2002
DOI: 10.1017/s0265021502000923
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Voltage-dependent block of neuronal and skeletal muscle sodium channels by thymol and menthol

Abstract: The results suggest that antinociceptive and local anaesthetic effects of thymol and menthol might be mediated via blockade of voltage-operated sodium channels with the phenol derivative thymol being as potent as the local anaesthetic lidocaine.

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Cited by 126 publications
(87 citation statements)
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“…It is now generally believed that activation of TRPM8 in cold-sensitive neurons of trigeminal and dorsal root ganglia underlies the cooling effect of the menthol (3,4), although characterization of a TRPM8-deficient mouse would be needed to fully prove this point. Moreover, menthol has been shown to inhibit voltage-dependent Na ϩ and Ca 2ϩ channels, which may contribute to the antinociceptive and local anesthetic effects of menthol (21). Interestingly, the sensory impact of menthol on mucosa or skin is clearly biphasic: whereas low doses evoke a cooling sensation, higher concentrations of menthol lead to irritation and even induce a burning feeling (1).…”
Section: Discussionmentioning
confidence: 99%
“…It is now generally believed that activation of TRPM8 in cold-sensitive neurons of trigeminal and dorsal root ganglia underlies the cooling effect of the menthol (3,4), although characterization of a TRPM8-deficient mouse would be needed to fully prove this point. Moreover, menthol has been shown to inhibit voltage-dependent Na ϩ and Ca 2ϩ channels, which may contribute to the antinociceptive and local anesthetic effects of menthol (21). Interestingly, the sensory impact of menthol on mucosa or skin is clearly biphasic: whereas low doses evoke a cooling sensation, higher concentrations of menthol lead to irritation and even induce a burning feeling (1).…”
Section: Discussionmentioning
confidence: 99%
“…The interpretation of these studies is further complicated by the findings that menthol is not selective for TRPM8. In fact, menthol was shown to inhibit voltage-gated Na + (Haeseler et al, 2002) and Ca 2+ channels (Swandulla et al, 1987), which could reduce nociceptive transmission. This may explain the observation that responses to menthol were markedly reduced, but not abolished, in TRPM8-null mice (Colburn et al, 2007).…”
Section: Transient Receptor Potential Channels: Acquired Diseasesmentioning
confidence: 99%
“…Menthol is known to cause local anaesthetic effects in neuronal and skeletal muscles via blocking voltage-operated sodium channels (Haeseler et al, 2002). This cellular response has led to its use as a marine anaesthetic (Alexander, 1964;Lauretta et al, 2014).…”
Section: Introductionmentioning
confidence: 99%