Effects of a New Positive Inotropic Agent with a Vasodilatory Action, 5-Methyl-6-(4-pyridyl)-2H-1,4-thiazin-3 (4H)-one (ZSY-27), on Agonists-Induced Contractions in the Isolated Rabbit Thoracic Aorta
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概要
- 論文の詳細を見る
The mechanism of the vasodilatory effect of 5-methyl-6-(4-pyridyl)-2H-1,4-thiazin-3 (4H)-one (ZSY-27), a non-catecholamine and non-glycoside positive inotropic agent with a vasodilatory action, was investigated using helically-cut strips of the rabbit thoracic aorta. The contractile responses of the thoracic aorta to phenylephrine and prostaglandin F_<2α> were antagonized noncompetitively in a concentration-dependent manner by ZSY-27 (1×10^<-4>-1×10^<-3>M). Furthermore, precontractions induced by high K (34.5 mM K) and by phenylephrine (1×10^<-6>M) were relaxed in a concentrationdependent manner by ZSY-27 (1×10^<-6>-1×10^<-3>M). These relaxant effects were not affected by a decrease in extracellular Ca or by pretreatment with methylene blue, an inhibitor of guanylate cyclase, but were significantly potentiated by pretreatment with forskolin, a direct stimulator of adenylate cyclase. Moreover, the amount of Ca stored in smooth muscle cells was estimated from the amplitude of the phasic contractions induced by phenylephrine in Ca-deprived medium. The first phasic contraction induced by phenylephrine was inhibited by pretreatment with ZSY-27. After ZSY-27 was washed out with a Ca-deprived solution, the seconed phasic contraction induced by phenylephrine occurred manifestly, but not in preparations untreated with ZSY-27. It is concluded that ZSY-27 caused a nonspecific relaxation of arterial smooth muscle contractility mainly by acting on some processes distal to adenosine 3', 5'-monophosphate (cAMP) production by adenylate cyclase ; probably inhibition of cAMP-phosphodiesterases.
- 公益社団法人日本薬学会の論文
著者
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TAKAYANAGI Issei
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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Furukawa Akira
Department of Radiology, Shiga University of Medical Science
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HISAYAMA Tetsuhiro
Department of Pharmacology, Faculty of Pharmaceutical Scienses, The University of Tokushima
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Takayanagi Issei
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo:(correspo
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Takayanagi I
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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YOSHIOKA Kimitomo
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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Hisayama T
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Hisayama Tetsuhiro
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Yoshioka K
Research Laboratory Zenyaku Kogyo Co. Ltd.
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Yoshioka Kimitomo
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences:(present Addre
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Furukawa Akira
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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