地尔硫卓,属于非二氢吡啶类钙通道阻滞剂,主要是通过与L型钙通道的α1亚基上P区临近部分的高度保守序列结合,从而导致钙通道的空间构象改变,阻滞其正常开放,导致细胞外钙离子内流受阻。这将会导致:1.平滑肌细胞MLC磷酸化磷酸化受阻,ATP酶活性减弱而阻碍化学能-机械能转换,使平滑肌兴奋收缩脱偶联,进而平滑肌舒张;2.心房室肌细胞钙通道开放的概率降低,心肌收缩力下降;3.心脏传导纤维及起搏细胞动作电位形成过程滞缓,自律性下降,传到减慢。上述作用使地尔硫卓得以用于降压,抗心律失常,外周血管扩张,平滑肌解痉,保护心肌,预防冠脉重建后缺血区无复流现象等。 Diltiazem, a non-dihydropyridine calcium channel blocker, binds primarily to a highly conserved sequence near the P-region of the α1 subunit of the L-type calcium channel, resulting in a change in the spatial conformation of the calcium channel that blocks its normal Open, leading to blocked extracellular calcium influx. This will lead to: 1. MLC phosphorylation of smooth muscle cell phosphorylation blocked ATPase activity and impede the chemical energy - mechanical energy conversion, the excitability of the smooth muscle uncoupling, and thus smooth muscle relaxation; 2. Atrial cell calcium channels open Decreased probability of myocardial contractility decreased; 3 cardiac conduction fibers and pacemaker cell action potential formation slow, self-discipline decreased, reaching slow down. These effects make diltiazem can be used for antihypertensive, antiarrhythmic, peripheral vasodilatation, smooth muscle spasm, protect the myocardium, prevent ischemic area after coronary reperfusion no reflow phenomena.