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钙通道阻滞剂地尔硫䓬对犬冠状动脉和股动脉中去甲肾上腺素、5-羟色胺及钾离子去极化所致血管收缩反应的影响。

The effect of diltiazem, a calcium channel blocking agent, on vasoconstrictor responses to norepinephrine, serotonin and potassium depolarization in canine coronary and femoral arteries.

作者信息

Mullett M, Gharaibeh M, Warltier D C, Gross G J

出版信息

Gen Pharmacol. 1983;14(2):259-64. doi: 10.1016/0306-3623(83)90006-x.

Abstract
  1. Diltiazem produced a dose-dependent inhibition of contractions due to norepinephrine (NE), serotonin (5HT) and high potassium depolarization in both coronary and femoral artery rings. 2. Diltiazem was a more potent and efficacious blocker of all 3 agonists in the coronary arteries. 3. Dose response curves to NE and 5HT indicated that diltiazem produced a noncompetitive type of blockade. 4. Diltiazem blocked contractions produced by 5HT more easily than those produced by NE in both coronary and femoral artery rings. 5. That diltiazem was more potent in coronary than femoral arteries suggests a basic difference in calcium regulation in the two vessels.
摘要
  1. 地尔硫䓬对冠状动脉和股动脉环中去甲肾上腺素(NE)、5-羟色胺(5HT)以及高钾去极化所引起的收缩产生剂量依赖性抑制作用。2. 地尔硫䓬对冠状动脉中所有这三种激动剂的阻断作用更强且更有效。3. 对NE和5HT的剂量反应曲线表明,地尔硫䓬产生的是一种非竞争性阻断作用。4. 在冠状动脉和股动脉环中,地尔硫䓬阻断5HT所引起的收缩比阻断NE所引起的收缩更容易。5. 地尔硫䓬在冠状动脉中比在股动脉中更有效,这表明这两种血管在钙调节方面存在根本差异。

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