Nerispirdine is a acetylcholine release enhancer, sodium channel blocker and K(V) 2.1 channel blocker. Nerispirdine inhibits voltage-dependent Na(+) channel currents recorded from human SH-SY5Y cells with an IC(50) of 11.9 micromol/L when measured from a -70 mV holding potential. Nerispirdine also inhibits K(v)1.1 and K(v)1.2 with IC(50) values of 3.6 and 3.7 micromol/L, respectively.