Hino T, Sakai K, Ichihara K, Abiko Y
Department of Pharmacology, Asahikawa Medical College, Japan.
Pharmacol Toxicol. 1989 Apr;64(4):324-8. doi: 10.1111/j.1600-0773.1989.tb00657.x.
In dogs anaesthetized with pentobarbital, the left anterior descending coronary artery (LAD) was occluded for 90 min. so that about 1/2 of the original flow was allowed to flow (partial occlusion). Bevantolol (a beta 1-adrenoceptor antagonist) or propranolol (a reference drug) was injected intravenously 30 min. after partial occlusion. Regional myocardial pH was measured by a micro glass pH electrode inserted in the LAD area. Partial occlusion decreased myocardial pH by 0.62 to 0.74. Bevantolol (1.0 mg/kg) or propranolol (1.0 mg/kg) significantly increased myocardial pH, that had been decreased by partial occlusion, within 60 min. after the injection. Restoration of myocardial [H+] (defined as return towards a lower [H+] to the preocclusion level) (calculated from the pH data) induced by bevantolol and that induced by propranolol were 64.0 and 66.4% (measured 60 min. after the injection), respectively. Bevantolol or propranolol decreased heart rate also. Even in the paced heart, bevantolol restored the myocardial [H+] that had been increased by partial occlusion. These results suggest that bevantolol has a favorable effect on the ischaemic myocardium as has propranolol, and that the pH effect of bevantolol is not primarily due to a decrease in heart rate.
在用戊巴比妥麻醉的犬中,将左冠状动脉前降支(LAD)闭塞90分钟,使血流量维持在原来的约1/2(部分闭塞)。部分闭塞30分钟后静脉注射贝凡洛尔(一种β1肾上腺素能受体拮抗剂)或普萘洛尔(一种对照药物)。通过插入LAD区域的微型玻璃pH电极测量局部心肌pH值。部分闭塞使心肌pH值降低0.62至0.74。注射后60分钟内,贝凡洛尔(1.0mg/kg)或普萘洛尔(1.0mg/kg)可使因部分闭塞而降低的心肌pH值显著升高。由贝凡洛尔和普萘洛尔诱导的心肌[H+]恢复(定义为朝着较低的[H+]恢复到闭塞前水平)(根据pH数据计算)分别为64.0%和66.4%(注射后60分钟测量)。贝凡洛尔或普萘洛尔也可降低心率。即使在起搏心脏中,贝凡洛尔也能使因部分闭塞而升高的心肌[H+]恢复正常。这些结果表明,贝凡洛尔与普萘洛尔一样,对缺血心肌有有益作用,且贝凡洛尔的pH效应并非主要归因于心率降低。