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佛波酯(PMA)可激活大鼠主动脉螺旋条而非环状条中的电压依赖性钙通道。

Phorbol ester (PMA) activates voltage-dependent Ca(2+)-channels in helical but not ring preparation of the rat aorta.

作者信息

Suenaga H, Kamata K, Kasuya Y

机构信息

Department of Pharmacology, Upjohn Research Laboratories, Ibaraki, Japan.

出版信息

Res Commun Chem Pathol Pharmacol. 1993 Aug;81(2):167-81.

PMID:8210696
Abstract

Effects of phorbol 12-myristate 13-acetate (PMA) on the helical and ring preparations from rat thoracic aorta was investigated in the present study. In helical strips, PMA produced biphasic contraction, i.e., sustained contraction followed by a phasic response superimposed on the sustained contraction. The phasic contraction was completely inhibited by removal of external Ca2+, whereas sustained contraction was not affected by the treatment. In the ring preparation, PMA produced only sustained contraction, whereas phasic contraction was not induced. On the other hand, in the ring preparation which had been treated with 15 mM K+, PMA was able to produce phasic contraction. Contractile response of the aorta to norepinephrine (NE) or clonidine in the ring preparations was significantly weaker than that in the helical strips. In the presence of nifedipine, however, these different sensitivity to NE between ring and helical preparations was not shown. These results suggest that an activation of C-kinase by PMA is able to stimulate voltage-dependent Ca(2+)-channels in the helical strips but not ring preparation of the aorta. An increased contractile response of the aorta to agonists in helical strips may be responsible for an increased activities of voltage-dependent Ca(2+)-channels.

摘要

本研究调查了佛波醇12 -肉豆蔻酸酯13 -乙酸酯(PMA)对大鼠胸主动脉螺旋条和环行条的影响。在螺旋条中,PMA产生双相收缩,即持续收缩后叠加一个时相性反应于持续收缩之上。去除细胞外Ca2+可完全抑制时相性收缩,而持续收缩不受该处理影响。在环行条制备中,PMA仅产生持续收缩,而不诱导时相性收缩。另一方面,在用15 mM K+处理过的环行条制备中,PMA能够产生时相性收缩。主动脉对去甲肾上腺素(NE)或可乐定在环行条制备中的收缩反应明显弱于在螺旋条中的反应。然而,在硝苯地平存在的情况下,环行条和螺旋条对NE的这种不同敏感性未表现出来。这些结果表明,PMA对C激酶的激活能够刺激螺旋条中电压依赖性Ca(2+)通道,但不能刺激主动脉环行条中的该通道。螺旋条中主动脉对激动剂收缩反应的增加可能是电压依赖性Ca(2+)通道活性增加的原因。

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