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Understanding Cannabinoid Receptors: Why Cannabis Affects Humans 28 Jul

By Gooey Rabinski | November 19, 2015

Many cannabis consumers are familiar with popular cannabinoids like THC and CBD, the therapeutic chemical compounds that provide a wealth of medicinal relief for dozens of conditions involving pain, inflammation, and nausea. Cannabinoids, as well as their cousins terpenes, are simply the chemicals that provide actual relief to patients by inserting themselves into special receptors in the tissues and cells of the human body. They are among more than 480 natural components found within the cannabis plant.

These special receptors are part of what is known as the endocannabinoid system. This mechanism, which helps modulate many bodily functions — including appetitesleepanxiety level, and cognition — is intimately tied to the nervous system and immune system. In fact, particular cannabinoids target specific types of receptors located on the surface of cells in different areas of the body.

This targeting is formally called a binding affinity. Some molecules may feature a relatively low binding affinity that offers poor or moderate efficacy for a patient, while other pairings feature a very strong affinity that, when combined with cannabinoids from high-quality plants, can result in superb medical benefit or psychoactive effects.

Endocannabinoid System / Receptors

Readers have already learned that molecules like cannabinoids and terpenes fit into special receptors within the endocannabinoid system, or ECS. A researcher or doctor would say that molecules like THC activate particular cannabinoid receptors. These receptors, called CB1 and CB2, work like a lock and key when flooded with cannabinoids, such as after a patient smokes, vaporizes, or ingests cannabis flowers, a concentrate, or an edible.

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The endocannabinoid system produces its own cannabinoids. This is the reason it exists, actually. Technically, this system is simply being supplemented when a person consumes cannabinoids, terpenes, or other chemicals from an herb like a cannabis plant that happen to bind with the receptors within this system. In 1992, it was discovered that the ECS produces an endocannabinoid within the brain called anandamide. This internal cannabinoid, which was discovered by Dr. Raphael Mechoulam at Hebrew University in Jerusalem, binds to CB1 receptors in the brain and nervous system and, to a lesser extent, CB2 receptors in the immune system. More about this powerful molecule later.

Many medical professionals and researchers have identified a shortage of endocannabinoids as a condition called endocannabinoid deficiency. It is theorized that a deficiency of these molecules — which are increasingly understood to be critical to good health and homeostasis (balance) within humans — may lead to a variety of diseases related to the immune and nervous systems. These conditions often involve inflammation, pain, and nausea, the side effects of diseases, pharmaceutical drugs, and treatments like chemotherapy.

Cannabinoid Receptors: CB1 and CB2

The CB1 receptor was discovered in 1990, while CB2 was uncovered shortly thereafter in 1993 by a research group at Cambridge University. One source claims that these two receptor types employ significantly different signaling mechanisms. It is known that they are expressed in vastly different ways, including their appearance in various parts of the body (different regions of the endocannabinoid system).

The cannabinoid THC has been shown to possess a very high binding affinity with CB1 receptors located throughout the brain, central nervous system, connective tissues, gonads, glands, and related organs. This is one reason that consumption of cannabis strains and plants containing a high amount of THC result in a relatively potent effect, giving patients significant relief from pain, nausea, or depression while delivering a strong euphoria to lifestyle users. Significant efficacy is gained by those undergoing chemotherapy and patients suffering conditions involving inflammation, like arthritis and lupus.

CB2 receptors, on the contrary, are located throughout the immune system and related organs, like the tissues of the spleen, tonsils, and thymus gland. They are also common in the brain, although they do not appear as densely as CB1 sites and are found on different types of cells.

CB2 sites are also found in greater concentrations (density) throughout the gastrointestinal system, where they modulate intestinal inflammatory response. This is why sufferers of Crohn’s disease and IBS gain such great relief from cannabis medicine. It is also a powerful example of how the endocannabinoid system, when supplemented by external cannabinoids (such as from cannabis), can provide such powerful and long-lasting relief for patients of diseases like Crohn’s. Cannabis has been shown to have such great efficacy for this condition that, in nearly half of cases, the kind herb puts the disease into full remission.

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Beyond binding affinity, the locations, density, and overall number of cannabinoid receptors are collectively labeled their expression. Researchers discuss how different patients, especially those with particular diseases, may have different expressions of CB1 and CB2 receptors than patients who are not afflicted with these conditions (one example is patients suffering from anorexia).

The expression of cannabinoid receptors in a person is akin to a fingerprint or hairline: It is a highly subjective characteristic of that individual resulting in a range of responses to different cannabis medicines. Some patients prefer a sativa like Durban Poison or Kali Mist, while others gravitate toward an indica such as Kosher Kush or Blue Cheese or lock in on a hybrid like Blue Dream or Sour Diesel.

Receptor Expression

One patient may overexpress a receptor like CB1 (meaning they have more receptors than average) and, as a result, be very sensitive to a cannab

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