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比较了蝙蝠葛碱(Dau)及其衍生物对离体兔胸主动脉条收缩的影响,与维拉帕米(Ver)对照表明,这些衍生物都非竞争性拮抗NE,KCl和CaCl2所致动脉条收缩,能抑制外钙内流及内钙释放引起的收缩,表明这些衍生物为钙通道阻滞剂。其中衍生物D7,D10,D20抑制NE激活ROC、KCl激活PDC、NE激发胞内钙释放引起的收缩,其作用较Dau为强。除D9外,其余8个衍生物对NE去极化后CaCl2引起的收缩及NE致胞外钙内流引起的收缩较Dau有更强的抑制作用。
The effects of Dau and its derivatives on contractility of isolated thoracic aortic strips were compared with those of verapamil (Ver), indicating that these derivatives are noncompetitively antagonistic to NE, KCl and CaCl2 Arterial contraction, can inhibit the influx of calcium and calcium release caused by contraction, indicating that these derivatives as calcium channel blockers. Derivatives D7, D10 and D20 could inhibit NE-activated ROC, KCl-activated PDC, and NE-induced intracellular calcium release-induced contractions, which were stronger than Dau. Except for D9, the other 8 derivatives showed a more potent inhibitory effect on the contractions induced by CaCl2 and NE induced extracellular calcium influx.