The psychoactive cannabinoid THC inhibits peripheral nociceptors by targeting Na(V)1.7 and Na(V)1.8 nociceptive sodium channels

精神活性成分大麻素THC通过靶向Na(V)1.7和Na(V)1.8伤害性钠通道来抑制外周伤害感受器。

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Abstract

Δ⁹-Tetrahydrocannabinol (THC), the primary psychoactive compound in cannabis, is widely recognized for its central effects mediated by cannabinoid receptors. Here, we uncover a distinct peripheral mechanism by which THC inhibits the excitability of nociceptive neurons. We show that THC directly targets the nociceptive voltage-gated sodium channels Na(V)1.7 and Na(V)1.8 through the conserved local anesthetic binding site. This interaction reduces sodium currents and suppresses action potential generation in peripheral sensory neurons. Our findings demonstrate that, beyond its central psychoactivity, THC exerts direct peripheral nociceptor inhibition via modulation of Na(V)1.7 and Na(V)1.8, offering new insight into cannabinoid-based analgesia independent of cannabinoid receptor signaling.

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