Pilsicainide (SUN 1165 free acid) 是一种有效的钠通道 (Sodium Channel) 阻滞剂和有效的 Ic 类抗心律失常剂。
产品描述
Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent [1] [2].
体外活性
Pilsicainide (SUN 1165 free acid; 10-200 μg/mL) decreases peak amplitude of the net inward current in a dose-dependent manner with an IC 50 of 29.2 μg/mL in levo-thyroxine (T 4 )-treated rat atrial cells [1].
体内活性
Pilsicainide (SUN 1165 free acid; 2 mg/kg; i.v.; once) decreases the conduction velocity in T 4 -treated rat atrium by decreasing the Max dV/dt and net inward current [1]. Animal Model: Male Sprague-Dawley (SD) rats weighing from 200 to 220 g, with levo-thyroxine (T 4 ) treatment [1] Dosage: 2 mg/kg Administration: Bolus injection into right external carotid vein within 2 minutes, once Result: Elongated the QT interval at 15 and 60 minutes after administration. Shortened P wave and QRS complex durations. Markedly decreased action potential amplitudes (APA) and Max dV/dt, and significantly lengthened the action potential durations.
Cas No.
88069-67-4
分子式
C17H24N2O
分子量
272.39
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years