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人胆囊动脉的血管活性反应:肾上腺素能受体特性

Vasoactive responses of a human cystic artery: adrenoceptor characterization.

作者信息

Wyse D G

机构信息

Department of Medicine, Cardiology, University of Calgary, Alberta, Canada.

出版信息

Br J Clin Pharmacol. 1988 Jun;25(6):741-9. doi: 10.1111/j.1365-2125.1988.tb05261.x.

Abstract
  1. The pharmacology of various agonists and antagonists was studied in the human isolated cystic artery. 2. The estimated pA2s for the alpha 1-adrenoceptor antagonist prazosin against the alpha-adrenoceptor agonists phenylephrine, alpha-methylnoradrenaline and noradrenaline were not significantly different. Similar results were seen for estimated pA2s of the alpha 2-adrenoceptor antagonist yohimbine against these same agonists. Equivalent responses to exogenous noradrenaline and to transmural electrical stimulation were blocked to the same degree by an antagonist with alpha 1-adrenoceptor blocking properties (prazosin). Responses to transmural electrical stimulation, however, tended to be more resistant than equivalent responses to exogenous noradrenaline to blockade by antagonists with alpha 2-adrenoceptor blocking properties (phentolamine, yohimbine). 3. Relaxation to isoprenaline was observed in partially contracted arterial strips using isoprenaline concentrations of up to 10(-6) M, but cumulative addition of higher concentrations of isoprenaline sometimes then evoked a contraction from the relaxation nadir. The relaxation effect of isoprenaline was antagonized by propranolol (10(-5) M). 4. These findings suggest the human cystic artery has almost exclusively alpha 1-adrenoceptors postjunctionally, although prejunctional alpha 2-adrenoceptors may be present; and, it also has some postjunctional beta-adrenoceptors which mediate relaxation.
摘要
  1. 在人离体胆囊动脉中研究了各种激动剂和拮抗剂的药理学特性。2. α1肾上腺素能受体拮抗剂哌唑嗪对α肾上腺素能激动剂去氧肾上腺素、α-甲基去甲肾上腺素和去甲肾上腺素的估计pA2值无显著差异。α2肾上腺素能受体拮抗剂育亨宾对这些相同激动剂的估计pA2值也得到了类似结果。具有α1肾上腺素能阻断特性的拮抗剂(哌唑嗪)对外源性去甲肾上腺素和经壁电刺激的等效反应具有相同程度的阻断作用。然而,与对外源性去甲肾上腺素的等效反应相比,经壁电刺激的反应对外具有α2肾上腺素能阻断特性的拮抗剂(酚妥拉明、育亨宾)的阻断作用往往更具抗性。3. 在部分收缩的动脉条中,使用高达10(-6) M的异丙肾上腺素浓度可观察到对异丙肾上腺素的舒张反应,但累积添加更高浓度的异丙肾上腺素有时会从舒张最低点诱发收缩。异丙肾上腺素的舒张作用被普萘洛尔(10(-5) M)拮抗。4. 这些发现表明,人胆囊动脉在节后几乎只具有α1肾上腺素能受体,尽管节前可能存在α2肾上腺素能受体;并且,它还具有一些介导舒张作用的节后β肾上腺素能受体。

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