阿片受体拮抗剂在心肌缺血中的立体特异性抗心律失常作用。
Stereospecific antiarrhythmic effect of opioid receptor antagonists in myocardial ischaemia.
作者信息
Parratt J R, Sitsapesan R
出版信息
Br J Pharmacol. 1986 Apr;87(4):621-2. doi: 10.1111/j.1476-5381.1986.tb14577.x.
Abstract
The effects of the stereoisomers of two different antagonists at opioid receptors were examined on the ventricular arrhythmias that result from acute coronary artery ligation in anaesthetized male rats. (-)-Mr 1452(but not the (+)-isomer, Mr 1453) reduced, in a dose-dependent manner, the number of ventricular ectopic beats and the incidence or duration of both ventricular tachycardia and fibrillation. (-)-WIN 44,441-3 (but not its (+)-isomer, WIN 44,441-2) had a similar protective effect in ischaemia. These results suggest that antagonism of the effects of endogenous opioid peptides at specific receptors results in reduced severity of arrhythmias in myocardial ischaemia.
摘要
研究了两种不同阿片受体拮抗剂的立体异构体对麻醉雄性大鼠急性冠状动脉结扎所致室性心律失常的影响。（-）-Mr 1452（而非其（+）-异构体Mr 1453）以剂量依赖性方式减少室性早搏的数量以及室性心动过速和颤动的发生率或持续时间。（-）-WIN 44,441-3（而非其（+）-异构体WIN 44,441-2）在缺血时具有类似的保护作用。这些结果表明，内源性阿片肽在特定受体上的作用被拮抗会导致心肌缺血时心律失常的严重程度降低。
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本文引用的文献
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Coronary artery ligation in anesthetized rats as a method for the production of experimental dysrhythmias and for the determination of infarct size.在麻醉大鼠中进行冠状动脉结扎，作为产生实验性心律失常和测定梗死面积的一种方法。
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Multiple opioid receptor profile in vitro and activity in vivo of the potent opioid antagonist Win 44,441-3.强效阿片类拮抗剂Win 44,441-3的体外多种阿片受体特征及体内活性
Life Sci. 1983;33 Suppl 1:303-6. doi: 10.1016/0024-3205(83)90503-9.
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Antiarrhythmic actions of meptazinol, a partial agonist at opiate receptors, in acute myocardial ischaemia.美普他酚（一种阿片受体部分激动剂）在急性心肌缺血中的抗心律失常作用。
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Naloxone inhibits early arrhythmias resulting from acute coronary ligation.纳洛酮可抑制急性冠状动脉结扎所致的早期心律失常。
Br J Pharmacol. 1982 Aug;76(4):504-6. doi: 10.1111/j.1476-5381.1982.tb09246.x.
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