DPI 201-106对电压门控钠通道的有心脏选择性调节活性,从而产生正性肌力作用。DPI 201-106 具有协同肌膜和细胞内作用机制。
产品描述
DPI 201-106 is a cardioselective inhibitor of the TTX-resistant h1 Na channel inactivation resulting in a positive inotropic effect. DPI-201-106 also inhibits the inward and delayed rectifier potassium currents and L-type calcium current.
体外活性
DPI 201-106(0.1 - 3 μM) produces concentration-dependent positive inotropic effects in guinea-pig and rat left atria, kitten, rabbit and guinea-pig papillary muscles and Langendorff perfused hearts of rabbits[2]. DPI 201-106 increases the Ca2+ sensitivity(EC50 = 0.2 nM) of skinned fibres from porcine trabecula septomarginalis[2].
体内活性
DPI 201-106(0.2 mg/kg i.v) administration increased left ventricular dP/dtmax in anesthetized dogs[3].
Cas No.
97730-95-5
分子式
C29H30N4O2
分子量
466.57
别名
DPI-201-106
储存和溶解度
DMSO:250 mg/mL (535.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years