Bepridil hydrochloride 是一种钙通道阻滞剂,还抑制 Na+/Ca2+ 交换 (NCX)、钠通道和心脏肌膜 KATP 通道,具有抗心绞痛的作用。
产品描述
Bepridil is a calcium channel blocker and also inhibits Na+/Ca2+ exchange (NCX), sodium channels and cardiac sarcolemmal KATP channels.
体外活性
Bepridil (1-100 microM) inhibited the K(ATP) channel current in a concentration-dependent manner. The IC(50) value of bepridil was estimated to be 10.5 microM for outward K(ATP) channel currents (holding potential, +60 mV) and 6.6 microM for inward K(ATP) channel currents (holding potential, -60 mV). Bepridil (0.1-30 microM) also inhibited K(Na) channel currents measured at the holding potential of -60 mV, in a concentration-dependent manner with an IC(50) value of 2.2 microM [2].
体内活性
The predominant effects of Bepridil (cumulative dose = 9.0 mg/kg i.v.) in the conscious rat were reduced coronary vascular resistance and heart rate. Bepridil showed selectivity for the coronary circulation since systemic vascular resistance was not significantly reduced until cumulative i.v. dosage of 21.0 mg/kg was administered [1].
Cas No.
68099-86-5
分子式
C24H35ClN2O
分子量
403.01
别名
CERM 1978;盐酸苄普地尔
储存和溶解度
DMSO:130 mg/mL (322.58 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years