nlm.nih.gov/pmc/articles/PMC2268199/.
Mijangos-Moreno, Stephanie, and Gloria Arankowsky-Sandoval. “Intrahypothalamic Injection of Cannabidiol Increases the Extracellular Levels of Adenosine in Nucleus Accumbens in Rats.” ResearchGate, 2014, www.researchgate.net/publication/262109303_Intrahypothalamic_injection_of_cannabidiol_increases_the_extracellular_levels_of_adenosine_in_nucleus_accumbens_in_rats.