한국식품위생안전성학회지 (Journal of Food Hygiene and Safety)

  • 제19권3호
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  • Pages.161-166
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  • 2004
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  • 1229-1153(pISSN)
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  • 2465-9223(eISSN)
한국식품위생안전성학회 (The Korean Society of Food Hygiene and Safety)
권호 표지

Antiplatelet Activity of KR-32558, a Novel Selective Sodium/hydrogen Exchanger-1 Inhibitor

  • Lee, Mi-Yea (College of Social Sciences, Cheongju University) ;
  • Yun, Yeo-Pyo (College of Pharmacy, Chungbuk National University)
  • 발행 : 2004.09.01
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초록

We investigated the antiplatelet effect of a newly synthesized guanidine derivative KR-32558, a sodium-hydrogen exchanger-1 (NHE-1) inhibitor, together with the elucidation of the possible mechanisms of action. KR-32558 concentration -dependently inhibited the aggregation of washed rabbit platelets induced by collagen (10 ${\mu}g/ml$) with an $IC_{50}$ value of 85.9 ${\mu}M$, but with much weaker potency against aggregation induced by thapsigargin (0.5 ${\mu}M$) or A23187 (5 ${\mu}M$). And had no effect on platelet aggregation induced by arachidonic acid (100 ${\mu}M$), thrombin (0.05 U/ml) and U46619 (1 ${\mu}M$) up to 100 ${\mu}M$. KR-32558 completely inhibited the $[Ca^{2+}]_i$ mobilization induced by collagen at concentration of 100${\mu}iM$. Taken together, these observation suggest that KR-32558 selectively inhibited collagen-mediated platelet aggregation by blocking the cytoplasmic calcium mobilization in addition to NHE-1 inhibition.

키워드

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