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美西拉酮的血管和心肌效应。

Vascular and myocardial effects of mecinarone.

作者信息

Pourrias B, Friedrich F

出版信息

Eur J Pharmacol. 1978 Jun 1;49(3):203-11. doi: 10.1016/0014-2999(78)90095-x.

Abstract

The effects of mecinarone on the contractions induced by noradrenaline, potassium and calcium were studied with the isolated aorta and central artery of the rabbit ear. In our experimental conditions mecinarone was found to act as a competitive antagonist of calcium. It preferentially inhibited the noradrenaline-evoked contraction induced in the rabbit ear artery and had a smaller effect on the extracellular calcium-induced contraction of depolarized arterial smooth muscle. In the isolated guinea pig heart, mecinarone produced a reversible decrease in the rate of rise of the ascendant phase of the action potential without significantly changing the resting potential. In hearts inactivated by depolarisation, mecinarone inhibited the contractions restored by isoproterenol without suppressing the calcium action potential. These results suggest that the mode of action of mecinarone is different from that of verapamil or nifedipine but is comparable to that of chlorpromazine, although mecinarone has no sedative effect.

摘要

用兔耳离体主动脉和中央动脉研究了美西律对去甲肾上腺素、钾和钙诱导的收缩的影响。在我们的实验条件下,发现美西律可作为钙的竞争性拮抗剂。它优先抑制兔耳动脉中去甲肾上腺素诱发的收缩,而对去极化动脉平滑肌的细胞外钙诱导收缩的作用较小。在离体豚鼠心脏中,美西律使动作电位上升相的上升速率可逆性降低,而静息电位无明显改变。在因去极化而失活的心脏中,美西律抑制异丙肾上腺素恢复的收缩,而不抑制钙动作电位。这些结果表明,美西律的作用方式不同于维拉帕米或硝苯地平,但与氯丙嗪相当,尽管美西律没有镇静作用。

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