There are many, many more PhytoCannabinoids that have been discovered in the Cannabis plant. To name a few: CBN, THCV, CBC, CBG. Most are present in very small amounts and most we still have not done the research to fully understand what they can do in the human body.
What we do know is that using Cannabinoid products that contain as full a range of Cannabinoids as the plant produces leads to the best results. This full spectrum has been titled the Entourage Effect.
One of the most exciting forms of the PhytoCannabinoids we are working with is the Acid Form. The Acid form is how the plant produces it.
Cannabis scientists had broadly classified the Cannabinoid molecule into 3 groupings. As with everything concerning Cannabis, nothing is hard and fast and no tight and rigid definition really will hold much water, but these family groups do have value to more easily understand the complexities of this molecule.
The Cannabis plant produces all of her Cannabinoid in the Acid Form. You know it’s an acid nomenclature when the name ends with an “A”. It starts as CBGA in the plant. The plant then converts this to THCA or CBDA or CBCA. It is a carboxylic acid. Through some sort of oxidation process, could be temperature or chemical, smoking, vaping and baking fits into this. Then the acid turns into CO2 and we have an alcohol grouping this is called the Netural Family. This is the molecule that we love. THC. Also all the others as CBD, CBG, etc.
Through further breakdown, either in Nature as age, light, oxidation, or in our body’s process of breaking complex molecules down to simpler ones, generally done in the liver. These Cannabinoids are known as Metabolites. CBN is one of these metabolites that gives the headache when cannabis is smoked that has been kept too long but when formulated with THC can be beneficial for insomnia.
So far nearly all the research has gone into Neturals. Only within the last couple of years has more research stated to happen.
A 1969 study showed no psychoactive effects from THCA were seen at high doses with monkeys. Same with mice. And dogs. Nothing has come along to disprove this.
We say that THCA is not psychoactive. With the caveat, “as far as we know.” It does not turn into THC in the body. It enters the body as THCA and leaves the body as THCA
THCA suppresses inflammation that is separate from CB1 or CB2 receptors. It seems that the acid of both THCA and CBDA inhibit Cox enzyme that produces pain and inflammation. CBDA has been shown to be a very potent Cox inhibitor
Another THCA study showed that it represses nausea in rats. WARNING: this is not the kindest treatment of laboratory animals. They gave rats lithium chloride that produces the gagging reflux. They then measured how often they gagged. It took 5mg/kg of THC to suppress gagging. THCA repressed nausea at 1/10th of that dose. .05mg/kg. When increased the THCA dose by 10 it did not get any better. In this model, THCA is 10X more powerful as an anti-emetic than THC.
More on THCA in the next blog.
Cannabinoids made by plants, primarily the cannabis plant
THC: This is the one. Endlessly written about, whose presence in human history has ranged from god-like to devil-sent. Whose persecution for possession has led individuals to lifelong suffering and even death. And this all through millennia of human history.
THC mimics Anandamide and 2-AG by acting as a partial agonist at CB1 and CB2 Receptor sites. An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response. But, THC does not stimulate the receptors all the way. And because it is a partial agonist and not a full agonist, it can at times actually block function and act as an anti-agonist. Antagonism to the receptors, both, is more likely when the ECS is down-regulated, that is, not functioning correctly.
Too high a dose of THC can actually down regulate the ECS and loose efficacy. At a weekly habit of smoking more than 1/8 oz, research has shown that the Receptors become over stimulated and the cells have the good sense of pulling them inward, closing them off. Full benefit from the Cannabinoids is then not gained.
Endocannabinoids are hydrophobic molecules. They cannot travel unaided for long distances in the aqueous medium surrounding the cells from where they are released, and therefore act locally on nearby target cells. They have much more restricted spheres of influence than do hormones, which can affect cells throughout the body.
Over the last two decade or so substantial research has gone into the medical benefits and usage of CBD. Over the last decade the amount of suffering this Cannabinoid is responsible for alleviating, without a doubt, is truly astonishing. We’ve all heard personal testimonies and stories and probably each know someone who has been deeply helped through this Cannabinoid. The amount of research on CBD has also exponentially increased over the last decade.
It is often repeated that CBD is NOT psychoactive. This is not true. CBD does affect the psyche, mildly, generally not impairing perceptions or creating that “stoned” high feeling. It does not affect motor coordination as THC does. It will not get you to that stoned place. But it can change a mood and bring about a psychological shift that can be felt.
Unlike THC, CBD does not attach directly to any of the receptors, but instead indirectly activates Endocannabinoid signaling by suppressing the enzyme fatty acid amide hydroxylase (FAAH). Say it now, “FAAH.”
FAAH breaks down Anandamide, so the more FAAH you have, the less Anandamide there is in the body. Turns out, CBD suppresses the production of FAAH, therefore allowing more Anandamide to be present and strengthening Endocannabinoid tone. The theory being that if you have a condition associated with low levels of Anandamide, taking CBD would return it to optimum levels, which in turn could improve the symptoms.
At this time in its history of research it is still not fully understood exactly how it works on the cellular level. That is, which mechanism is having the clinical effects. But its affects are widespread as are all the Cannabinoids. Very high doses have shown no problems. And it is also effective at very low doses, as low as 1 microgram.
So saying all these things is really repeating what the research is showing and anecdotal stories. Always, Less is Better. Start low. Go slow.
CBD can modulate the effect of THC. That is, CBD can affect how the THC molecule attaches to a receptor. It says, this is enough stimulation. So the THC effect is turned down. It is an antidote for consuming extremely high levels of THC and getting to that “freaking out” zone.
It seems that lower doses can be more stimulating while higher doses tend to be sedating.
CBD and THC work well together. If use just CBD alone, it will take more mg of CBD than a mixture THC and CBD at a combined lesser amount.
CBD is not sedating, it is very stimulating molecule at low and moderate doses. It is true certain cannabis plants that have CBD in them will be sedating, but it’s not because of the CBD. It is more likely due to the presence of Terpenes. Some researchers think that it is Myrcene causing the sedating, narcotic-type properties. Others think it is B-caryophylene.
What makes the ECS receptors from all other receptors is that most receptors have just one substance or impulse that will stimulate it, the usual single key and lock model, with only one key to unlock functionality to do one thing. The ECS receptors do the impossible. They allow multiple keys to open the same gate entering into multiple rooms initiating a wide array of responses. The permutation of what these receptors can initiate leads to the complexity of how they affect our bodies. Or we could say the system functions below the level of specific tasks and more in an oceanic environment where all is connected.
There are currently, I stress currently, two receptors that are known and studied. CB1 and CB2. CB stands for Cannabinoid.
CB1 is primarily found in the central nervous system, but also in a wide range of other places. The more we look the more we realize they are not limited to certain tissues, but are found all over and throughout the body. So really saying they are primarily found in the central nervous system is more an historical observation, for that is where they were first found.
CB1 is the most abundant G-protein coupled receptor in the central nervous system. There are more CB1 receptors in the brain than any other G-type. It has a major neuro-modulatatory function, A neuron is an electrically excitable cell that processes and transmits information through electrical and chemical signals. CB1’s role has been characterized as “relax, eat, sleep, forget and protect.”
CB2 has an immuno-modulatory function, which as the name refers, is about activating the immune functions. These receptors are found mainly in the peripheral nervous system, metabolic tissue and immune cells. It plays an important role in pain and inflammation.
But all of these descriptions and classifications are like looking at a flat model of a 4 dimensional landscape. We do not know enough and our descriptions fall short of a true picture.
CB2, originally thought to be mainly limited to immune cells, but now we see it is in other parts of the body. Density is high in the liver, spleen and connective tissues.
One of the really interesting things about CB2 is that tissues that don’t typically have CB2 will begin to do so after they are injured or inflamed or stressed or in some way dis-regulated. That is part of the body’s way to deal with that injury.
CB receptors are virtually absent in the brain stem cardiovascular centers. This is one of the facts that explains the lack of toxicity or overdosing when taking Cannabinoids. Because there are no receptors in the brain stem they do not suppress breathing or heart rate. Opioids do have receptors in this area and so can lead to overdose and death.
The body uses endogenous Cannabinoids, speaking through the receptors, calling our body into action at the cellular level.
A receptor is a protein molecule that receives messaging signals from outside a cell and passes it into the interior of the cell to initiate a cellular response. Cannabinoid receptors are in the family of G-protein coupled receptors.
Cannabinoid receptors function as subtle sensing devices, tiny vibrating scanners perpetually primed to pick up biochemical cues that flow through fluids surrounding each cell.
Think of the receptor as a gate sitting on the surface of the cell. It is a locked pathway from outside the cell to inside. A specific key will open it so a bio chemical message or some other stimulate can be sent to the interior of the cell. This initiates the cell into some type of action.
The concept of receptors traces itself back to the early 1900’s. The G-protein coupled receptor family represents the largest and most versatile group of cell surface receptors. Drugs active at these receptors have therapeutic actions across a wide range of human diseases.
We still do not understand everything about how they work. It was not until around the 1980 that the mechanism of how they functioned was understood. Since 1992 eight Nobel Prizes have been awarded about work with these receptors. Approximately 1/3 to 1/2 of all pharmaceutical drugs available, and two largest selling drugs world wide, all work through affecting G receptors.
The Cannabinoid receptors are in the shape of a helix. Imagine it as a corkscrew that opens outside the cell and transports messenger molecules to inside the cell. But it does not go vertically through the cell wall into the interior. Rather imagine looking at the lacing on a football. They weave in and out 6 times before opening up to the inside.
As a side, why in a helix form? And why so long a pathway for getting into the cell, the longest possible distance following the curving form of the helix? There are answers, though not in the science yet, but in the more imaginative realm of observing and listening to Nature.
When looking at a topological map of a river we always see the meandering pathway the river follows. Each unique, but always the same overall pattern. The same pattern we see when every water is flowing. What we are seeing is a two dimensional slice of a three dimensional helix form. Water always moves in this manner. It renews and enlivens itself in this sensitive chaos. Take the rhythm out, straighten the river, and it dies. Our receptors have taken the form most loved by Nature. The helix forms gives the greatest strength and allows the most encoding of information in the shortest length. Because of its circular path. This is why DNA is in this shape and the shape is continually repeated in our bodies. Following how the river flows. Following Nature’s wisdom.
Imagine the CB receptors as mountain creeks. Taking these little packets of information on the longest possible circular distance on their journey from outside the cell depositing them inside. Enlivening, charging the message with each turn of the helix and having more time to gain access to the most information.
What other “listening” part of our body is in this curved return on itself shape? The Cochlea in the ear. Though here it is more a vortex than a helix, both giving the most surface area to receive information in the least space. Both avenues of communication within the body. It only makes sense.