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