Hashimoto K, Tsukada T, Matsuda H, Nakagawa Y, Imai S
J Cardiovasc Pharmacol. 1979 Mar-Apr;1(2):205-17. doi: 10.1097/00005344-197903000-00004.
We compared the beta-adrenoceptor blocking actions of bupuranolol and propranolol using the response to isoprenaline of the strength of contraction of the canine blood-perfused ventricular muscle, of the rate and strength of contraction of the isolated guinea pig heart and of a guinea pig tracheal ring preparation. The potency ratios of bupuranolol to propranolol were 3.6, 3.0, 3.4, and 2.4, respectively. Bupuranolol decreased the maximum dV/dt of the canine ventricular action potential and had no sympathomimetic action. Bupuranolol effectively suppressed halothane-adrenaline ventricular arrhythmias in the dog, reflecting its potency as a beta-adrenoceptor antagonist. In contrast, bupuranolol did not suppress ventricular arrhythmias induced by two-stage coronary ligation in the dog. Compared to propranolol and certain other antiarrhythmic drugs, bupuranolol had weaker effects on prolonging the effective refractory period than on the maximum dV/dt of canine ventricular muscle. This suggests that lengthening of the refractory period may be important for suppressing the two-stage coronary ligation arrhythmia and that the mechanism of this arrhythmia might be reentry.
我们利用犬血液灌注心室肌收缩强度对异丙肾上腺素的反应、离体豚鼠心脏的收缩速率和强度以及豚鼠气管环标本,比较了布普洛尔和普萘洛尔的β-肾上腺素受体阻断作用。布普洛尔与普萘洛尔的效价比分别为3.6、3.0、3.4和2.4。布普洛尔降低了犬心室动作电位的最大dV/dt,且无拟交感神经作用。布普洛尔有效抑制了犬的氟烷-肾上腺素性室性心律失常,反映了其作为β-肾上腺素受体拮抗剂的效力。相比之下,布普洛尔不能抑制犬两期冠状动脉结扎诱导的室性心律失常。与普萘洛尔和某些其他抗心律失常药物相比,布普洛尔延长有效不应期的作用比降低犬心室肌最大dV/dt的作用弱。这表明延长不应期可能对抑制两期冠状动脉结扎心律失常很重要,并且这种心律失常的机制可能是折返。