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尼普地洛对犬缺血性心脏心肌能量代谢的影响。

Effect of nipradilol on myocardial energy metabolism in the dog ischaemic heart.

作者信息

Hayase N, Chiba K, Ichihara K, Inagaki S, Abiko Y

机构信息

Department of Hospital Pharmacy, Asahikawa Medical College, Japan.

出版信息

J Pharm Pharmacol. 1990 Jun;42(6):419-22. doi: 10.1111/j.2042-7158.1990.tb06582.x.

Abstract

The effect of nipradilol, a newly developed beta-adrenoceptor blocking agent with a vasodilatory action, on myocardial energy metabolism has been examined in the dog ischaemic heart, and compared with that of propranolol. Ischaemia was induced by ligating the left anterior descending coronary artery. Either saline, nipradilol (0.3 mg kg-1), or propranolol (1 mg kg-1) was injected intravenously 5 min before coronary ligation. After 3 or 30 min of coronary ligation, the ischaemic region of the myocardium was removed, and the endocardial portion used to determine the levels of adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), creatine phosphate (CrP) and lactate. Ischaemia decreased the levels of ATP and CrP, and increased the levels of ADP, AMP and lactate. Immediately after the injection of nipradilol, rapid falls in blood pressure and heart rate were observed. Pretreatment with nipradilol lessened the decreases in the levels of ATP and CrP and the increases in the levels of AMP and lactate, caused by 3 min of ischaemia, to the same extent as propranolol. However, after 30 min of ischaemia, nipradilol had no effect on myocardial metabolism unlike propranolol. These results indicate that nipradilol can reduce ischaemic influences on myocardial metabolism as well as propranolol, but only in the early stages of ischaemia.

摘要

尼普地洛是一种新开发的具有血管舒张作用的β-肾上腺素受体阻滞剂,本研究在犬缺血性心脏中检测了其对心肌能量代谢的影响,并与普萘洛尔进行了比较。通过结扎左冠状动脉前降支诱导缺血。在冠状动脉结扎前5分钟,静脉注射生理盐水、尼普地洛(0.3mg/kg)或普萘洛尔(1mg/kg)。冠状动脉结扎3或30分钟后,取出心肌缺血区域,取心内膜部分测定三磷酸腺苷(ATP)、二磷酸腺苷(ADP)、一磷酸腺苷(AMP)、磷酸肌酸(CrP)和乳酸的水平。缺血使ATP和CrP水平降低,ADP、AMP和乳酸水平升高。注射尼普地洛后立即观察到血压和心率迅速下降。尼普地洛预处理减轻了3分钟缺血引起的ATP和CrP水平下降以及AMP和乳酸水平升高,其程度与普萘洛尔相同。然而,缺血30分钟后,与普萘洛尔不同,尼普地洛对心肌代谢没有影响。这些结果表明,尼普地洛与普萘洛尔一样,能够减轻缺血对心肌代谢的影响,但仅在缺血早期。

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