Lercanidipine hydrochloride (Corifeo) is a calcium channel blocker of the dihydropyridine class.

Lercanidipine的体外钙通道拮抗活性主要通过逐渐阻断L型钙通道，减少钙离子进入平滑肌细胞来实现。同时，Lercanidipine能够抑制细胞内胆固醇酯的形成。在临床常见浓度下，它可能抑制体外巨噬细胞功能，这些功能与动脉粥样硬化的形成及斑块稳定性有关[1]。

在长期插管的实验性肾血管性高血压犬模型中，Lercanidipine以剂量依赖的方式降低舒张压（ED25 = 0.9 mg/kg p.o）。同一动物模型中，Lercanidipine的长期应用显示出舒张压持续下降，表明其抗高血压效果没有耐受性出现[3]。Lercanidipine具有显著的抗惊厥效果，并且不影响小鼠的肌肉协调能力或运动活动[5]。在临床研究中，Lercanidipine具有24小时的抗高血压效果，并且不会导致心率显著增加。研究表明，Lercanidipine在包括轻至中度高血压、重度高血压、老年人及孤立性收缩期高血压患者在内的广泛的高血压患者中均有效，且与低发生率的不良事件相关[4]。

Cell-free enzyme assays are performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions are performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 are used to phosphorylate 30 μM of the synthetic ROCK peptide substrate S6 Long, prepared at American Peptide with the addition of 10 μM ATP, containing?33P-ATP in the presence of 10 mM Mg2+, 50 mM Tris, pH 7.5, 0.1 mM EGTA and 1 mM DTT at room temperature. One unit is the amount of kinase needed to catalyze the transfer of 1 nmol phosphate/min to the peptide. The reactions are allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions are captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation is measured on a Perkin-Elmer MicroBeta 1450.

Cells are incubated for 24 hours in DMEM+EFAF 0.2% and lercanidipine, then with lercanidipine and AcLDL for 24 hours. In the last 2 hours [14C]-oleic acid albumin complex is added for the determination of cholesterol esterification (ACAT activity). (Only for Reference)