Ramipril (Altace) is a long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.

ACE:5 nM

在自发性高血压鼠中,Ramipril显著抑制主动脉及肺ACE（IC50：~5 mg/kg）, 但不影响脑部ACE.缓慢给药小鼠时,Ramipril与体外处理HUVECs时相似,具有降血压的效果,且和其他ACE抑制剂相比,对脂多糖诱导的凋亡率有显著降低作用.作用于自发性高血压大鼠时,Ramipril抑制收缩压（IC50：1.97 mg/kg）,与AT1受体阻断剂联用可协同提高SBP的降低数.作用于骨原壳蛋白处理的鼠时,Ramipril抑制beta细胞功能紊乱,通过降低单核白细胞/巨噬细胞渗透率, 及凋亡和纤维化,且降低 生长因子基因,RAS和炎症分子表达.

用Ramipril长期处理原代人内皮细胞,能够增加ACE表达, JNK抑制剂SP600125阻断该作用。 作用于血清饥饿法处理的体外内皮细胞时,Ramipril不会促进凋亡。作用于培养的内皮细胞时,Ramipril使ACE结合的CK2活性及ACE在Ser1270位点磷酸化增强,但作用于ACE缺陷或S1270A ACE突变的细胞时,不能刺激c-Jun在核内累积或不能激活JNK。

The HUVECs are pretreated with the active metabolites of Ramipril for 24 hours. A serum deprivation method is used to induce apoptosis in the presence of Ramipril for an additional 24 hours. The rate of apoptosis is then determined using flow cytometry with two makers annexinV fluorescein isothiocyanate (FITC+) and propidium iodide (PI).(Only for Reference)