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Voltage-gated sodium channels (VGSCs), also known as Nav channels, are large transmembrane proteins essential for the initiation and propagation of action potentials in excitable cells such as neurons, muscle cells, and cardiac tissue. Local anesthetics exert their primary effect by blocking VGSCs, preventing sodium influx during depolarization, inhibiting action potential generation and thus nerve conduction.
Blockade/modulation via inner pore binding, preferentially when channels are open or inactivated ("use-dependent block")
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