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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Celiprolol induces β3-adrenoceptors-dependent relaxation in isolated porcine coronary arteries
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Celiprolol induces β3-adrenoceptors-dependent relaxation in isolated porcine coronary arteries

机译：头孢洛尔在分离的猪冠状动脉中诱导β3-肾上腺素受体依赖性舒张

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摘要

In porcine coronary arteries (PCAs), celiprolol, a selective β1-adrenoceptors antagonist, induces vasodilatation by an endothelium- and nitric oxide (NO)-dependent pathway. However, the mechanisms of that vascular effect have not been precisely established. β3-Adrenoceptors have been shown to be involved in the relaxation per se of various vascular beds, including coronary vessels. Thus, we evaluated (i) the presence of β3-adrenoceptors in the PCA and (ii) their role in celiprolol induced vasodilatation. PCA rings were placed in organ baths and preconstricted with KCl. All experiments were performed in the presence of nadolol (a β1/β2-adrenoceptor antagonist). Cumulative concentration-response curves to SR 58611A and ICI 215001 (2 β3-adrenoceptor agonists) and to celiprolol were constructed. We also used semiquantitative reverse transcription -polymerase chain reaction, which clearly showed the presence of β3-adrenoceptor transcripts. SR 58611A, ICI 215001, and celiprolol induced concentration-dependent relaxations in PCA rings. SR 58611A-induced relaxation was almost abolished after removal of endothelium or pretreatment with L-NAME (a NO synthase inhibitor). The vasorelaxations induced by SR 58611A and celiprolol were inhibited in the presence of SR 59230A and L-748337 (2 selective β3-adrenoceptor antagonists). We showed (i) that PCAs possess functional β3-adrenoceptors mediating endothelium- and NO-dependent relaxation, and (ii) that celiprolol exerts a β3-adrenoceptor agonistic activity in this vascular bed.
机译：在猪冠状动脉（PCA）中，头孢洛尔是一种选择性的β1肾上腺素受体拮抗剂，可通过内皮和一氧化氮（NO）依赖性途径诱导血管舒张。但是，尚未确切地确定这种血管作用的机制。已经证明β3-肾上腺素能受体参与包括冠状血管在内的各种血管床本身的松弛。因此，我们评估了（i）PCA中存在β3-肾上腺素能受体，以及（ii）它们在头孢洛尔诱导的血管舒张中的作用。将PCA环放在器官浴中，并预先用KCl收缩。所有实验均在纳多洛尔（一种β1/β2-肾上腺素受体拮抗剂）的存在下进行。构建了对SR 58611A和ICI 215001（2种β3-肾上腺素受体激动剂）和对西酞洛尔的累积浓度-响应曲线。我们还使用了半定量逆转录-聚合酶链反应，该反应清楚地表明了β3-肾上腺素能受体转录物的存在。 SR 58611A，ICI 215001和西酞洛尔在PCA环中诱导了浓度依赖性的弛豫。去除内皮或使用L-NAME（NO合酶抑制剂）预处理后，SR 58611A引起的松弛几乎被消除。在SR 59230A和L-748337（2种选择性β3-肾上腺素受体拮抗剂）的存在下，SR 58611A和头孢洛尔诱导的血管舒张受到抑制。我们显示（i）PCA具有介导内皮依赖性和NO依赖性松弛的功能性β3-肾上腺素能受体，以及（ii）头孢洛尔在该血管床中发挥β3肾上腺素受体激动活性。

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