BUY Pilsicainide hydrochloride

Pilsicainide hydrochloride. A Use Dependent Anti-Arrhythmic Na_v Channel Blocker.

Voltage-gated sodium channels (VGSC, Na_v) are critically important for electrogenesis and nerve impulse conduction. Certain sodium channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Na_v in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation.
Pilsicainide is a class IC anti-arrhythmic drug widely used in the treatment of supraventricular and ventricular tachyarrhythmias in Japan.
Results from voltage clamp experiments show that Pilsicainide is a pure sodium channel blocker with little or no effect on other cardiac channels, probably with the exception of HERG channels.

Measurements of Pilsicainide�s ability to block hNa_v1.4 channels resulted in half-maximum inhibitory concentrations (IC₅₀) of 189 � 10 μM at 0.1 Hz, and 76 � 7 μM at 10 Hz. Effects of Pilsicainide were similar on skeletal muscle hNa_v1.4, brain hNa_v1.1 and heart hNa_v1.5 channels.

Ion Channel Modulators; Voltage-Gated Na⁺ Channel Blockers