Sodium Channels

Sodium channel blockers act on voltage-gated sodium channels, which start and propagate action potentials. Voltage-gated sodium (NaV) channels open within milliseconds of depolarization and let sodium ions enter nerve and muscle cells. The first channel sequence, from the electric eel, was deduced from complementary DNA in 1984. A crystal structure of the sodium channel from Arcobacter butzleri (NavAb), reported in 2011, showed its pore and voltage-sensing modules at atomic resolution. Local anesthetics such as lidocaine and bupivacaine HCl block the channel pore in nerve conduction studies. Carbamazepine and disopyramide are used to study neuronal and cardiac excitability. The set also includes amiloride HCl, a blocker of the epithelial sodium channel (ENaC), and digoxin, an inhibitor of the sodium-potassium pump.

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