Abstract
Cannabidiol (CBD), a major non-psychotropic cannabinoid found in the Cannabis plant, has been shown to exert anti-nociceptive, anti-psychotic, and anti-convulsant effects and to also influence the cardiovascular system. In this study, the effects of CBD on major ion currents were investigated using the patch-clamp technique in rabbit ventricular myocytes. CBD inhibited voltage-gated Na+ and Ca2+ channels with IC50 values of 5.4 and 4.8 µM, respectively. In addition, CBD, at lower concentrations, suppressed ion currents mediated by rapidly and slowly activated delayed rectifier K+ channels with IC50 of 2.4 and 2.1 µM, respectively. CBD, up to 10 μM, did not have any significant effect on inward rectifier I K1 and transient outward I to currents. The effects of CBD on these currents developed gradually, reaching steady-state levels within 5–8 min, and recoveries were usually slow and partial. Hill coefficients higher than unity in concentration-inhibition curves suggested multiple CBD binding sites on these channels. These findings indicate that CBD affects cardiac electrophysiology by acting on a diverse range of ion channels and suggest that caution should be exercised when CBD is administered to carriers of cardiac channelopathies or to individuals using drugs known to affect the rhythm or the contractility of the heart.
Highlights
Cannabis cultivars have been used since ancient times for recreational and medicinal purposes
Ventricular myocytes were prepared by slight modification of the method described earlier (Al Kury et al, 2014a; Ali et al, 2015)
The main finding of this study is that CBD appears to be effective in suppressing the delayed rectifier currents IKr and IKs
Summary
Cannabis cultivars have been used since ancient times for recreational and medicinal purposes. Cannabis plant extracts contain over 100 structurally related, highly lipophilic terpenoid derivatives, collectively designated as phytocannabinoids (Pertwee et al, 2010). Among these phytocannabinoids, cannabidiol (CBD) is of great pharmacological interest because of its lack of potency on cannabinoid type 1 and type 2 receptors that are thought to mediate the psychotropic activity of the cannabis plant, an effect mainly mediated by (-)-trans-Δ9-Tetrahydrocannabinol (Mechoulam and Hanus, 2002; Pertwee et al, 2010). Cannabidiol has been shown to exert antinociceptive, anti-psychotic, and anti-convulsant effects (Hill et al, 2012; Vitale et al, 2021). The specific molecular and cellular mechanisms underlying the effects of CBD remain largely unknown
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