具有钙激动特性的二氢吡啶类化合物BAY K 8644和CGP 28392对大鼠门静脉自发机械活动影响的比较：紫外线辐射对其作用的改变

A comparison of effects of BAY K 8644 and CGP 28392, dihydropyridines with Ca agonistic properties, on spontaneous mechanical activity in rat portal vein: modification of effect by ultraviolet radiation.

作者信息

Mikkelsen E O, Nyborg N C, Jakobsen P

出版信息

Acta Pharmacol Toxicol (Copenh). 1985 Nov;57(5):340-4. doi: 10.1111/j.1600-0773.1985.tb00055.x.

DOI:10.1111/j.1600-0773.1985.tb00055.x

Abstract

The effect of CGP 28392 and BAY K 8644 was studied on isolated portal veins from male Wistar Kyoto rats. BAY K 8644 and CGP 28392 induced a concentration dependent increase in spontaneous mechanical activity in low but not in high concentrations. The portal vein was more sensitive to the effect of BAY K 8644 than to that of CGP 28392. In Ca free medium the increasing effect of BAY K 8644 and CGP 28392 on the mechanical activity was abolished and restored by readdition of calcium. Nifedipine abolished the augmenting effect of BAY K 8644 and CGP 28392 on mechanical activity. Ultraviolet radiation (UVR) depressed the effect of BAY K 8644 but had no effect on mechanical activity induced by CGP 28392. BAY K 8644 and CGP 28392 degradate slowly under influence of UVR; BAY K 8644 was far more resistant to the destroying effect of UVR than CGP 28392. The results indicate that both BAY K 8644 and CGP 28392 increase the spontaneous mechanical activity in rat portal vein by enhancing Ca influx. The effect of BAY K 8644 differs from that of CGP 28392 by being sensitive to UVR; this action seems not to be due to a direct UVR destroying effect of the substances, but rather to a BAY K 8644 induced sensibilisation of the tissue to UVR.

摘要

研究了CGP 28392和BAY K 8644对雄性Wistar Kyoto大鼠离体门静脉的作用。低浓度而非高浓度时，BAY K 8644和CGP 28392可引起自发性机械活动呈浓度依赖性增加。门静脉对BAY K 8644的作用比CGP 28392更敏感。在无钙培养基中，BAY K 8644和CGP 28392对机械活动的增强作用消失，重新添加钙后恢复。硝苯地平消除了BAY K 8644和CGP 28392对机械活动的增强作用。紫外线辐射（UVR）抑制了BAY K 8644的作用，但对CGP 28392诱导的机械活动无影响。在UVR影响下，BAY K 8644和CGP 28392降解缓慢；BAY K 8644比CGP 28392对UVR的破坏作用更具抗性。结果表明，BAY K 8644和CGP 28392均通过增强钙内流增加大鼠门静脉的自发性机械活动。BAY K 8644的作用与CGP 28392不同，对UVR敏感；这种作用似乎不是由于物质的直接UVR破坏作用，而是由于BAY K 8644诱导组织对UVR敏感。