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目的研究原阿片碱对离体兔胸主动脉的松弛作用及其机制。方法应用血管平滑肌等张收缩的方法。结果原阿片碱呈浓度依赖性地松弛去氧肾上腺素和高钾预收缩的离体兔胸主动脉螺旋条,而且对二者的作用强度相当;该药使PE和高钾的量效曲线非平行右移,最大反应压低,呈非竞争性拮抗;在无钙液中,原阿片碱抑制去氧肾上腺素引起的内钙释放和复钙后血管条的收缩,却不影响咖啡因在无钙液中的收缩血管作用。结论原阿片碱不是典型的钙拮抗剂和竞争性α-受体阻断剂;其松弛兔胸主动脉平滑肌的作用与抑制受体中介的钙内流和钙释放有关。
Objective To study the relaxation effect of protopine on isolated rabbit aorta and its mechanism. Methods The method of isometric contraction of vascular smooth muscle was applied. Results The original opioid was in a concentration-dependent relaxation of phenylephrine and potassium precontracted isolated rabbit thoracic aortic spine, and the intensity of the two of the same effect; the drug PE and potassium dose-effect curve is not In the calcium-free solution, protopine inhibited the phenylephrine-induced release of endogenous calcium and the contraction of vascular strips after recalcification, but did not affect caffeine in non-calcium-free Systolic blood vessels in the fluid. CONCLUSION Protopine is not a typical calcium antagonist and competitive α-blocker; its effect on relaxing the smooth muscle of thoracic aorta in rabbits is related to inhibition of calcium influx and calcium influx in receptor mediators.