Isradipine (PN 200-110) is a dihydropyridine calcium channel blockers with antihypertensive and vasodilator activities. Isradipine blocks the calcium entry through the calcium ion channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This increases oxygen delivery due to an increased blood flow and reduces oxygen requirements due to decreasing in total peripheral resistance.

Ca2+ channel:34±8 μM

在易吸收乙醇的大鼠体内,Isradipine（1 mg/kg,3次/天）减少超过70%的乙醇摄入,减少的乙醇以成比例的水消耗补偿,且在处理的5天中该作用一直存在.在小鼠体内,Isradipine抑制可卡因和吗啡的戒断症状,也许可以成为针对海洛因和可卡因滥用的有效药物疗法.在自发性高血压大鼠体内,Isradipine使两种菌株中动脉管壁胶原蛋白含量显著减少,使颈动脉中弹性蛋白含量显著增加,但对主动脉壁中弹性蛋白的含量没有影响.Isradipine使低氧诱导的钙依赖型黄嘌呤氧化酶,胞质磷脂酶A(2),单胺氧化酶和环氧合酶-2的活化减少,并伴随细胞色素C释放和自由基产生的减少.Isradipine可预防低压缺氧伴随的神经病变增加,并预防caspase 3与钙蛋白酶表达增加诱导的记忆障碍.

体内摄氧量(I50 = 31.1 mM)和生长培养(I50 = 20.8 mM)测定显示Isradipine是效果最好的衍生物。在微摩尔浓度下,Isradipine对克氏锥虫Tulahuen菌株短膜型的耗氧量和生长培养即有抑制作用。