【摘要】 ①在猪离体冠状动脉环上比较了莱马卡林和吡那地尔的作用,结果表明:二药对20mmol/L KCl 所致的血管收缩均有明显抑制作用,但莱马卡林的作用较强。②在同一标本上,莱马卡林与吡那地尔均可使高钾去极化标本的CaCl₂量效曲线右移,最大反应压低,其PD′₂值分别为5.93和5.25,莱马卡林的作用比吡那地尔强4倍。③在去或未去内皮的大鼠离体动脉环上,莱马卡林和吡那地尔对去甲肾上腺素所致的收缩均有明显松弛作用,且这种作用为非内皮依赖性。以上结果提示二药对一些血管内皮受损的疾病可能有独特的治疗意义。更多还原

【Abstract】 Lemakalim and pinacidil were studied for their ability to relax blood vessels. It was found that; 1) Lemakalim and pinacidil caused near maximal relaxant response of pre constricted pig circumflex coronary artery ring with 20 mmol/L KC1. 2) In the same sample Lemakalim and pinacidil, concentration-dependently, inhibited CaCl2-induced contraction, producing a shift of the dose-response curve both rightwards and downwards, indicating a non-competitive aatagonism. Their PD2’ values were 5. 93 (Lemakalim) and 5. 25 (Pinacidil) respectively. The vasolaxant response of lemakalim was approximately more than 4-fold that of pinacidil. 3) In the rat aortic ring with or without endothelium, Limakalim and pinacidil produced an inhibition of tension development induced by opening a type of K+ channel. However, Limakalim was more potent as a vasorelaxant than pinacidil.更多还原