Understanding Endocannabinoid Receptors

Welcome back to our ongoing series on the introduction to the Endocannabinoid System. In our previous segment, we provided a basic introduction to the ECS (endocannabinoid system) functions. In this segment we will be discussing the different receptors of the ECS, including their locations, functions, and signalling that make the therapeutic potential of cannabinoids a possibility.

CANNABINOID RECEPTORS

As mentioned in our previous segment the first cannabinoid receptor, aptly named the CB1 receptor, was first discovered in the late 1980s. Since then, researchers have learned a great deal about cannabinoid receptors, with the two most discussed and most abundantly found in the human body being the CB1 and CB2 receptors. These cannabinoid receptors fall under a classification of cell membrane receptors known as G protein coupled receptors and are responsible for the effects of cannabinoids, including CBD (cannabidiol) effects.

Cannabinoid receptor activation occurs following the introduction of ligands from one or more of three groups.

• Endocannabinoids – Cannabinoids produced and released within the body.
• Phytocannabinoids – Plant based cannabinoids such as those found in cannabis.
• Synthetic cannabinoids – Manufactured pharmaceutical synthetic THC and CBD.

Receptor Signalling

What makes the process of cannabinoid receptor signalling unique is that it is presynaptic. This means that unlike in the case of neurotransmitters that travel from a neuron to a postsynaptic cell, cannabinoids attach to cannabinoid receptors located on the presynaptic neuron and effect ECS (endocannabinoid system) functions. Due to this presynaptic process, the therapeutic potential of cannabinoids can lead to a direct effect on neurotransmission.

LOCATIONS & FUNCTIONS

In a slight over-simplification, cannabinoids and cannabinoid receptors work similar to a lock and a key in that certain cannabinoids will ‘fit’ or bind with their matching receptors, creating CBD (cannabidiol) effects as well as other cannabinoids’ effects. The body’s ECS consists of a vast network of these cannabinoid receptors or ‘locks’. In fact, the CB1 receptor is one of the most abundant receptors found in the brain and in the central nervous system and plays a key role in ECS (endocannabinoid system) functions.

Cannabinoid receptors can be found throughout the body, and are primarily concentrated in the brain, spinal cord, and the tissues of the immune system to help activate the therapeutic potention of cannabinoids.

Much is still to be explored to fully understand ECS (endocannabinoid system) functions and its network of receptors. While there is still ongoing investigation and debate, research has shown that activation of the CB1 and CB2 receptors can influence many of the different systems and functions of the body. The popularity of CBD (cannabidiol) effects is on the rise for this reason. 

SECONDARY CANNABINOID RECEPTORS

While research is limited on receptors of the ECS other than the CB1 and CB2 receptors, other receptors do exist that might contribute in the therapeutic potential of cannabinoids, with the two most notable being:

• Transient Receptor Potential Channels (TRPV-1) – Membrane proteins involved in the modulation of ion entry.
• Peroxisome Proliferator Activated Receptors (PPARS) – A group of nuclear hormone receptors.

UP NEXT – In the next segment of our series covering the Endocannabinoid System, we will be discussing the endocannabinoids Anandamide (AEA) and 2-Arachidonoylglycerol (2-AG).

To begin your cannabis medicine journey today, book an appointment now with the Savikalpa Virtual Clinic for an online doctor consultation, or request more information from a member of our highly trained clinic staff (eclinic@savikalpa.com).

We pride ourselves on being one of India’s most qualified sources of fast, friendly, and professional access to cannabinoid medicine online!

Interested in learning more? Send us your questions (eclinic@savikalpa.com). It is our mission to educate patients in any way we can, and we would be delighted to hear from you.

Research regarding the endocannabinoid system:

• Clinical Endocannabinoid Deficiency Reconsidered: Current Research Supports the Theory in Migraine, Fibromyalgia, Irritable Bowel, and Other Treatment-Resistant Syndromes https://www.liebertpub.com/doi/full/10.1089/can.2016.0009
• CB1 and CB2 Receptor Pharmacology https://www.sciencedirect.com/science/article/abs/pii/S1054358917300340?via%3Dihub
• Neurobiological Interactions Between Stress and the Endocannabinoid System https://pubmed.ncbi.nlm.nih.gov/26068727/
• The endocannabinoid system in guarding against fear, anxiety and stress https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5871913/
• Endocannabinoid system and stress and anxiety responses https://www.sciencedirect.com/science/article/abs/pii/S0091305705001346
• Endocannabinoid system and pain: an introduction https://pubmed.ncbi.nlm.nih.gov/24148358/
• The endocannabinoid system in pain and inflammation: Its relevance to rheumatic disease https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5685274/
• Endocannabinoid system in irritable bowel syndrome and cannabis as a therapy https://www.sciencedirect.com/science/article/abs/pii/S0965229919310179
• CB2 receptors in reproduction https://bpspubs.onlinelibrary.wiley.com/doi/full/10.1038/sj.bjp.0707444
• Endocannabinoids in the regulation of appetite and body weight https://journals.lww.com/behaviouralpharm/Abstract/2005/09000/Endocannabinoids_in_the_regulation_of_appetite_and.4.aspx
• The endocannabinoid system: directing eating behavior and macronutrient metabolism https://www.frontiersin.org/articles/10.3389/fpsyg.2014.01506/full
• Endocannabinoids and immune regulation https://www.sciencedirect.com/science/article/abs/pii/S104366180900108X?via%3Dihub
• Endocannabinoid Catabolic Enzymes Play Differential Roles in Thermal Homeostasis in Response to Environmental or Immune Challenge https://link.springer.com/article/10.1007%2Fs11481-015-9593-1
• Antidepressants and Changes in Concentration of Endocannabinoids and N-Acylethanolamines in Rat Brain Structures https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4067538/
• Cannabinoid Receptors and the Endocannabinoid System: Signaling and Function in the Central Nervous System https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5877694/
• Cannabinoid Receptors in the Central Nervous System: Their Signaling and Roles in Disease https://www.frontiersin.org/articles/10.3389/fncel.2016.00294/full
• Endocannabinoid Binding to the Cannabinoid Receptors: What Is Known and What Remains Unknown https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4120766/
• Cannabinoid CB1 and CB2 Receptor Signaling and Bias https://www.liebertpub.com/doi/10.1089/can.2016.0037

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