Azimilide (dihydrochloride)

Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of I_Ks (IC₅₀ = 2.6 μM (2mM [K⁺]ₑ)) and I_Kr (IC₅₀ = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC₅₀s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (I_Ca) (IC₅₀ = 17.8 μM) and sodium current (I_Na) (IC₅₀ = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation^[1][2][3][4]. In Vitro:Azimilide dihydrochloride (0.1-100 μM) blocks I_Kr (reversibly dependent, affected by [K⁺]ₑ) and I_Ks channels (dependently on use, unaffected by [K⁺]ₑ) in mouse AT-1 cells and African clawed frog oocytes^[1].
Azimilide dihydrochloride (0.3-5 μM) shortens the action potential duration (APD) of canine and guinea pig ventricular muscle cells^[2][3].
In Vivo:Azimilide dihydrochloride (10 mg/kg, i.v., single dose) significantly reduces the occurrence of ventricular tachycardia (VT) induced by electrical stimulation (PES) in dogs^[4].