Broughton Pipkin F, Chinnery E
Br J Pharmacol. 1985 Nov;86(3):705-9. doi: 10.1111/j.1476-5381.1985.tb08949.x.
Six point concentration-response curves were established for the contractile effect of prostaglandin E2 (PGE2) on helically-cut strips of human chorionic plate arteries. Tissues were then allocated to one of four treatment groups: a control group and 3 groups exposed to the calcium channel blocker nitrendipine at 10(-9), 10(-7) or 10(-5) M. The concentration-response curves were then repeated. The addition of nitrendipine was associated with a significant depression of the induced contraction. The contractile response to the lower doses of PGE2 was replaced by a small relaxation in 63% of the treated tissues. It is suggested that in these tissues PGE2 exerts its constrictor effect via the receptor-operated channels and that nitrendipine is blocking this effect. Similar experiments performed with PGE1 showed great variability in the initial response. Nitrendipine 10(-5) M failed to exert any detectable effect on this response. Pregnancy-induced hypertension is associated with vasoconstriction in both the maternal and placental circulations. There also appears to be a relative excess of vasoconstrictor eicosanoid production. Nitrendipine may be of use in the treatment of this condition.
建立了六点浓度-反应曲线，以研究前列腺素E2（PGE2）对人绒毛膜板动脉螺旋形切片的收缩作用。然后将组织分配到四个治疗组之一：一个对照组和三个分别暴露于10(-9)、10(-7)或10(-5) M钙通道阻滞剂尼群地平的组。然后重复浓度-反应曲线。加入尼群地平与诱导收缩的显著抑制有关。在63%的处理组织中，对较低剂量PGE2的收缩反应被轻微舒张所取代。提示在这些组织中，PGE2通过受体操纵通道发挥其收缩作用，而尼群地平阻断了这种作用。用PGE1进行的类似实验显示初始反应存在很大差异。10(-5) M的尼群地平对该反应未产生任何可检测到的作用。妊娠高血压与母体和胎盘循环中的血管收缩有关。似乎还存在血管收缩性类花生酸产生的相对过量。尼群地平可能用于治疗这种病症。
