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尼莫地平对血小板聚集及花生四烯酸代谢中酶活性的影响。

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

作者信息

Li J, Wang Z

机构信息

Institute of Basic Medical Sciences, CAMS, Beijing.

出版信息

Proc Chin Acad Med Sci Peking Union Med Coll. 1990;5(1):47-50.

PMID:2115166
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.

摘要

为探讨尼莫地平对血栓形成或心血管疾病患者的影响,研究了其对血小板聚集和花生四烯酸(AA)代谢的作用。结果表明,尼莫地平(50 - 350μmol/L)以剂量依赖性方式显著抑制由二磷酸腺苷(ADP)、AA和离子载体A23187诱导的血小板聚集。离子载体A23187诱导的抑制作用可被钙(1 mmol/L)部分拮抗。当底物为AA且酶由猪肺微粒体提供时,尼莫地平(50 - 400μmol/L)同时显著降低血栓素B2(TXB2)和6 - 酮 - 前列腺素F1α(6 - keto - PGF1α)的生成。然而,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 - keto - PGF1α的水平无显著变化。结果提示,尼莫地平是一种环氧化酶抑制剂,其抑制血小板聚集的能力与其钙阻滞作用有关。

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