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钙拮抗剂对糖尿病大鼠和年龄匹配的对照大鼠离体主动脉中钾离子诱导收缩的影响。

Effects of calcium antagonists on K(+)-induced contraction in isolated aorta from diabetic and age-matched control rats.

作者信息

Heijnis J B, van Zwieten P A

机构信息

Department of Pharmacotherapy, Academic Medical Center, University of Amsterdam, The Netherlands.

出版信息

Pharmacology. 1993 Apr;46(4):193-7. doi: 10.1159/000139045.

Abstract

The effects of nifedipine, verapamil and diltiazem on K(+)-induced contraction were investigated in isolated aortic rings from diabetic and age-matched control rats. Six weeks after streptozotocin injection there was no significant difference between the maximum isometric contraction to KCl (80 mmol/l), when expressed per milligram tissue weight, in aortic rings from diabetic rats and those from controls. A concentration-dependent inhibition of the K(+)-induced contraction was observed for the three Ca antagonists in aortic rings from both diabetic and age-matched control rats. Notably, the K(+)-induced contraction in aortic preparations from diabetic rats was more sensitive to nifedipine compared to control preparations (pD2: 8.61 vs. 8.31, p < 0.05), while no significant change in sensitivity towards verapamil (pD2: 6.99 vs. 6.92, p > 0.05) or diltiazem (pD2: 6.33 vs. 6.28, p > 0.05) could be demonstrated. Our data indicate a greater interference of nifedipine with voltage-operated channels in diabetic aortas compared with controls. Since a similar antispasmodic activity was found for diltiazem and verapamil it might be specific for dihydropyridine Ca antagonists.

摘要

在糖尿病大鼠和年龄匹配的对照大鼠的离体主动脉环中,研究了硝苯地平、维拉帕米和地尔硫䓬对钾离子诱导收缩的影响。链脲佐菌素注射六周后,按每毫克组织重量计算,糖尿病大鼠主动脉环和对照大鼠主动脉环对氯化钾(80毫摩尔/升)的最大等长收缩之间无显著差异。在糖尿病大鼠和年龄匹配的对照大鼠的主动脉环中,观察到三种钙拮抗剂对钾离子诱导的收缩具有浓度依赖性抑制作用。值得注意的是,与对照制剂相比,糖尿病大鼠主动脉制剂中钾离子诱导的收缩对硝苯地平更敏感(亲和力常数的负对数:8.61对8.31,p<0.05),而对维拉帕米(亲和力常数的负对数:6.99对6.92,p>0.05)或地尔硫䓬(亲和力常数的负对数:6.33对6.28,p>0.05)的敏感性无显著变化。我们的数据表明,与对照相比,硝苯地平对糖尿病主动脉中电压门控通道的干扰更大。由于地尔硫䓬和维拉帕米具有相似的解痉活性,这种作用可能是二氢吡啶类钙拮抗剂所特有的。

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