May 28, 2017

Brief summary of CBD (cannabidiol) effects

Endocannabinoids are naturally produced in the body. The endocannaboid system operates through the nervous system with roles in several regulatory, physiological, and metabolic processes. They are produced in response to calcium levels in the cells to help stabilize nerve transmissions. The main endocannabinoids are called anandamide (N-arachidonoylethanolamine, AEA) and 2-arachidonyl glycerol (2-AG). The endocannabinoids act as activators (“agonists”) of the cannabinoid receptors which are also naturally present in the body.

There are two types of cannabinoid receptors:
CB1R is most prominent centrally as well as in the gastrointestinal tract. It modulates several inhibitory and excitatory neurotransmitters, and its activation inhibits the anxiety response. AEA is a partial agonist and 2-AG a full agonist.
CB2R is most prominent peripherally with roles in the immune and hematopoietic systems. AEA is a weak agonist and 2-AG a full agonist. Its activation causes an inflammatory response.

Cannabidiol (CBD) is the main phytocannabinoid in Cannabis besides tetrahydrocannabinol (THC, the intoxicating cannabinoid, which mimics AEA but at higher concentrations can increase anxiety; CBD can reduce the side-effects of THC). In “hemp”, which has negligible THC, CBD is the main cannabinoid.

CBD has strong analgesic and anti-inflammatory properties. Its half-life is ~9 hours. Unlike THC, it works mostly by preventing the breakdown of the endocannabinoids AEA and 2-AG, which serves to reduce anxiety and depression, respectively. Instead of activating the endocannabinoid receptors, it binds with the proteins that carry AEA and 2-AG to the enzymes that break them down.

CBD has other actions and consequent effects as well:

  • CBD binds with CB2R as an inverse agonist (deactivator), reducing inflammatory response.
  • CBD binds with 5-hydroxytryptamine (5-HT, serotonin) 1A receptor, reducing depression.
  • CBD binds with transient receptor potential cation channel subfamily V member 1 (TrpV1, vanilloid receptor 1, capsaicin receptor) as an antagonist (blocker), reducing pain response.
  • CBD binds with peroxisome proliferator–activated receptor (PPAR) gamma, reducing inflammation.
  • CBD has direct antioxidant effects.

In addition, the terpenes in Cannabis have anti-inflammatory and analgesic properties.

Cannabidiol in Pubmed-indexed science publications