Tatsuno H, Goto K, Shigenobu K, Kasuya Y
Eur J Pharmacol. 1976 Nov;40(1):145-52. doi: 10.1016/0014-2999(76)90364-2.
The antiarrhythmic activity of a new beta-adrenergic blocking agent, 6-(2-hydroxy-3-isopropylaminopropyloxy)-benzothiazole succinate (KF-577), was compared with that of propranolol. KF-577 antagonized ouabain-induced arrhythmias in normal and bilaterally vagotomized guinea pigs; its antagonistic activity was equal to that of propranolol. Reserpinization greatly reduced ouabain intoxication and neither of the two beta-blockers produced further reduction. Aconitine-induced arrhythmias in rats were not antagonized by the two agents. In intact guinea pigs, the reduction of ouabain intoxication by both beta-blockers could not exceed that produced by simulataneous infusion of KCl, and vice versa. In isolated guinea pig atria, propranolol was about 10 times more effective than KF-577 in reducing the ouabain intoxication. The antiaarhythmic activity of KF-577 paralleled its beta-blocking activity in the isolated preparations but not in the intact animals.
将一种新型β-肾上腺素能阻滞剂6-(2-羟基-3-异丙氨基丙氧基)-苯并噻唑琥珀酸盐（KF-577）的抗心律失常活性与普萘洛尔进行了比较。KF-577可对抗哇巴因诱导的正常和双侧迷走神经切断豚鼠的心律失常；其拮抗活性与普萘洛尔相当。利血平化大大降低了哇巴因中毒，两种β受体阻滞剂均未进一步降低中毒程度。两种药物均未拮抗大鼠乌头碱诱导的心律失常。在完整豚鼠中，两种β受体阻滞剂降低哇巴因中毒的程度均不超过同时输注氯化钾所产生的程度，反之亦然。在离体豚鼠心房中，普萘洛尔在减轻哇巴因中毒方面比KF-577有效约10倍。在离体制剂中，KF-577的抗心律失常活性与其β受体阻滞活性平行，但在完整动物中并非如此。
