Platelet Anti-aggregant Activity of 2,2-Dimethylthiazolidine Hydrochloride and 2-(4-Hydroxy-3-methoxyphenyl)thiazolidine

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概要

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• The characteristics of platelet anti-aggregant activity of 2,2-dimethylthiazolidine hydrochloride (I) and 2-(4-hydroxy-3-methoxyphenyl)thiazolidin (II) have been evaluated. Compounds I and II were potent inhibitors of collagen- and arachidonic acid-induced aggregation of rat and rabbit platelets (IC_<50> or IC_<100> values : 10^<-5>-10^<-4> M), while they were less effective in the cases of adenosine 5'-diphosphate 2Na, A-23187 and labile aggregation-stimulating substance. Also, both compounds inhibited platelet shape change induced by a low concentation of arachidonic acid. Compounds I (100μM) and II (25μM) significantly inhibited serotonin release and thromboxane B_2 formation induced by arachidonic acid in rabbit platelets. Compound I (100μM) inhibited prostaglandin I_2 formation in rat aorta, but II (100μM) did not. In contrast, neither compound had any effect on platelet adhesiveness. These results strongly suggest that I and II prevented platelet aggregation, shape change and serotonin release reaction via their inhibitory effects on arachidonic acid metabolism of platelets, and the inhibiting potency of II was higher than that of I.

• 社団法人日本薬学会の論文
• 1988-03-25

著者

• 今西 武

  Faculty Of Pharmaceutical Sciences Osaka University

• 田中 徹明

  Faculty of Pharmaceutical Sciences, Osaka University

• 岩田 宙造

  Faculty of Pharmaceutical Sciences, Osaka University

• 千葉 義行

  Central Research Laboratory, Nihon Suisan Kaisha, Ltd.,

• 佐竹 幹雄

  Central Research Laboratory, Nihon Suisan Kaisha, Ltd.,

• 小浜 靖弘

  Faculty of Pharmaceutical Sciences, Osaka University

• 川島 豊

  大正製薬・総合研

• 小宮山 豊

  Faculty Of Pharmaceutical Sciences Osaka University

• 小濱 靖弘

  大阪大学 薬 微薬品化

• 三村 務

  Faculty of Pharmaceutical Sciences, Osaka University

• 三村 務

  大阪大学薬学部

• 田中 徹明

  阪大院薬

• 田中 徹明

  Faculty Of Pharmaceutical Sciences Osaka University

• Tanaka T

  Kvushu Univ. Fukuoka Jpn

• 佐藤 正基

  School Of Pharmaceutical Sciences University Of Shizuoka(present Address):marusa Corporation

• 宮下 和之

  Faculty of Pharmaceutical Sciences, Osaka University

• Tanaka T

  Osaka Univ. Osaka Jpn

• 小浜 靖弘

  大阪大学薬学部

• 岩田 宙造

  Faculty Of Pharmaceutical Sciences Osaka University

• Sato M

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

• 小宮 山豊

  Faculty Of Pharmaceutical Sciences Osaka University

• 桑原 栄樹

  Faculty of Pharmaceutical Sciences, Osaka University

• 山本 浩二

  Faculty of Pharmaceutical Sciences, Osaka University

• 佐竹 幹雄

  日本水産

• 山本 浩二

  Faculty Of Pharmaceutical Sciences Osaka University

• 佐藤 真友美

  Univ. Shizuoka Shizuoka Jpn

• Imamura T

  Faculty Of Pharmaceutical Sciences Osaka University

• 千葉 義行

  Central Research Laboratory Nihon Suisan Kaisha Ltd.

• 宮下 和之

  大阪大学大学院薬学研究科

• 宮下 和之

  Faculty Of Pharmaceutical Sciences Osaka University

• 桑原 栄樹

  Faculty Of Pharmaceutical Sciences Osaka University

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