Background:

Moricizine is an antiarrhythmia agent used primarily for ventricular rhythm disturbances.Target: Sodium ChannelMoricizine is an antiarrhythmia agent used primarily for ventricular rhythm disturbances. Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes. Moricizine induced the tonic block of INa with the apparent dissociation constant (Kd,app) of 6.3 microM at -100 mV and 99.3 microM at -140 mV. Moricizine at 30 microM shifted the h infinity curve to the hyperpolarizing direction by 8.6 +/- 2.4 mV. Moricizine also produced the phasic block of INa, which was enhanced with the increase in the duration of train pulses, and was more prominent with a holding potential (HP) of -100 mV than with an HP of -140 mV. Moricizine would exert an antiarrhythmic action on atrial myocytes, as well as on ventricular myocytes, by blocking Na+ channels with a high affinity to the inactivated state and a slow dissociation kinetics [1].

[1]. Ahmmed, G.U., et al., Analysis of moricizine block of sodium current in isolated guinea-pig atrial myocytes. Atrioventricular difference of moricizine block. Vascul Pharmacol, 2002. 38(3): p. 131-41.