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α-Adrenoreceptor blocker phentolamine inhibits voltage-gated sodium channels via the local anaesthetic binding site.
Authors
Toklucu I, Sudha Bhagavath Eswaran V, Bott RA, Kesdoğan AB, Gaebler AJ, Stingl J, Hausmann R, Körner J, Lampert AAbstract
Phentolamine is a non-selective α-adrenoreceptor antagonist used to reverse local anaesthesia, for example, during dental procedures when a vasoconstrictor is co-applied. Phentolamine-mediated vasodilation leads to faster clearance of injected drugs. Previous electrophysiological studies hypothesized that phentolamine acts as a modulator of voltage-gated sodium channels, which could conflict with its indication as local anaesthetic reversal agent.