Effect of PP1D-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets

スポンサーリンク

概要

• 論文の詳細を見る

• 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.

• 社団法人 日本薬理学会の論文

著者

• KUO Sheng-Chu

  Graduate Institute of Pharmaceutical Chemistry, College of Pharmacy, China Medical University

• Teng Che-ming

  Pharmacological Institute College Of Medicine National Taiwan University

• Kuo Sheng-chu

  Graduate Institute Of Pharmaceutical Chemistry China Medical College

• LIAO Chang-Hui

  Pharmacological Institute, College of Medicine, National Taiwan University

• KO Feng-Ning

  Pharmacological Institute, College of Medicine, National Taiwan University

• Liao Chang-hui

  Pharmacological Institute College Of Medicine National Taiwan University

• Ko Feng-ning

  Pharmacological Institute College Of Medicine National Taiwan University

• Kuo Sheng-Chu

  Graduate Institute of Pharmaceutical Chemistry, China Medical College

関連論文

• The synthesized 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one (CHM-1) promoted G2/M arrest through inhibition of CDK1 and induced apoptosis through the mitochondrial-dependent pathway in CT-26 murine colorectal adenocarcinoma cells
• Synthesis and Antiplatelet, Antiinflammatory and Antiallergic Activities of 2,3-Disubstituted 1,4-Naphthoquinones
• Synthesis of 2-Alkoxy 1,4-Naphthoquinone Derivatives as Antiplatelet, Antiinflammatory, and Antiallergic Agents
• Synthesis and Evaluation of Coumarin α-Methylene-γ-butyrolactones : A New Class of Platelet Aggregation Inhibitors
• Antiplatelet Effect and Selective Binding to Cyclooxygenase by Molecular Docking Analysis of 3-Alkylaminopropoxy-9,10-anthraquinone Derivatives(Medicinal Chemistry)
• α-Methylene-γ-butyrolactones : Synthesis and Vasorelaxing Activity Assay of Coumarin, Naphthalene, and Quinoline Derivatives
• Synthesis and Antiplatelet Evaluation of α-Methylene-γ-butyrolactone Bearing 2-Methylquinoline and 8-Hydroxyquinoline Moieties
• Synthesis and Anti-platelet, Anti-inflammatory and Anti-allergic Activities of Methoxyisoflavanquinone and Related Compounds
• Effect of PP1D-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets
• The Inhibitory Mechanism of YC-1, a Benzyl Indazole, on Smooth Muscle Cell Proliferation : an In Vitro and In Vivo Study
• Ca2+-Channel Blockade in Rat Thoracic Aorta by Protopine Isolated from Corydalis Tubers.

もっと見る 閉じる

スポンサーリンク