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恩屈嗪、肼屈嗪和维拉帕米对人离体动脉和静脉作用的比较。

Comparison of the effects of endrallazine, hydrallazine and verapamil on human isolated arteries and veins.

作者信息

Lipe S, Moulds R F

出版信息

Clin Exp Pharmacol Physiol. 1982 Nov-Dec;9(6):613-20. doi: 10.1111/j.1440-1681.1982.tb00832.x.

Abstract
  1. The antagonist effects of endrallazine (BQ 22-708), hydrallazine and verapamil have been studied on the contractile responses produced by various agonists on human digital arteries and metacarpal veins obtained post mortem. 2. Endrallazine and hydrallazine antagonized the contractile responses to noradrenaline and serotonin in arteries by shifting the concentration-effect curves to the right and by reducing the maximum responses to both agonists. Neither drug had any effect on responses to BaCl2 in either tissue. 3. The same concentrations of endrallazine and hydrallazine which antagonized responses to noradrenaline and serotonin in arteries, had no effect on concentration-effect curves to those agonists in veins. 4. Hydrallazine was significantly more potent than endrallazine in reducing the maximum response to noradrenaline in arteries, and was less potent than endrallazine in reducing the maximum response to serotonin. 5. Verapamil antagonized the vasoconstrictor effect of all agonists tested in both arteries and veins. 6. It is concluded that in a similar manner to hydrallazine, endrallazine has a direct effect on human vascular smooth muscle at concentrations which are probably similar to those occurring in vivo. Both hydrallazine and endrallazine may produce selective arterio-dilatation by preventing the release of bound calcium from intracellular storage sites, an effect which is different to that of verapamil.
摘要
  1. 研究了恩屈嗪(BQ 22 - 708)、肼屈嗪和维拉帕米对各种激动剂在人死后获取的指动脉和掌静脉上产生的收缩反应的拮抗作用。2. 恩屈嗪和肼屈嗪通过将浓度 - 效应曲线右移并降低对两种激动剂的最大反应,拮抗动脉中去甲肾上腺素和5 - 羟色胺的收缩反应。两种药物对两种组织中对氯化钡的反应均无影响。3. 在动脉中拮抗去甲肾上腺素和5 - 羟色胺反应的相同浓度的恩屈嗪和肼屈嗪,对静脉中这些激动剂的浓度 - 效应曲线无影响。4. 在降低动脉中去甲肾上腺素的最大反应方面,肼屈嗪比恩屈嗪显著更有效,而在降低5 - 羟色胺的最大反应方面,肼屈嗪比恩屈嗪效力更低。5. 维拉帕米拮抗在动脉和静脉中测试的所有激动剂的血管收缩作用。6. 得出的结论是,与肼屈嗪类似,恩屈嗪在可能与体内发生的浓度相似的浓度下对人血管平滑肌有直接作用。肼屈嗪和恩屈嗪都可能通过阻止结合钙从细胞内储存部位释放而产生选择性动脉扩张,这一作用与维拉帕米不同。

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