The Japanese Journal of Pharmacology | |
Effect of PP1D-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets | |
Feng-Ning Ko1  Chang-Hui Liao1  Sheng-Chu Kuo2  Che-Ming Teng1  | |
[1] Pharmacological Institute, College of Medicine, National Taiwan University;Graduate Institute of Pharmaceutical Chemistry, China Medical College | |
关键词: 2-Chloro-3-methoxycarbonylpropionamido-1; 4-naphthoquinone (PP1D-1); Platelet (rabbit); Inositol 1; 4; 5-trisphosphate (IP3); Intracellular calcium concentration; Thapsigargin; | |
DOI : 10.1254/jjp.76.141 | |
学科分类:药理学 | |
来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society | |
【 摘 要 】
References(28)Cited-By(4)The antiplatelet mechanism of a synthetic compound, 2-chloro-3-methoxycarbonylpropionamido-1, 4-naphthoquinone (PP1D-1), was studied by employing washed rabbit platelets in vitro. PP1D-1 concentration-dependently inhibited thrombin (0.1 U/ml)-, platelet-activating factor (2 ng/ml)-, collagen (10 μg/ml)-, arachidonic acid (100 μM)- and U46619 (1 μM)-induced aggregation and ATP release in washed rabbit platelets. The IC50 values of PP1D-1 for aggregation induced by the above inducers are 17.9±1.7, 9.8±1.1, 3.9±0.4, 1.8±0.3 and 1.7±0.3 μM, respectively. PP1D-1 did not affect platelet thromboxane B2 or prostaglandin D2 formation induced by arachidonic acid, indicating that it did not affect cyclooxygenase and thromboxane synthase activities. PP1D-1 significantly inhibited the formation of inositol 1, 4, 5-trisphosphate caused by these five platelet stimulators. Moreover, PP1D-1 inhibited the increase in intracellular calcium concentration induced by these agents. On the contrary, PP1D-1 did not inhibit thapsigargin-elevated intracellular calcium concentration in indomethacin-pretreated platelets, indicating it did not influence the effect of thapsigargin. According to these data, PP1D-1 exerts antiplatelet effects mainly by inhibiting phosphoinositide turnover.
【 授权许可】
Unknown
【 预 览 】
Files | Size | Format | View |
---|---|---|---|
RO201912080714270ZK.pdf | 949KB | download |