What is a Cannabinoid Receptor and Why Should You Care?

By Rachel Wellendorf

Ever wonder how inhaling the smoke of a plant gets you high? It involves many complex signaling systems acting together at the cellular level.

The endocannabinoid system (ECS) is found in all mammals and it is why you are able to feel that stoney euphoria. As of current research, there are only two known cannabinoid receptors: CB1 and CB2. CB2 receptors show up in immune cells, while CB1 receptors are present in the brain. In fact, the CB1 receptors are the most common receptors of its class found in the brain. iAnd you don’t have to get down with dabs to utilize these receptors. Mammalian bodies (yes, your dog too) produce chemicals called endocannabinoids. Endocannabinoid is a fancy word for cannabinoids that naturally occur in the body and they can be compared to neurotransmitters like serotonin and melatonin.

All cannabinoids are not created equally with respect to these receptors, however. According to Project CBD, there are different binding sites on the CB1 receptor for different cannabinoids. Meaning multiple cannabinoids can bind to 1 protein.

So how does this system actually work? After ingesting cannabis, an array of cannabinoids diffuse into your blood and eventually cross the blood-brain barrier, entering the tissues of the brain and spinal cord. From there, cannabinoids bind to cannabinoid receptors based on shape and size, similar to how two puzzle pieces would fit together. Once the cannabinoid is locked into the receptor, a stepwise release of chemicals occurs.

To the average pot smoker, you start feeling the effects physiologically within 30 minutes after consumption. In the meantime, your brain activity levels are spiking with the down-regulation and up-regulation of many different compounds.

Many patients have seen that CBD can mediate the psychotropic effects of THC. Though the mechanism is still being studied, Project CBD reports that CBD acts as an anti-depressant and is anxiety-reducing.

Another study found that CB1 receptors have been found in adipocytes (fat cells), which could lead to promise in using cannabis and endocannabinoids to treat obesity. Researchers published in the journal of Experimental Brain Research found that THC could provide Neuroprotection following brain damage in mice. An ultra low dose of THC was used in the study and was shown to have long-lasting effects including increased brain plasticity.

Although legalization and eye opening research are on the rise, there is still negative stigma regarding the plant. However, this isn’t all bad news. Pharmaceutical companies can create drugs that mimic endocannabinoids as opposed to creating drugs that are synthetic to our biology. Researches at the University of Aberdeen in Scotland have created a drug that acts similar to a cannabinoid.  The drug, named ZCZ011, binds to CB1 receptors and allows more of the endocannabinoid anadamine to bind to receptors, thus reducing pain and inflammation. Drugs like this can reshape industry standards in pharmacology so that there are no longer addictive medications with a long list of negative side effects on the market.

 

Sources and more information:

Butterfield, Delilah. "THC: Everything You Need To Know About Delta9-Tetrahydrocannabinol." HERB. Herb, 24 July 2016. Web. 09 Jan. 2017.

Dr. Raphael Mechoulam on the Endocannabinoid System. Perf. Raphael Mechoulam. YouTube, 20 July 2015. Web. 9 Jan. 2017.

Ledent, Catherine, Olga Valverde, Gregorio Cossu, Francois Petitet, Jean-Francois Aubert, Francoise Beslot, Georg A. Bohme, Assunta Imperato, Thierry Pedrazzini, Bernard P. Roques, Gilbert Vassart, Walter Fratta, and Marc Parmentier. "Unresponsiveness to Cannabinoids and Reduced Addictive Effects of Opiates in CB1 Receptor Knockout Mice." Science 283.5400 (1999): 401-04. Web. 9 Jan. 2017.

Lee, M.A., 2012. The discovery of the Endocannabinoid System. O’Shaughnessy's Online, p.1-2

Marcu, Jahan, Ali S. Matthews, and Martin A. Lee. "Is CBD Really Non-Psychoactive?" Is CBD Really Non-Psychoactive? Project CBD, 17 May 2016. Web. 09 Jan. 2017.

Pagotto, Uberto, Giovanni Marsicano, Daniela Cota, Beat Lutz, and Renato Pasquali. "The Emerging Role of the Endocannabinoid System in Endocrine Regulation and Energy Balance." Endocrine Reviews 27.1 (2011): n. pag. Web. 9 Jan. 2017.

Thomas, Nadulski, Fritz Pragst, Gordon Weinberg, Patrik Roser, Martin Schnelle, Eva-Maria Fronk, and Andreas Michael Stadelmann. "Randomized, Double-Blind, Placebo-Controlled Study About the Effects of Cannabidiol (CBD) on the Pharmacokinetics of ∆9-Tetrahydrocannabinol (THC) After Oral Application of THC Verses Standardized Cannabis Extract." Therapeutic Drug Monitoring 27.6 (2005): 799-810. Web. 9 Jan. 2017.

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