Yoshioka K, Takayanagi I, Koike K
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
J Pharmacobiodyn. 1989 Nov;12(11):667-70. doi: 10.1248/bpb1978.12.667.
The effects of 5-methyl-6-(4-pyridyl)-2H-1,4-thiazin-3(4H)-one (ZSY-27), a positive inotropic agent with a vasodilatory action, on a concentration-response curve of CaCl2 in the KCl-depolarized rabbit thoracic aorta and Ca-uptake by the microsomal fraction from the rabbit artery were tested. ZSY-27 (10(-5) - 10(-4) M) inhibited noncompetitively a concentration-response curve of CaCl2 in the KCl-depolarized preparation. Furthermore, ZSY-27 (10(-5) M) stimulated significantly Ca-uptake by the microsomal fraction in the presence of oxalate, as an indicator for Ca-uptake by the internal membrane, in every incubation time. However, it inhibited significantly that in the absence of oxalate, as an indicator for Ca-uptake by the plasma membrane-derived vesicle, after 6 min of incubation time. These results suggest that ZSY-27 stimulates Ca-uptake by the internal membranes and inhibits Ca-uptake by the plasma membrane-derived vesicles. Therefore, these effects of ZSY-27 are considered to be related to relaxation of vascular smooth muscle.
对具有血管舒张作用的正性肌力药5-甲基-6-(4-吡啶基)-2H-1,4-噻嗪-3(4H)-酮（ZSY-27）在氯化钾去极化的兔胸主动脉中对氯化钙浓度-反应曲线以及兔动脉微粒体部分钙摄取的影响进行了测试。ZSY-27（10⁻⁵ - 10⁻⁴ M）非竞争性抑制氯化钾去极化制剂中氯化钙的浓度-反应曲线。此外，作为内膜钙摄取指标，在每个孵育时间，ZSY-27（10⁻⁵ M）在草酸盐存在下显著刺激微粒体部分的钙摄取。然而，作为质膜衍生囊泡钙摄取指标，在孵育6分钟后，它在无草酸盐时显著抑制钙摄取。这些结果表明，ZSY-27刺激内膜的钙摄取并抑制质膜衍生囊泡的钙摄取。因此，ZSY-27的这些作用被认为与血管平滑肌舒张有关。
