Antiplatelet Effect of 2-Chioro-3-(4-acetophenyl)-amino-1,4-naphthoquinone(NQ301): A Possible Mechanism through Inhibition of Intracellular Ca〔2+〕 Mobilization
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- ZHANG Yong-He
- College of Pharmacy, Chungbuk National University
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- CHUNG Kwang-Hoe
- Cardiovascular Research Institute, Yonsei University College of Medicine
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- RYU Chung-Kyu
- College of Pharmacy, Ewha Womans University
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- KO Myong-Hwa
- College of Pharmacy, Chungbuk National University
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- LEE Myung-Koo
- College of Pharmacy, Chungbuk National University
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- YUN Yeo-Pyo
- College of Pharmacy, Chungbuk National University
書誌事項
- タイトル別名
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- Antiplatelet Effect of 2-Chloro-3-(4-acetophenyl)-amino-1,4-naphthoquinone (NQ301): A Possible Mechanism through Inhibition of Intracellular Ca2+ Mobilization.
- Antiplatelet Effect of 2 Chioro 3 4 acetophenyl amino 1 4 naphthoquinone NQ301 A Possible Mechanism through Inhibition of Intracellular Ca 2 Mobilization
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抄録
The effects of 2-chloro-3-(4-acetophenyl)-amino-1,4-naphthoquinone (NQ301), an antithrombotic agent, on aggregation, binding of fibrinogen to glycoprotein (GP)Iib/IIIa complex and intracellular signals were investigated using human platelets. NQ301 significantly inhibited the collagen-, thrombin-, arachidonic acid-, thapsigargin- and calcium ionophore A23187-induced aggregation of washed human platelets with IC50 values of 13.0±0.1, 11.2±0.5, 21.0±0.9, 3.8±0.1 and 46.2±0.8 μM, respectively. NQ301 also significantly inhibited FITC-conjugated fibrinogen binding to human platelet surface GPIIb/IIIa complex, but failed to inhibit the fibrinogen binding to purified GPIIb/IIIa complex. These data demonstrate that NQ301 inhibits platelet aggregation by suppression of the intracellular pathway, rather than by direct inhibition of fibrinogen-GPIIb/IIIa complex binding. NQ301 significantly inhibited the increase of cytosolic Ca2+ concentration and ATP secretion, and also significantly increased platelet cAMP levels in the activated platelets. These results suggest that the antiplatelet activity of NQ301 may be mediated by inhibition of cytosolic Ca2+ mobilization, enhancement of cAMP production and inhibition of ATP secretion in activated platelets.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 24 (6), 618-622, 2001
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679603180928
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- NII論文ID
- 110003638526
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- NII書誌ID
- AA10885497
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- COI
- 1:CAS:528:DC%2BD3MXktFygtr4%3D
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 5793276
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- PubMed
- 11411547
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可