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利马前列素是PGE1的类似物,经过结构改造,可延长其半衰期并提高药效。利马前列素口服剂量为100µg/kg,可抑制ADP和胶原诱导的血小板聚集,对大鼠和豚鼠均有效。体外测量显示,作为血小板粘附抑制剂,利马前列素的药效比PGE1高10-1,000倍。麻醉狗冠状动脉内注射(100ng/kg)或静脉注射(3µg/kg)可引起血管舒张,冠状动脉血流量增加60-80%。大鼠口服100和300µg/kg时可见显著的降压作用。Limaprost is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency. Limaprost is orally active in both rats and guinea pigs at doses of 100 µg/kg as an inhibitor of ADP and collagen induced platelet aggregation. Limaprost is 10-1,000 times more potent than PGE1 as an inhibitor of platelet adhesiveness measured in vitro. Intra coronary injection (100 ng/kg) or intravenous injection (3 µg/kg) in anesthetized dogs causes vasodilation and increased coronary blood flow by 60-80%. Significant hypotensive effects were seen at 100 and 300 µg/kg orally in rats.
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Limaprost
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