The Endocannabinoid System (ECS) is a relatively newly discovered (1988) biological system that is found in all mammalian species, including humans. Primarily it acts as a central nervous system (CNS) neuro-signaling system.
It was initially discovered by scientists conducting research into how cannabis, and THC in particular, interacted within the human brain to produce the famous high associated with marijuana. It was discovered that delta9 tetrahydrocannabinol (THC) binds directly to an, at the time, undiscovered receptor site found on many cells (primarily CNS and peripheral cells). It was speculated, and later proven, that that binding process directly resulted in the intoxicating effects of marijuana, and specifically THC.
Within a few years, research established that the ECS was a very sophisticated molecular cell signaling system with at least two cannabinoid receptors located on cells throughout the body and named as CB1 and CB2 receptors. It was discovered that endocannabinoids, which are endogenous (produced from within) lipid-based retrograde neurotransmitters, interact directly and indirectly with the CB1 and CB2 receptors.
What are endocannabinoids?
Simply put, endocannabinoids are a group of internally produced neurotransmitters within all mammals that are made up of proteins, ligands, and enzymes. They generally act as modulators, attempting to keep the biological system in balance, which is known as homeostasis in humans.
When a specific set of conditions are faced, the body will automatically produce on-demand endocannabinoids that will interact with the CB1 and CB2 receptors to either turn on, or turn off a particular cellular response that will bring the system back into harmony. Think of a traffic light at a busy intersection. Without this system of signaling when to go or stop, the intersection would soon go out of control and dissolve into chaos.
Endocannabinoids act as the traffic light in a very busy intersection. There are several identified endocannabinoids, and the one in particular we will focus on is anandamide, otherwise known as the bliss molecule.
Anandamide, the human equivalent of THC
Anandamide, also referred to as the bliss molecule, is chemically very similar to THC, which is the most prominent cannabinoid found in cannabis. THC is also the cannabinoid that produces the intoxicating effects in cannabis. If it wasn’t for THC, anandamide may not have been discovered at all. It’s known as the bliss molecule because our mood, anxiety, fear, happiness, and ability to endure stress have all been tied to it.
Anandamide is also known as N-arachidonoylethanolamine (AEA) and is a lipid-based ligand that directly binds to the CB1 receptor. It’s an on-demand endocannabinoid that, when it binds with the CB1 receptor, acts as an agonist and causes a cascade of positive effects that produces euphoria and also regulates stress response, general joyfulness, fear, and pain. This is generally the same effect attributed to THC. To reverse the binding, the system produces an enzyme known as fatty acid amide hydrolase (FAAH) to down regulate or degrade anandamide completely. These two compounds turn on and off as needed to ideally keep the system in balance.
If you are looking for a real world example of the power of anandamide, look no further than the runner’s high. The euphoric feeling after a period of prolonged exercise was long thought to be tied to the dopamine system but has recently been proven to be the direct effect of a flood of anandamide into the ECS system post exertion. An even simpler example: chocolate. Ever wonder why pure chocolate makes you feel so good? Simple. Cocoa (from which pure chocolate is made) is loaded with natural anandamide.
Phytocannabinoids and the ECS
Phytocannabinoids are molecules that are synthesized by the cannabis plant. There are approximately 113 phytocannabinoids identified in the cannabis plant, and they are structurally very similar to endocannabinoids. As we have already discussed, delta9 tetrahydrocannabinol (THC), the most prominent phytocannabinoid in cannabis, is directly akin to the endocannabinoid anandamide and docks to the same CB1 receptor as a potent agonist.
THC has been demonstrated to be much more potent and more resistant to FAAH breakdown than anandamide. This goes a long way to explain how THC produces much stronger effects and for longer periods than anandamide alone.
What about Cannabinol (CBD) you may ask? Where does it fit in? Excellent question. Cannabidiol (CBD) is the second most active phytocannabinoids found in the cannabis plant. It does play a special role, just not in a conventional way.
Cannabidiol (CBD), anandamide, and the ECS.
Unlike THC, Cannabidiol (CBD) does not bind with either CB1 or CB2 directly. This may explain why CBD is completely non-psychoactive and does not produce a high or altered feeling like THC does. It does, however, play a very important regulative role in the ECS. Anandamide is a very fragile molecule that is easily degraded by the enzyme FAAH. Cannabidiol (CBD) has been scientifically proven to inhibit the production of FAAH. Inhibited FAAH, which breaks down anandamide, allows the bliss molecule to hang around a bit longer and to collect in great abundance. By gathering in the system, it continues to distribute its positive effects. More anandamide in the system means a more positive outlook.