罂粟碱对豚鼠输尿管电活动和机械活动的影响。
The effects of papaverine on the electrical and mechanical activity of the guinea-pig ureter.
作者信息
Brading A F, Burdyga T V, Scripnyuk Z D
出版信息
J Physiol. 1983 Jan;334:79-89. doi: 10.1113/jphysiol.1983.sp014481.
Abstract
- The effects of papaverine (10(-5)-2 X 10(-4) M) were studied on the evoked electrical and mechanical activity of the guinea-pig ureter smooth muscle. In normal conditions the action potential consists of an initial spike followed by further spikes superimposed on a plateau phase. Papaverine reversibly decreased the duration of the plateau of the action potential, blocked the associated spikes, greatly reduced the amplitude of the contraction but enhanced the initial component of the action potential. 2. Papaverine did not change the membrane potential and had little effect on the membrane resistance. 3. Tetraethylammonium (5 mM), which blocks the delayed outward K current, did not prevent the decrease in the duration of the plateau nor the decrease of the contractile response caused by papaverine. 4. In Na-free solution the duration of the action potential was decreased until only a single spike was seen, due to suppression of the plateau. An effect of papaverine could not be observed under these conditions. 5. Mn2+ ions (1 mM) completely suppressed the spike component and tension while the plateau component was substantially increased. Papaverine in the presence of Mn2+ reversibly blocked the generation of the action potential. When Mn2+ ions were added to Na-free solution the duration as well as the amplitude of the spike was increased. Again, papaverine reversibly blocked the generation of the action potential. 6. Noradrenaline (10(-4) M) and histamine (10(-5) M) in normal conditions prolonged the duration of the action potential plateau and increased both the duration and amplitude of the concentration. Papaverine again blocked the plateau and greatly reduced the contractile response. 7. Papaverine caused the relaxation of KCl-induced contractures, preferentially blocking the tonic component. 8. It is suggested that the inhibitory action of papaverine on ureter smooth muscle results from its specific blockade of the 'slow' Na/Ca channels responsible for the generation of the plateau component of the action potential.
摘要
- 研究了罂粟碱（10⁻⁵ - 2×10⁻⁴M）对豚鼠输尿管平滑肌诱发的电活动和机械活动的影响。在正常情况下，动作电位由一个初始尖峰组成，随后是叠加在平台期上的进一步尖峰。罂粟碱可逆地缩短了动作电位平台期的持续时间，阻断了相关的尖峰，极大地降低了收缩幅度，但增强了动作电位的初始成分。2. 罂粟碱不改变膜电位，对膜电阻影响很小。3. 阻断延迟外向钾电流的四乙铵（5 mM）并不能阻止平台期持续时间的缩短，也不能阻止罂粟碱引起的收缩反应的降低。4. 在无钠溶液中，由于平台期的抑制，动作电位的持续时间缩短，直到只看到一个单一的尖峰。在这些条件下未观察到罂粟碱的作用。5. Mn²⁺离子（1 mM）完全抑制了尖峰成分和张力，而平台成分显著增加。在Mn²⁺存在的情况下，罂粟碱可逆地阻断动作电位的产生。当将Mn²⁺离子加入无钠溶液中时，尖峰的持续时间和幅度都增加了。同样，罂粟碱可逆地阻断动作电位的产生。6. 在正常情况下，去甲肾上腺素（10⁻⁴M）和组胺（10⁻⁵M）延长了动作电位平台期的持续时间，并增加了收缩的持续时间和幅度。罂粟碱再次阻断了平台期，并大大降低了收缩反应。7. 罂粟碱引起氯化钾诱导的挛缩松弛，优先阻断强直成分。8. 提示罂粟碱对输尿管平滑肌的抑制作用是由于其特异性阻断了负责动作电位平台成分产生的“慢”钠/钙通道。
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