可乐定在离体大鼠主动脉的双相反应。

Artery Pub Date : 1992-01-01
K K Wong
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引用次数: 0

摘要

可乐定在Wistar大鼠主动脉中作为α肾上腺素受体的部分激动剂已有文献记载。然而,我们观察到可乐定对Sprague Dawley大鼠离体主动脉的影响略有不同。可乐定诱导的浓度效应曲线位于苯肾上腺素诱导的浓度效应曲线的右侧,苯肾上腺素和可乐定诱导的EC50分别为1.5 × 10(-7) M和3.5 × 10(-4) M;但可乐定引起的最大收缩与苯肾上腺素相似。在可乐定存在的情况下,苯肾上腺素的浓度效应曲线向右偏移。哌唑嗪对苯肾上腺素和可乐定诱导的收缩均有抑制作用,哌唑嗪对苯肾上腺素和可乐定诱导的收缩的EC50值分别为1.0 × 10(-8) M和1.8 × 10(-6) M。育亨宾的浓度足以几乎完全对抗苯肾上腺素的作用,发现它能轻微地阻止可乐定的作用。当可乐定浓度进一步增加到2 × 10(-3) M以上时,足以引起最大收缩,但会使可乐定引起的收缩减弱,且这种现象具有浓度依赖性。对这一现象的可能解释进行了讨论。
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Biphasic response of clonidine in isolated rat aortae.

Clonidine as a partial agonist of alpha adrenoceptor in Wistar rat aorta has been documented. It was however observed that the effect of clonidine on the isolated rat aorta of Sprague Dawley rats was slightly different. The concentration effect curve induced by clonidine was on the right of that induced by phenylephrine, with EC50 of 1.5 x 10(-7) M and 3.5 x 10(-4) M for the phenylephrine- and clonidine-induced responses, respectively; but the maximal contraction induced by clonidine was similar to that of phenylephrine. In the presence of clonidine, the concentration effect curve of phenylephrine was shifted to the right. Both the phenylephrine- and clonidine-induced contraction were inhibited by prazosin, and the EC50 values for prazosin in phenylephrine- and clonidine-induced contraction were 1.0 x 10(-8) M and 1.8 x 10(-6) M, respectively. Yohimbine in concentration sufficient to antagonize almost completely the effect of phenylephrine was found to slightly prevent the effects of clonidine. Further increase of clonidine above 2 x 10(-3) M, the concentration sufficient to induce the maximal contraction, however induced depression of the clonidine-induced contraction, and this phenomenon was concentration dependent. Possible explanation of this phenomenon was discussed.

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