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β1肾上腺素能受体部分激动剂(ICI 118,587)对冠心病左心室功能及代谢的影响

[Effects of a partial agonist of beta 1 adrenergic receptors (ICI 118,587) on left ventricular performance and metabolism in coronary disease].

作者信息

Rousseau M F, Pouleur H, Etienne J, Mengeot P, Cheron P

出版信息

Arch Mal Coeur Vaiss. 1984 Jan;77(1):76-84.

PMID:6142702
Abstract

ICI 118/587 is a partial agonist of beta 1 adrenergic receptors, a partial agonist being an agent which has both agonist and antagonist properties. The agonist properties of ICI 118/587 stabilise 43 p. 100 of the maximal activity of the beta 1 receptors whilst preventing a resulting increase in sympathetic stimulation. The aim of this study was to evaluate the effects of this new inotropic agent on left ventricular function and metabolism in patients with chronic myocardial infarction and left ventricular dysfunction. The study of LV function was performed in an initial group of 14 patients. After control left ventriculography, the injection of 0,1 mg/kg of ICI 118/587 increased the peak dP/dt by 35 p. 100 (p less than 0,005), reduced mean systolic parietal stress by 8 p. 100 (p less than 0,05) and LV end systolic volume from 58 to 53 ml/m2 (p less than 0,05). The global ejection fraction rose slightly, largely due to increases in the regional ejection fractions of abnormal segments (from 20 +/- 5 p. 100 to 26 +/- 5 p. 100, p less than 0,02). Left ventricular diastolic function also improved as shown by a 38 p. 100 fall (p less than 0,001) in mean diastolic stress and an increase in the time constant of isovolumic relaxation. The metabolic effects of ICI 118/587 were assessed in a second group of 11 patients with anterior myocardial infarction.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

ICI 118/587是β1肾上腺素能受体的部分激动剂,部分激动剂是一种兼具激动剂和拮抗剂特性的药物。ICI 118/587的激动剂特性可使β1受体最大活性稳定在43%,同时防止交感神经刺激增加。本研究的目的是评估这种新型正性肌力药物对慢性心肌梗死合并左心室功能不全患者左心室功能和代谢的影响。对最初的14例患者进行了左心室功能研究。在对照左心室造影后,注射0.1mg/kg的ICI 118/587可使dp/dt峰值增加35%(p<0.005),平均收缩期壁应力降低8%(p<0.05),左心室舒张末期容积从58ml/m²降至53ml/m²(p<0.05)。总体射血分数略有上升,主要是由于异常节段的局部射血分数增加(从20±5%增至26±5%,p<0.02)。左心室舒张功能也有所改善,表现为平均舒张期应力下降38%(p<0.001)和等容舒张时间常数增加。在第二组11例前壁心肌梗死患者中评估了ICI 118/587的代谢效应。(摘要截选至250字)

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