对人离体动脉对去甲肾上腺素反应的拮抗作用。
Antagonism of the response of human isolated arteries to noradrenaline.
作者信息
Birmingham A T, Ernest K, Newcombe J F
出版信息
Br J Pharmacol. 1969 Jan;35(1):127-31. doi: 10.1111/j.1476-5381.1969.tb07973.x.
Abstract
- Spirally-cut strips from human visceral arteries isolated in vitro were contracted by noradrenaline and this contraction was antagonized by the alpha-receptor blocking agent, thymoxamine.2. The cumulative log dose-response curves to noradrenaline in the presence of thymoxamine were moved to the right of and parallel to the curve for noradrenaline alone. The blockade was surmountable and reversible.3. The quantitative criteria for simple competitive antagonism were satisfied. When log (x - 1) was plotted against pA(x) the points fitted a straight line with a slope (-n) of 0.91. The pA(2) for thymoxamine was 7.54 and the mean value for log K(2) was 7.82. These values are in approximate agreement with those previously reported for animal isolated arterial strips.
摘要
体外分离的人内脏动脉的螺旋形切片可被去甲肾上腺素收缩，且这种收缩可被α受体阻断剂噻吗洛尔拮抗。
在噻吗洛尔存在的情况下，去甲肾上腺素的累积对数剂量-反应曲线向右移动且与单独使用去甲肾上腺素的曲线平行。这种阻断是可克服且可逆的。
满足简单竞争性拮抗的定量标准。当绘制log(x - 1)对pA(x)的图时，各点拟合为一条斜率(-n)为0.91的直线。噻吗洛尔的pA(2)为7.54，log K(2)的平均值为7.82。这些值与先前报道的动物离体动脉切片的值大致相符。
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