阿片类激动剂和拮抗剂及其立体异构体的抗心律失常活性。
Anti-arrhythmic activities of opioid agonists and antagonists and their stereoisomers.
作者信息
Sarne Y, Flitstein A, Oppenheimer E
机构信息
Department of Physiology and Pharmacology, Sackler School of Medicine, Tel Aviv University, Israel.
出版信息
Br J Pharmacol. 1991 Mar;102(3):696-8. doi: 10.1111/j.1476-5381.1991.tb12235.x.
Abstract
- A series of opioid agonists, antagonists and their (+)-stereoisomers were tested for antiarrhythmic activity in the rat coronary artery occlusion model. 2. Naloxone (0.01-2 mg kg-1) significantly reduced the incidence and severity of cardiac arrhythmias, in accordance with previous published studies. 3. The non-opioid stereoisomer, (+)-naloxone, was equipotent with naloxone against occlusion-induced arrhythmia. 4. Similar non-stereospecific antiarrhythmic effects were induced by another opioid antagonist, Win 44,441-3 and its stereoisomer Win 44,441-2. 5. The opioid agonists, morphine and levorphanol, protected against occlusion-induced arrhythmia as did the opioid antagonists, and the (+)-stereoisomer, dextrorphan, was equipotent to levorphanol. 6. It is concluded that the antiarrhythmic effects of opioid drugs are not mediated by opioid receptors. A direct effect on ionic currents in cardiac muscle is suggested as the mechanism of opioid antiarrhythmic activity.
摘要
- 一系列阿片类激动剂、拮抗剂及其（+）-立体异构体在大鼠冠状动脉闭塞模型中进行了抗心律失常活性测试。2. 纳洛酮（0.01 - 2毫克/千克）显著降低了心律失常的发生率和严重程度，这与先前发表的研究一致。3. 非阿片类立体异构体（+）-纳洛酮在对抗闭塞性心律失常方面与纳洛酮等效。4. 另一种阿片类拮抗剂Win 44,441 - 3及其立体异构体Win 44,441 - 2也诱导了类似的非立体特异性抗心律失常作用。5. 阿片类激动剂吗啡和左啡诺与阿片类拮抗剂一样能预防闭塞性心律失常，并且（+）-立体异构体右啡烷与左啡诺等效。6. 得出的结论是，阿片类药物的抗心律失常作用不是由阿片受体介导的。提示对心肌离子电流的直接作用是阿片类抗心律失常活性的机制。
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