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蝙蝠葛碱衍生物的钙拮抗作用

Antagonistic Effects of Several Dauricine Derivatives on Ca ̄(2+)

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【作者】 张虞安李自强胡卓逸米剑菁

【Author】 Zhang Yuan; Li Ziqiang; Hu Zhuoyi;Mi Jianjing(Division of Biochemistry,China Pharmaceutical Uniuersity, Nan jing 210009)

【机构】 中国药科大学生物化学研究室

【摘要】 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。

【Abstract】 With the Verapamil(Ver) and dauricine(Dau)as references,the effects of nine kinds of Dau derivatives inhibiting rabbit thoracic aortic strips in normal Krebs solution were compared.The results indicated that Dau derivatives can shift the dose-response curve of NE,KCl and CaCl2 to the right and depress their maximal responses──showed non-competitive antagonistic manner,and Dau derivatives also inhibited the contractions induced by intracellular Ca2+ and extracel ular Ca2+ after NE administration──were antagonistic reagents of calcium channel.Dau derivative D7,D10,D20 exhibited stronger inhibitions than Dau to contractions induced by(1) NE activating ROC(receptor operated calcium channel);(2)KCl activating PDC(potential dependent calcium channel); (3) release of intracellular Ca2+ after NE. Except for D9,other Dau derivatives showed deeper depressions than Dau to contractions induced by(1) CaCl2 after NE;(2) excelullar Ca2+ after NE.

  • 【文献出处】 中国药科大学学报 ,JOURNAL OF CHINA PHARMACEUTICAL UNIVERSITY , 编辑部邮箱 ,1994年05期
  • 【分类号】R972.2
  • 【被引频次】4
  • 【下载频次】48
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