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人类心肌中的功能性β1和β2肾上腺素能受体。

Functional beta 1- and beta 2-adrenoceptors in the human myocardium.

作者信息

Ask J A, Stene-Larsen G, Helle K B, Resch F

出版信息

Acta Physiol Scand. 1985 Jan;123(1):81-8. doi: 10.1111/j.1748-1716.1985.tb07564.x.

Abstract

Functional beta-adrenoceptor populations in the human heart were studied in vitro in electrically-paced strips of the right auricular and ventricular myocardium. The relative potency of selected agonists in producing inotropic responses (Tmax, T'max) in the presence of blockers for neuronal and extraneuronal uptakes was found to be as follows: isoprenaline greater than noradrenaline = adrenaline = salbutamol greater than dobutamine. Prenalterol had a negative inotropic effect in these preparations. The selective beta 1-(practolol) and beta 2-(H 35/25) blockers reduced inotropic responses to adrenaline (Tmax, T'max) and noradrenaline (T'max) in the auricular strips. These results indicate the participation of beta 2-adrenoceptors in inotropic responses in the human auricular and ventricular myocardium. For comparison, inotropic responses of electrically-paced rat myocardium to beta-adrenergic agonists in the presence of blockers for neuronal and extraneuronal uptakes were likewise studied. The relative potencies for Tmax were: noradrenaline = adrenaline greater than prenalterol greater than dobutamine = salbutamol. Given the high relative potency of salbutamol in the human myocardial strips (analogous to that previous shown in the beta 2-dominated atria of the frog and trout) and the low relative potency of salbutamol in the rat tissue, these findings indicate a greater population of functionally active beta 2-adrenoceptors in the human than in the rat myocardium.

摘要

在体外对人心脏中具有功能的β - 肾上腺素能受体群体进行了研究,研究对象为右心房和心室心肌的电刺激条带。在存在神经元和非神经元摄取阻滞剂的情况下,选定激动剂产生变力反应(Tmax、T'max)的相对效价如下:异丙肾上腺素大于去甲肾上腺素 = 肾上腺素 = 沙丁胺醇大于多巴酚丁胺。普瑞特罗在这些制剂中具有负性变力作用。选择性β1 - (心得宁)和β2 - (H 35/25)阻滞剂降低了心房条带对肾上腺素(Tmax、T'max)和去甲肾上腺素(T'max)的变力反应。这些结果表明β2 - 肾上腺素能受体参与了人心房和心室心肌的变力反应。为作比较,同样研究了在存在神经元和非神经元摄取阻滞剂的情况下,电刺激的大鼠心肌对β - 肾上腺素能激动剂的变力反应。Tmax的相对效价为:去甲肾上腺素 = 肾上腺素大于普瑞特罗大于多巴酚丁胺 = 沙丁胺醇。鉴于沙丁胺醇在人心肌条带中的相对效价较高(类似于先前在青蛙和鳟鱼以β2为主的心房中所显示的)以及沙丁胺醇在大鼠组织中的相对效价较低,这些发现表明人心脏中功能活跃的β2 - 肾上腺素能受体群体比大鼠心肌中的更多。

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