四种钙拮抗剂在大鼠体内作为子宫收缩抑制剂的效能和选择性。
The potencies and selectivities of four calcium antagonists as inhibitors of uterine contractions in the rat in vivo.
作者信息
Abel M H, Hollingsworth M
出版信息
Br J Pharmacol. 1985 May;85(1):263-9. doi: 10.1111/j.1476-5381.1985.tb08855.x.
The potencies of four calcium antagonists (nifedipine, gallopamil, verapamil and diltiazem) at inhibiting uterine contractions in vivo have been assessed in the conscious ovariectomized, post-partum rat. Their selectivities for this action, relative to their effects on blood pressure and heart rate, have been compared with salbutamol. All compounds produced a dose-dependent inhibition of intra-uterine pressure cycles. The rank order of potency was salbutamol greater than nifedipine greater than diltiazem = gallopamil greater than verapamil. All compounds produced a dose-dependent fall of mean blood pressure. The rank order of potency was salbutamol greater than nifedipine greater than gallopamil greater than verapamil greater than diltiazem. Salbutamol and nifedipine produced a tachycardia, which was very marked with salbutamol. Gallopamil, verapamil and diltiazem induced a moderate tachycardia at low doses but temporary cessation of heart beat occurred at high doses. Nifedipine and diltiazem, like salbutamol, exhibited some selectivity for inhibition of uterine contractions relative to their cardiovascular actions. Gallopamil and verapamil showed no selectivity for the uterus.
在清醒的去卵巢产后大鼠体内评估了四种钙拮抗剂（硝苯地平、加洛帕米、维拉帕米和地尔硫䓬）抑制子宫收缩的效能。已将它们对该作用的选择性与其对血压和心率的影响相比较，并与沙丁胺醇进行了对比。所有化合物均产生剂量依赖性的子宫内压周期抑制作用。效能的排序为沙丁胺醇＞硝苯地平＞地尔硫䓬 = 加洛帕米＞维拉帕米。所有化合物均产生剂量依赖性的平均血压下降。效能的排序为沙丁胺醇＞硝苯地平＞加洛帕米＞维拉帕米＞地尔硫䓬。沙丁胺醇和硝苯地平引起心动过速，沙丁胺醇引起的心动过速非常明显。加洛帕米、维拉帕米和地尔硫䓬在低剂量时引起中度心动过速，但在高剂量时出现心跳暂时停止。硝苯地平和地尔硫䓬与沙丁胺醇一样，相对于其心血管作用，对子宫收缩的抑制表现出一定的选择性。加洛帕米和维拉帕米对子宫无选择性。
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