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β2肾上腺素能受体激动剂非诺特罗和沙丁胺醇对离体人心室肌收缩力的影响。

Effects of the beta 2-adrenoceptor agonists fenoterol and salbutamol on force of contraction in isolated human ventricular myocardium.

作者信息

Mügge A, Posselt D, Reimer U, Schmitz W, Scholz H

出版信息

Klin Wochenschr. 1985 Jan 2;63(1):26-31.

PMID:3974172
Abstract

The effects of fenoterol and salbutamol on isometric force of contraction were studied in isolated, electrically driven human papillary muscle preparations. Fenoterol increased force of contraction at concentrations of 1 mumol l-1 and higher. The maximally effective concentration of fenoterol (100 mumol l-1) increased force of contraction by about 130%. The positive inotropic effect of fenoterol was not influenced by 0.1 mumol l-1 prazosin. The beta 1-selective antagonist atenolol (2 mumol l-1) and the beta 2-selective antagonist ICI 118551 (1 mumol l-1) shifted the concentration-response curve of fenoterol to the right, indicating that beta 1- and beta 2-adrenoceptors may contribute to the positive inotropic effect of fenoterol. In contrast to fenoterol, salbutamol increased force of contraction only by about 11% at 100 mumol l-1. The results indicate that: (1) fenoterol exerts a direct positive inotropic effect in the human heart which may support the beneficial effects of the reduction of systemic vascular resistance in patients with congestive heart failure; (2) this positive inotropic effect of fenoterol is mediated by beta 1- and beta 2-adrenoceptors; (3) the clinically observed improvement of cardiac performance in the case of salbutamol is presumably not due to any direct positive inotropic effect.

摘要

在离体电驱动的人乳头肌标本中研究了非诺特罗和沙丁胺醇对等长收缩力的影响。非诺特罗在浓度为1μmol/L及更高时可增加收缩力。非诺特罗的最大有效浓度(100μmol/L)可使收缩力增加约130%。非诺特罗的正性肌力作用不受0.1μmol/L哌唑嗪的影响。β1选择性拮抗剂阿替洛尔(2μmol/L)和β2选择性拮抗剂ICI 118551(1μmol/L)使非诺特罗的浓度-反应曲线右移,表明β1和β2肾上腺素能受体可能参与非诺特罗的正性肌力作用。与非诺特罗相反,沙丁胺醇在100μmol/L时仅使收缩力增加约11%。结果表明:(1)非诺特罗在人心脏中发挥直接的正性肌力作用,这可能支持了充血性心力衰竭患者降低全身血管阻力的有益作用;(2)非诺特罗的这种正性肌力作用由β1和β2肾上腺素能受体介导;(3)临床上观察到的沙丁胺醇治疗时心脏功能的改善可能并非由于任何直接的正性肌力作用。

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