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Source (EN)
Target (AR)
Lozenges for the treatment of sore throat provide relief of discomfort in
cases of oral inflammation.
This effect has not been fully explained so far. Here, we have examined the
proposition that key components of pharmaceutical preparations for the
treatment of sore throat which are routinely regarded antiseptics might have
sodium channel- blocking, i.e. local anaesthetic-like effects.
We investigated the effects of hexylresorcinol, amylmetacresol and
dichloro- benzylalcoholonvoltage-operatedneuronal(NaV1.2) sodium
channels heterologously expressed in HEK 293 cells in vitro.
Hexylresorcinol, amylmetacresol and dichloro-benzylalcohol reversibly
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blocked depolarisation-induced whole-cell sodium inward currents. The
half-maximum blocking concentrations (EC50) at−150 mV were 23.1, 53.6
and 661.6 µM, respectively.
Block induced by hexylresorcinol and amylme- tacresol was increased at
depolarised potentials and use-dependent during trains of depolarisations
applied at high frequency (100 Hz) indicating that both drugs bind more
tightly to inactivated conformations of the channel. Estimates for the
inactivated state affinity were 1.88 and 35 µM for hexylresorcinol and
amylmetacresol, respectively.
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