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目的:研究抗高血压新药盐酸埃他卡林对大、小动脉舒张作用的药理学特性。方法:采用大鼠主动脉离体血管环和尾动脉血管条两种组织,对比观察盐酸埃他卡林对大、小动脉舒张作用的药理学特性,并且利用膜片钳技术观察盐酸埃他卡林对大鼠尾动脉平滑肌细胞钾电流的影响。结果:盐酸埃他卡林在1×10-7～1×10-3mol/L范围内对氯化钾预致收缩的大鼠尾动脉血管条产生剂量依赖性舒张反应,而对主动脉离体血管环却无明显的舒张反应,该作用能被ATP敏感性钾通道特异性拮抗剂格列苯脲阻断,并且能显著增强大鼠尾动脉平滑肌细胞的钾电流。结论:盐酸埃他卡林具有选择性舒张小动脉作用,具有ATP敏感性钾通道开放剂的主要药理学特征。
Objective: To study the pharmacological properties of antihypertensive drug iptakalim on diastolic function of large and small arteries. Methods: The isolated rat aortic vascular rings and caudal artery vascular strips of two organizations were compared and observed the pharmacological properties of vasodilatory effects of iptakalim hydrochloride on the large and small arteries, and the use of patch-clamp technique to observe the etanercept hydrochloride Effect of Lin on Potassium Currents in Rat Tail Artery Smooth Muscle Cells. Results: In the range of 1 × 10-7 ~ 1 × 10-3mol / L, iptakalim hydrochloride produced a dose-dependent relaxation response to rat tail artery strips pre-contracted by potassium chloride, However, there was no obvious relaxation response of vascular rings, which could be blocked by glibenclamide, an ATP-sensitive potassium channel antagonist, and could significantly increase the potassium current of rat tail artery smooth muscle cells. Conclusion: Iptakalim hydrochloride has a selective diastolic arteriole effect and possesses the main pharmacological properties of ATP-sensitive potassium channel openers.