Chiba S, Furukawa Y, Saegusa K, Ogiwara Y
Jpn Heart J. 1986 Sep;27(5):749-57. doi: 10.1536/ihj.27.749.
A new cardiotonic compound, 5-methyl-6-(4-pyridinyl)-2H-1,4-thiazine-3(4H)-one X hydrochloride (ZSY-27), was investigated in cross-circulated dog atrial muscle preparations. When ZSY-27 was intravenously administered to the donor dog, a dose-dependent depressor effect with slight sinus tachycardia was induced in the donor dog. At the same time, a significant dose-dependent increase in developed tension was usually observed in an isolated atrium perfused with donor's arterial blood, but there were no significant changes in sinus cycle length and sinoatrial conduction time. The ZSY-27-induced positive inotropic effect was not significantly influenced by treatment with propranolol in doses which completely inhibited norepinephrine-induced positive chronotropic and inotropic effects. When ZSY-27 was injected into the cannulated sinus node artery of the isolated atrium, dose dependent positive chronotropic and inotropic effects were induced. The dominant increases in developed tension by ZSY-27 were similar to effects of other phosphodiesterase inhibitors, such as papaverine and aminophylline. From these results, it is concluded that ZSY-27 has non-adrenergic, cardiotonic properties with a depressor effect.
一种新型强心化合物,5-甲基-6-(4-吡啶基)-2H-1,4-噻嗪-3(4H)-酮X盐酸盐(ZSY-27),在交叉循环犬心房肌制备物中进行了研究。当向供体犬静脉注射ZSY-27时,供体犬出现剂量依赖性降压作用并伴有轻微窦性心动过速。同时,在用供体动脉血灌注的离体心房中,通常观察到明显的剂量依赖性张力增加,但窦性周期长度和窦房传导时间无明显变化。完全抑制去甲肾上腺素诱导的正性变时和变力作用的普萘洛尔剂量,对ZSY-27诱导的正性肌力作用无显著影响。当将ZSY-27注入离体心房的插管窦房结动脉时,可诱导剂量依赖性的正性变时和变力作用。ZSY-27引起的张力增加主要与其他磷酸二酯酶抑制剂如罂粟碱和氨茶碱的作用相似。从这些结果可以得出结论,ZSY-27具有非肾上腺素能的强心特性并伴有降压作用。