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兔静脉中对有机钙通道阻滞剂有抗性的钙通道

Calcium channels resistant to organic calcium entry blockers in a rabbit vein.

作者信息

Winquist R J, Baskin E P

出版信息

Am J Physiol. 1983 Dec;245(6):H1024-30. doi: 10.1152/ajpheart.1983.245.6.H1024.

Abstract

We compared the effects of calcium entry blockers on myogenic tone with the effects of these compounds on agonist- and depolarization-induced mechanical responses in isolated rings of the rabbit facial vein. The development of intrinsic tone in response to distension of the vessel wall and its potentiation by increasing the ambient temperature were antagonized by MnCl2 (0.5 mM) but not verapamil, diltiazem, or nifedipine. Similarly, the contractile response to histamine was blocked by MnCl2 but was unaffected by moderate concentrations of the organic calcium entry blockers. The histamine contractile response elicited at 34 degrees C (a condition which abolishes intrinsic tone) was also refractory to verapamil (10(-6) M). Verapamil, diltiazem, and nifedipine antagonized the contractile response to calcium in depolarized facial vein rings. Thus both extrinsic and intrinsic contractile responses in the rabbit facial vein depend on an extracellular source of calcium. The distension-operated channels are unique in exhibiting a marked temperature sensitivity. However, receptor- and distension-operated calcium channels can be distinguished from the voltage-operated channels in their insensitivity to the organic calcium entry blockers.

摘要

我们比较了钙通道阻滞剂对肌源性张力的影响,以及这些化合物对兔面静脉离体血管环中激动剂诱导和去极化诱导的机械反应的影响。血管壁扩张引起的固有张力的发展及其通过升高环境温度的增强作用被MnCl2(0.5 mM)拮抗,但维拉帕米、地尔硫卓或硝苯地平无此作用。同样,对组胺的收缩反应被MnCl2阻断,但不受中等浓度有机钙通道阻滞剂的影响。在34摄氏度(消除固有张力的条件)下引发的组胺收缩反应对维拉帕米(10^-6 M)也无反应。维拉帕米、地尔硫卓和硝苯地平拮抗去极化面静脉环中对钙的收缩反应。因此,兔面静脉中的外在和内在收缩反应均依赖于细胞外钙源。牵张激活通道的独特之处在于表现出明显的温度敏感性。然而,受体激活和牵张激活的钙通道在对有机钙通道阻滞剂不敏感方面可与电压激活通道区分开来。

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