cannabinoids

Cannabinoids and Receptors

cannabinoids

In 1963, Raphael Mechoulam, determined the structure of cannabidiol (CBD), and isolated the psychoactive ingredient delta-9 tetrahydrocannabinol (THC).

Over the ensuing decades, Mechoulam and his team continued to isolate numerous compounds from Cannabis and identified the known endogenous cannabinoid, a chemical actually made by the brain itself; they named it “anandamide.” In the Sanskrit language, ananda means “supreme bliss”.

There are more than 480 natural components found within the Cannabis plant, of which 66 have been classified as “cannabinoids.” Cannabinoids are groups of chemical compounds that affect body and mind through their interaction with special receptors.

Perhaps the most beneficial medical discovery are all the different effects of cannabinoids. There are many including: Cannabigerols (CBG); Cannabichromenes (CBC); other Cannabidiols (CBD); other Tetrahydrocannabinols (THC); Cannabinol (CBN) and cannabinodiol (CBDL); other cannabinoids (such as cannabicyclol (CBL), cannabielsoin (CBE), cannabitriol (CBT) and other miscellaneous types).

These components exert some therapeutic effect, more than any single compound alone. Cannabinoids are more effective together than in isolation: That is the “entourage effect.”Unlike other drugs that may work well as single compounds, synthesized in a lab, Cannabis offers its most profound benefit in its complete form.

Cannabinoids

A brief description of the medical uses for the six primary cannabinoids.

 

cannabinoids

  • CBN is somewhat psychoactive at roughly 10% the activity of THC and is a breakdown product that occurs when THC is exposed to light or heat. CBN causes drowsiness and reduces spasms.
  • CBG, which is more commonly found in the non-psychoactive plant varieties, has shown significant ability to counteract and prevent tumour formation.
  • CBD is not psychoactive; studies have shown it to have anti-inflammatory, anti-anxiety, anti-nausea, neuroprotective, blood pressure lowering and pain killing properties, among many others.
  • THC, the most well-known cannabinoid and most psychoactive, THC has the ability to alter behaviour, mood perception, and consciousness. THC is responsible for euphoric feeling some people consider as being “high”.
  • THCV is a psychoactive cannabinoid that may help treat diabetes and is being investigated as an anti-obesity drug.
  • CBC has analgesic, anti-inflammatory, and very promising antibiotic properties.

Receptors

CB1 is the most abundant receptor in the mammalian brain, but is also found throughout the body in much lower concentrations. Its activation is responsible for the psychoactive effect of tetrahydrocannabinol (THC), one of the main compounds in cannabis.

Distribution of CB1 is not uniform; the highest concentrations are in the basal ganglia, hippocampus, cerebral cortex, cerebellum, and amygdaloid nucleus. There are virtually no cannabinoid receptors in the brainstem, which controls breathing. This layout explains why THC (cannabis-derived or synthetic) and other CB1 agonists affect memory, emotion, cognition, motor function, and pain.

Also, the lack of receptors in the brainstem accounts for why overdosing on cannabis cannot cause death.

CB2 receptors are distributed primarily throughout the immune and hematopoietic systems, meaning the receptors are found on white blood cells and tissues in the spleen, lymph nodes, bone marrow, and tonsils. In lesser quantities, they are found in the brain, pancreas, and liver.

Activation of CB2 receptors can be immensely therapeutic, but unlike CB1, its stimulation does not cause psychoactivity. One of the chief effects of CB2 activation is a reduction in inflammation.

The Endocannabinoid System (ECS)

Named after the plant that led to its discovery, the ECS is perhaps the most important physiologic system involved in establishing and maintaining human health.

Endocannabinoids and their receptors are found throughout the body: in the brain, organs, connective tissues, glands, and immune cells. In each tissue, the cannabinoid system performs different tasks, but the goal is always the same: homeostasis, the maintenance of a stable internal environment despite fluctuations in the external environment.

Cannabinoids promote homeostasis at every level of biological life, from the sub-cellular, to the organism, and perhaps to the community and beyond.

Here’s one example: autophagy, a process in which a cell sequesters part of its contents to be self-digested and recycled, is mediated by the cannabinoid system.

While this process keeps normal cells alive, allowing them to maintain a balance between the synthesis, degradation, and subsequent recycling of cellular products, it has a deadly effect on malignant tumor cells, causing them to consume themselves in a programmed cellular suicide or apoptosis.

The death of cancer cells, of course, promotes homeostasis and survival at the level of the entire organism.

Endocannabinoids and cannabinoids are also found at the intersection of the body’s various systems, allowing communication and coordination between different cell types. At the site of an injury, for example, cannabinoids can be found decreasing the release of activators and sensitisers from the injured tissue, stabilising the nerve cell to prevent excessive firing, and calming nearby immune cells to prevent release of pro-inflammatory substances.

Three different mechanisms of action on three different cell types for a single purpose: minimise the pain and damage caused by the injury.

The endocannabinoid system, with its complex actions in our immune system, nervous system, and all of the body’s organs, is literally a bridge between body and mind. By understanding this system we begin to see a mechanism that explains how states of consciousness can promote health or disease.

In addition to regulating our internal and cellular homeostasis, cannabinoids influence a person’s relationship with the external environment.

Socially, the administration of cannabinoids clearly alters human behaviour, often promoting sharing, humour, and creativity. By mediating neurogenesis, neuronal plasticity, and learning, cannabinoids may directly influence a person’s open-mindedness and ability to move beyond limiting patterns of thought and behaviour from past situations.

Reformatting these old patterns is an essential part of health in our quickly changing environment.

 

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