Deep Dive: Cannabidiol Skin Receptor Science

Deep Dive:
Cannabidiol Skin Receptor Science

Endocannabinoid System

The Endocannabinoid System has been recently recognized as an important modulatory system in the function of brain, endocrine, and immune tissues. It appears to play a very important regulatory role in the secretion of hormones related to reproductive functions and response to stress.

Cannabinoid Receptors located throughout the body are part of the endocannabinoid system, which is involved in a variety of physiological processes including appetite, pain-sensation, mood, and memory. Cannabinoid receptors are of a class of cell membrane receptors in the G protein-coupled receptor superfamily.

Therapeutic Potential of Cannabidiol (CBD)

Cannabinoids are recognized as a valuable option in the treatment of inflammation, pain or other conditions with positive efficacy and safety profiles.

Many published studies support the use of medical cannabis as an adjunct to the treatment of inflammation and chronic pain.

In particular, the cannabinoid, CBD has been heavily investigated for it’s therapeutic potential

How Does Cannabidiol (CBD) Work?

Endocannabinoids Within the Skin

Trends in Pharmacological Sciences points out that the endocannabinoid system found within the skin plays a large physiological role in the health of skin cells.

TRPV1 Receptor (+): Significantly decreased pro-inflammatory cytokines IL-2, TNF-a, IFN-c, IL-6, IL-12 (p-40), IL-17, MCP-1 and eotaxin-1 (CCL11)
CB2 Receptor (-): Reductions in IL-6 concentration, and TNF-a, COX-2, and iNOS expression
Adenosine A2A receptor (+): Decreases TNF-a production and IL-6 and chemokines (MCP-1 and MIP-2)
GPR55 Receptor (-): resulting in increased IL-12 and TNF-a production, and increased endocytic activity in LPS-activated monocytes.
Arachidonic acid release (+): Significant stimulation of arachidonic acid release
Cyclooxygenase and products: inhibit both COX-1 and COX-2 activity
TRPV3 Receptor (+): Effects on intracellular Ca++ levels and mast cells

S. Burstein / Bioorg. Med. Chem. 23 (2015) 1377–1385

Safety and Side Effects of Cannabidiol

Often described favorable safety profile of CBD in humans was confirmed and extended by the reviewed research
Chronic use and high doses up to 1,500 mg/day of CBD are reportedly well tolerated in humans
CBD does not affect physiological parameters (heart rate, blood pressure and body temperature), does not affect gastrointestinal transit
CBD is non-toxic and does not alter psychomotor or psychological functions
In comparison with other drugs used for the treatment of these medical conditions, CBD has a better side effect profile
The most commonly reported side effects were tiredness, diarrhea, and changes of appetite/weight

(1) Bergamaschi et al. Current Drug Safety, 2011, 6
(2) Iffland and Grotenherman, 2017 Cannabis and Cannabinoid Research 2:1, 139–154