Eugenol and lidocaine inhibit voltage-gated Na⁺ channels from dorsal root ganglion neurons with different mechanisms.

ABSTRACT: Eugenol (EUG) is a bioactive monoterpenoid used as an analgesic, preservative, and flavoring agent. Our new data show EUG as a voltage-gated Na⁺ channel (VGSC) inhibitor, comparable but not identical to lidocaine (LID). EUG inhibits both total and only TTX-R voltage-activated Na⁺ currents (I_Na) recorded from VGSCs naturally expressed on dorsal root ganglion sensory neurons in rats. Inhibition is quick, fully reversible, and dose-dependent. Our biophysical and pharmacological analyses showed that EUG and LID inhibit VGSCs with different mechanisms. EUG inhibits VGSCs with a dose-response relationship characterized by a Hill coefficient of 2, while this parameter for the inhibition by LID is 1. Furthermore, in a different way from LID, EUG modified the voltag

SUBMITTER: Moreira-Junior L 

PROVIDER: S-EPMC11234063 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature