Investigation of antiischemic properties and mechanism of action of azacrown ether derivative.

K G Gurbanov, A A Paperno, S A Bogomaz
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Abstract

The influence of the azacrown ether derivative benzylaza-15-crown-5 on myocardial tolerance to ischemia and on the functional state of the zone of myocardial ischemia during coronary artery occlusion was investigated in experiments on anaesthetized open-chest cats. The compound tested produced a dose-dependent antiischemic effect and prevented the development of myocardial ischemia. In experiments on isolated guinea-pig papillary muscle benzylaza-15-crown-5 inhibited the first and second components of the isoproterenol-induced muscle contraction. The compound decreased the maximal contraction force and had no effect on the cardiac cycle duration and on the time necessary for reaching maximal tension. It is suggested that the protective effect of benzylaza-15-crown-5 during myocardial ischemia is mediated through the inhibition of calcium release from the sarcoplasmic reticulum.

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氮冠醚衍生物的抗缺血特性及作用机制研究。
通过对麻醉开胸猫的实验,研究了氮杂冠醚衍生物苄基-15-冠-5对冠状动脉闭塞期心肌缺血耐受性和心肌缺血区功能状态的影响。该化合物具有剂量依赖性的抗缺血作用,可防止心肌缺血的发生。在离体豚鼠乳头肌实验中,苄基-15-冠-5抑制异丙肾上腺素诱导的第一和第二组分肌肉收缩。该化合物降低了最大收缩力,对心脏周期持续时间和达到最大张力所需的时间没有影响。提示:苄基-15-冠-5对心肌缺血的保护作用可能是通过抑制肌浆网钙的释放而介导的。
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