Cannabinoids Receptors Function: CB1 and CB2
7 min readUnderstanding Cannabinoids and the Endocannabinoid System
As the opioid crisis gains notoriety as a dangerous plague on the global society, health consumers are increasingly seeking natural homeopathic alternatives as part of a new age of safe, sustainable health. The term “nutraceutical” is coming into use for CBD and other therapeutic herbs, but this is merely a marketing term rather than a formal scientific classification. The recent discovery of the human endocannabinoid system (ECS) has opened the door to that era, leading scientists to take a fresh look at the therapeutic power of the cannabis Sativa L species which includes hemp and marijuana. Cannabinoids function in natural harmony with the human body to provide an astounding range of health benefits, most notably, the CBD cannabinoid derived from the hemp plant.
CBD (cannabidiol) is the most popular therapeutic cannabinoid from the hemp plant which is now legal and widely available in all 50 US states. We’ll also touch on some lesser known cannabinoids which are demonstrating some interesting medicinal properties of their own as modern cannabis research continues.
We’ll begin with the scientist who started it all just about a half a century ago.
Raphael Mechoulam
In the 1960s, Israeli chemist Raphael Mechoulam began his revolutionary research on the therapeutic effects of the cannabis species. His subsequent discoveries revealed how the endocannabinoid system can benefit from supplemental CBD and launched hemp on the slow but steady road to the popular hemp revival we’re experiencing now. Today, Professor Mechoulam is honored as the grandfather of cannabis research, and he continues to be instrumental in leading the promotion of CBD for medical applications.
Cannabinoids
Cannabinoids are the unique chemical compounds found in the cannabis plant species. Many definitions found at popular health and medical sites on the internet are committing an error of omission when they wrongly attribute marijuana as the sole source of cannabinoids. Poor hemp, so often forgotten even today! Ongoing research has uncovered over 100 distinct cannabinoids and work has just begun to discover the therapeutic potential of them all.
CBN (Cannabinol)
Don’t get this cannabinoid confused with cannabidiol (CBD). Cannabinol (CBN) is the result of degraded THC in marijuana which has aged or been improperly stored. Since it derives from THC, and hemp has very little THC content, cannabinol doesn’t occur in the hemp plant. Even young marijuana has very little CBN content since the THC hasn’t had the opportunity for the oxidation necessary to convert it to cannabinol. CBN may have anti-seizure, antibiotic, and anti-inflammatory properties similar to those of CBD. CBN is mildly psychoactive and it also delivers a pronounced “couch potato” sedative effect, making it a good candidate for use as a safe, natural sleep aid.
CBG (Cannabigerol)/CBGA
The CBGA (cannabigerol acid) cannabinoid is the parent cannabinoid source of both CBD and THC. Most CBG converts to CBD in hemp and very little CBG content, less than 1% remains in its original form. In marijuana, a similar percentage converts to THC, so capturing CBG at the right moment can prove to be a difficult process, but it might be worth the effort. CBG shows promising therapeutic potential for treating glaucoma, fighting bacterial infections, alleviating inflammatory bowel disease and muscle spasms, and even as a cancer fighter.
To complicate cannabis science even further, the evidence is pointing to significantly increased potency when the cannabinoids from the entire cannabis plant are all present and working together. This brings us to several useful cannabinoid terms which you’re sure to run across while browsing the booming CBD market.
Synergistic Effect/ Entourage Effect
Two commonly used terms for describing the significantly increased potency and better performance observed when two or more cannabinoids or other plant elements are present and working together.
Full Spectrum CBD
This is the term for CBD which is accompanied by all other available cannabinoids from the whole hemp plant. Terpenes which give the hemp plant its unique aroma also provide the optimized therapeutic benefits of the synergistic effect and are present in full spectrum CBD products.
CBD Isolates or Concentrates
Products containing CBD content alone in its molecular form are marketed as “isolates”. Ironically, CBD isolates may cost more and provide less in the way of pharmacological action due to the lack of the powerful entourage effect described above.
Phytocannabinoids
The term used to distinguish supplemental plant-derived cannabinoids from endogenous, or endocannabinoids produced by the body naturally. Phytocannabinoids can be tricky, morphing from one form to another throughout different phases of cannabis growth and even after harvesting. (see above)
Endocannabinoids
This is the term for cannabinoid compounds produced naturally in the body by the ECS, or endocannabinoid system. The prefix “endo” is of Greek origin translating as “internal” or “within”. This is why CBD is classified as a supplement rather than as a synthetic drug. Even if you’ve never ingested CBD from hemp, or partaken of the occasional toke of marijuana, your body is already making and using its own natural supply of beneficial endocannabinoids.
Endocannabinoid System (ECS)
All mammals have an endocannabinoid system, which is why CBD products for pets are now appearing, along with the plethora of CBD products for humans. The ECS is comprised of the endocannabinoids generated naturally by the body, certain enzymes, as well as an intricate network of cannabinoid receptors designated as CB1 and CB2. As of this writing, scientists are beginning to suspect that a third type of cannabinoid receptor may also be present, but as happens so often in these early stages of cannabis science, further research is required.
The ECS operates primarily in the limbic and paralimbic regions of the brain to regulate important biological processes throughout the body. These vital regions control mood, emotion, fight or flight response, memory, cognitive thought, sleep patterns, appetite, motor control, and more. The ECS is arguably the most significant medical discovery to date, one “that will save more lives than the discovery of sterile surgical techniques” according to Dr. David Allen, a retired cardiac surgeon.
Anandamide
Anandamide was one of the first endocannabinoids identified by Raphael Mechoulam in the early stages of his cannabinoid research. Anandamide is a natural mood elevating substance often referred to as the body’s natural antidepressant. The word “anandamide” is derived from the Sanskrit word for “bliss” and is sometimes referred to as the bliss molecule. CBD can raise levels of anandamide in a unique way by slowing down the enzymatic breakdown of anandamide to allow its effects to last longer. Anandamide also increases “neurogenesis” which is the medical term for fostering the growth of new nerve and brain cells.
2-AG (2-arachidonoylglycerol)
2-AG targets the CB2 receptors of the ECS involved with regulation of appetite, immune system response, inflammation, and pain management.
CB1 cannabinoid receptor
CB1 receptors are located most intensely in the brain and nervous system with some distribution throughout the body, especially the lungs, liver, and kidneys. Raphael Mechoulam was intrigued by the incredible number of these receptors which are more numerous than any other type of neurotransmitter. Cannabinoids from any source can seek out and activate the CB1 receptors to provide relief from pain, nausea, anxiety or depression to name just a few effects.
CB2 cannabinoid receptor
The CB2 receptors are found mainly in the immune system, concentrated in the spleen and gastrointestinal system. Only a small number exist in the brain. CB2 receptors have diverse actions in liver and kidney function, bone and skin condition, and pain management. Changes to CB2 activation are involved with every type of human disease including cardiovascular, neurodegenerative, autoimmune, and psychiatric disorders. Activating the CB2 receptor has been shown to break down the proteins responsible for the plaque which causes Alzheimer’s disease.
Homeostasis
This is the scientific term for that state of overall well-being where all systems are go and everything in mind and body is operating just right. The mission of the ECS is to maintain that optimized state via the complex biocommunication network of CB1 and CB2 receptors.
Endocannabinoid Deficiency
This is the theory behind much of the current research efforts about CBD, cannabinoids, and the operating of the ECS. Many scientists believe that stress, toxic environments, and disease can overwhelm the ECS leaving it with an insufficient supply of natural endocannabinoids. Research is now supporting the conclusion that endocannabinoid deficiency plays a role in disorders such as migraine, irritable bowel syndrome, and chronic pain disorders such as fibromyalgia and other treatment-resistant syndromes.
Conclusion
By now it’s obvious that any human or mammal on the planet can benefit from the wide array of therapeutic properties in supplemental CBD. Working in natural harmony with the body’s own endocannabinoid system, full spectrum cannabidiol from the whole hemp plant is ushering in a new safer era of sustainable health with the nontoxic, non-addictive, non-psychoactive health essential from Mother Nature.
Sources:
Meet Raphael Mechoulam, the ‘father of Cannabis Research’ Who Says CBD Needs to Be Reclassified—Now
https://www.leafly.com/news/cannabis-101/list-major-cannabinoids-cannabis-effects
https://www.leafly.com/news/cannabis-101/what-is-cbg-cannabinoid
https://www.ncbi.nlm.nih.gov/pmc/a