Department of Physiology, Jefferson Medical College, Thomas Jefferson University, Philadelphia, Pennsylvania, 19107.
Pharm Res. 1985 May;2(3):130-4. doi: 10.1023/A:1016363316777.
We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival time of 1.9 ± 0.1 hours. Neither verapamil analog had any significant effect on attenuating the shock-induced rise in plasma cathepsin D activity. However, both anipamil and ronipamil (p < 0.01) significantly blunted the rate of MDF accumulation in the plasma. In addition, these agents significantly inhibited proteolysis in vitro. Both analogs significantly prolonged survival time to 3.1 ± 0.6 h at 0.25 mg/kg (p < 0.05) and to 4.4 ± 0.3 h at 1.0 mg/kg (p < 0.001). Anipamil appears to provide a more potent protection in this shock model; however, both verapamil derivatives possess promising anti-shock potential.
我们研究了两种异搏定类似物,即阿尼帕米和罗尼帕米,在创伤性休克中的作用。 Noble-Collip 鼓创伤导致休克状态,其特征是血浆组织蛋白酶 D 活性增加 8 倍,血浆心肌抑制因子 (MDF) 积累率增加 13 倍,存活时间为 1.9 ± 0.1 小时。两种异搏定类似物均未对减轻休克引起的血浆组织蛋白酶 D 活性升高产生任何显著影响。然而,阿尼帕米和罗尼帕米(p < 0.01)均显著减弱了血浆中 MDF 积累的速率。此外,这些药物还显著抑制了体外的蛋白水解。两种类似物均能显著延长 0.25mg/kg 时的存活时间至 3.1 ± 0.6 小时(p < 0.05)和 1.0mg/kg 时的 4.4 ± 0.3 小时(p < 0.001)。阿尼帕米在这种休克模型中似乎提供了更有效的保护;然而,两种异搏定衍生物均具有有前途的抗休克潜力。