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Antiplatelet Activity of KR-32558, a Novel Selective Sodium/hydrogen Exchanger-1 Inhibitor
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  • Antiplatelet Activity of KR-32558, a Novel Selective Sodium/hydrogen Exchanger-1 Inhibitor
  • Antiplatelet Activity of KR-32558, a Novel Selective Sodium/hydrogen Exchanger-1 Inhibitor
저자명
Lee. Mi-Yea,Yun. Yeo-Pyo
간행물명
한국식품위생안전성학회지
권/호정보
2004년|19권 3호|pp.161-166 (6 pages)
발행정보
한국식품위생안전성학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

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.