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标题：Cardiotonic Activity of 5-Methyl-6-(4-pyridyl)-2H-1, 4-thiazin-3 (4H)-one Hydrochloride (ZSY-27)
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作者：Kimitomo YOSHIOKA ; Masataka HINO ; Akira YOSHIMURA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1988
卷号：11
期号：11
页码：715-721
DOI：10.1248/bpb1978.11.715
出版社：The Pharmaceutical Society of Japan
摘要：Cardiotonic activity of a new, non-catecholamine and non-glycoside positive inotropic agent, 5-methyl-6-(4-pyridyl)-2H-1, 4-thiazin-3 (4H)-one hydrochloride (ZSY-27), was investigated in isolated guinea pig left atria, cat right ventricular papillary muscle and cross-circulated excised dog papillary muscle preparations, and in anesthetized open-chest dogs. In electrically driven guinea pig left atria and cat papillary muscle preparations, ZSY-27 (3×10^-6-10^-4M) increased the developed tension in a concentration-related manner. The positive inotropic effect of ZSY-27 was not blocked by propranolol (3×10^-8M) in the guinea pig atria, but was significantly inhibited by carbachol (5×10^-6M) in cat papillary muscle preparations. The positive inotropic effect of ZSY-27 was comparable to that of milrinone in guinea pig atria. ZSY-27 (0.01-3mg) increased dose-dependently the developed tension in cross-circulated excised dog papillary muscle preparations as well. In anesthetized dogs, ZSY-27 (0.03-1 mg/kg, i.v.) produced a dose-dependent increase in left ventricular contractile force and a decrease in blood pressure, while the increase in heart rate was relatively small. The pharmacological profile of ZSY-27 in anesthetized dogs was similar to that of milrinone. These results suggest that ZSY-27 is potent cardiotonic agent with vasodilator activity and its effect may be partially due to an increase in the intracellular adenosine 3', 5'-cyclic monophosphate level.
关键词：cyclic AMP