Effects of nimodipine on platelet aggregation and the activity of enzymes in arachidonic acid metabolism.

J Li, Z Wang
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Abstract

The effects of nimodipine on platelet aggregation and arachidonic acid (AA) metabolism were studied in order to explore its effect on patients with thrombosis or cardiovascular disease. The results indicate that nimodipine (50-350 mumol/L) significantly inhibits platelet aggregation induced by ADP, AA, and ionophore A23187 in a dose dependent manner. The inhibitory effects induced by ionophore A23187 could be partially antagonized by calcium (1 mmol/L). When the substrate was AA and the enzyme was supplied by pig lung microsomes, nimodipine (50-400 mumol/L) significantly reduced the generation of TXB2 and 6-keto-PGF 1 a in parallel. When the substrate was prostaglandin endoperoxide, however, the levels of TXB2 and 6-keto-PGF 1 a were not significantly altered in the same concentration range. The results suggest that nimodipine is a cyclooxygenase inhibitor, and its ability to inhibit platelet aggregation is related to its calcium blocking effect.

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尼莫地平对血小板聚集及花生四烯酸代谢酶活性的影响。
研究尼莫地平对血小板聚集和花生四烯酸(AA)代谢的影响,探讨其对血栓形成或心血管疾病患者的影响。结果表明,尼莫地平(50 ~ 350 μ mol/L)显著抑制ADP、AA和离子载体A23187诱导的血小板聚集,且呈剂量依赖性。1 mmol/L钙可部分拮抗离子载体A23187的抑制作用。当底物为AA,酶由猪肺微粒体供给时,尼莫地平(50-400 mumol/L)可显著降低TXB2和6-keto-PGF - 1a的生成。而当底物为前列腺素内过氧化物时,在相同浓度范围内,TXB2和6-酮- pgf - 1a的水平没有显著变化。结果提示尼莫地平是一种环加氧酶抑制剂,其抑制血小板聚集的能力与其钙阻断作用有关。
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