IndraLab

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Amide inhibits KCNK18. 1 / 1
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"In heterologous systems and sensory neurons, pyrethroids significantly inhibited K 2P currents, similar to hydroxy-α-sanshool, a compound extracted from Szechuan peppercorns, which inhibits TRESK, TASK-1, and TASK-3 and activates sensory neurons. xref Sanshool also inhibits Na v 1.3, Na v 1.7, and Na v 1.8, xref and the subsequent blocking effect on action potential firing is thought to mediate its analgesic effects by silencing Aδ-nociceptors. xref The synthetic alkylamide isobutylalkenyl amide, a sanshool derivative, also inhibits TRESK, activates sensory neurons, and produces tingling, numbing, and burning sensations in humans and painful behaviors in rodents. xref , xref , xref Another alkylamide insecticide, BTG502, structurally related to sanshool, inhibits Na v channels by binding to a site that overlaps with the pyrethroid-binding site. xref These different compounds exhibit characteristic somatosensory effects via their actions on both Na + and K + channels expressed in sensory neurons and resulting sensations might depend on the particular neuronal subtypes affected."