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The Basic Science of Cannabinoids

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The cannabis plant has been used for centuries to manage the symptoms of various ailments including pain. Hundreds of chemical compounds have been identified and isolated from the plant and elicit a variety of physiological responses by binding to specific receptors and interacting with numerous other proteins. In addition, the body makes its own cannabinoid-like compounds that are integrally involved in modulating normal and pathophysiological processes. As the legal cannabis landscape continues to evolve within the United States and throughout the world, it is important to understand the rich science behind the effects of the plant and the implications for providers and patients. This narrative review aims to provide an overview of the basic science of the cannabinoids by describing the discovery and function of the endocannabinoid system, pharmacology of cannabinoids, and areas for future research and therapeutic development as they relate to perioperative and chronic pain medicine.

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Cannabigerolic Acid (CBGA) inhibits the TRPM7 ion channel through its kinase domain

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In this study, we comprehensively investigated the most common major and minor cannabinoids to determine their potential efficacy on TRPM7 channel function. Here, we found that approximately half of the cannabinoids tested suppressed TRPM7 currents to some degree, with CBGA having the strongest inhibitory effect on TRPM7. We determined that the CBGA-mediated inhibition of TRPM7 requires a functional kinase domain , is sensitized by both intracellular Mg⋅ATP and free Mg2+, and reduced by increases in intracellular Ca2+. Finally, we demonstrate that CBGA inhibits native TRPM7 in B lymphocytes cell line.

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