张炜芳, 支建明, 郭薇, 赵荣瑞, 金国章. 左旋千金藤啶碱对外周血管多巴胺DA1和DA2受体亚型的作用J. 药学学报, 1998, 33(10): 721-726.
引用本文: 张炜芳, 支建明, 郭薇, 赵荣瑞, 金国章. 左旋千金藤啶碱对外周血管多巴胺DA1和DA2受体亚型的作用J. 药学学报, 1998, 33(10): 721-726.
Zhang Weifang, Zhi Jianming, Guo Wei, Zhao Rongrui , Jin Guozhang, . EFFECTS OF l-STEPHOLIDINE ON THE PERIPHERAL VASCULAR DOPAMINE DA1 AND DA2 RECEPTOR SUBTYPESJ. Acta Pharmaceutica Sinica, 1998, 33(10): 721-726.
Citation: Zhang Weifang, Zhi Jianming, Guo Wei, Zhao Rongrui , Jin Guozhang, . EFFECTS OF l-STEPHOLIDINE ON THE PERIPHERAL VASCULAR DOPAMINE DA1 AND DA2 RECEPTOR SUBTYPESJ. Acta Pharmaceutica Sinica, 1998, 33(10): 721-726.

左旋千金藤啶碱对外周血管多巴胺DA1和DA2受体亚型的作用

EFFECTS OF l-STEPHOLIDINE ON THE PERIPHERAL VASCULAR DOPAMINE DA1 AND DA2 RECEPTOR SUBTYPES

  • 摘要: 用家兔离体血管环方法,研究左旋千金藤啶碱(l-SPD)对外周血管DA1和DA2受体亚型的作用。结果表明,l-SPD使DA1受体激动剂FODA诱发的肾、肺和肠动脉以及DA2受体激动剂PBDA诱发的肠和股动脉舒张反应的量效曲线非平行右移,最大反应(Emax)降低,均呈非竞争性拮抗;l-SPD本身还可使肾和肺血管产生轻度的浓度依赖性舒张反应,表现为DA1受体激动剂的作用特性。提示l-SPD为外周血管DA1和DA2受体的混合性阻滞剂并兼有DA1受体部分激动剂的双重作用特性。

     

    Abstract: The effects of l-stepholidine(l-SPD) on peripheral vascular dopamine DA1 and DA2receptors were studied using isolated vascular rings in rabbits. It was shown that (1) l-SPD(0.1~10μmol·L-1) shifted the dose-response curves to the right in a nonparallel fashion and decreased the maximal response (Emax) of both the fenoldopam(FODA,a selective DA1 agonist)-induced and the propyl-buty-dopamine(PBDA, a selective DA2 agonist)-induced vasorelaxation showing a non-competitive antagonistic action. The pD2 values of l-SPD for FODA in the renal, pulmonary and mesenteric arteries were 5.43, 5.48 and 5.58,respectively. The pD2 values for PBDA in the mesenteric and femoral arteries were 5.35 and 5.89,respectively. The potencies of its antagonistic action were comparable to SCH23390, a selective DA1 antagonist, and to domperidone, a selective DA2 antagonist.(2)l-SPD(0.1~100μmol·L-1) per se was also found to induce slight but doserelated vasorelaxations in the renal and pulmonary arteries displaying its DA1 agonistic activity.Its pD2 values were 4.98 and 5.02, respectively. However, its Emax were considerably smaller than that of FODA. These results suggest that l-SPD is a mixed peripheral DA1 and DA2receptor antagonists and weak DA1 receptor agonist with pharmacological property of dual action. 

     

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