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三种β-氨基酰胺(IQB-M-81、利多卡因和妥卡尼)对离体大鼠心房作用的比较。

Comparison of three beta-amino anilides: IQB-M-81, lidocaine and tocainide, on isolated rat atria.

作者信息

Tejerina T, Barrigón S, Tamargo J

出版信息

Eur J Pharmacol. 1983 Nov 11;95(1-2):93-9. doi: 10.1016/0014-2999(83)90271-6.

Abstract

The effects of a new beta-amino anilide, IQB-M-81, on electrical and mechanical activity of isolated rat atria were studied and compared with those of lidocaine and tocainide. In spontaneously beating right atria IQB-M-81 produced a dose-dependent decrease in rate, contractile force and maximum following frequency and prolonged the sinus node recovery time and the effective refractory period of atrial fibers. The negative inotropic effect was not modified by pretreating the atria with atropine or practolol. In isolated right atria IQB-M-81 did not block the positive chronotropic and inotropic responses to isoprenaline but shifted the dose-response curve to the right. IQB-M-81 and lidocaine, but not tocainide, reduced in a dose-dependent manner the slow contractions induced by isoprenaline in K-depolarized right atria. These results suggest that in contrast to other beta-amino anilides, IQB-M-81 exerted a negative chronotropic effect and that it presented a class I antiarrhythmic effect on isolated rat atria. A possible class IV antiarrhythmic effect is also discussed.

摘要

研究了一种新型β-氨基苯胺类化合物IQB-M-81对离体大鼠心房电活动和机械活动的影响,并与利多卡因和妥卡尼进行了比较。在自发搏动的右心房中,IQB-M-81可使心率、收缩力和最大跟随频率呈剂量依赖性降低,并延长窦房结恢复时间和心房纤维的有效不应期。用阿托品或心得宁预处理心房后,负性肌力作用未被改变。在离体右心房中,IQB-M-81不阻断对异丙肾上腺素的正性变时和变力反应,但使剂量-反应曲线右移。IQB-M-81和利多卡因(而非妥卡尼)可剂量依赖性地降低异丙肾上腺素在低钾去极化右心房中诱导的缓慢收缩。这些结果表明,与其他β-氨基苯胺类化合物不同,IQB-M-81具有负性变时作用,并且对离体大鼠心房具有Ⅰ类抗心律失常作用。还讨论了其可能的Ⅳ类抗心律失常作用。

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