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幼年和老年大鼠肺动脉和主动脉制剂中β-1和β-2肾上腺素能受体介导的反应。

Beta-1 and beta-2 adrenoceptor-mediated responses in preparations of pulmonary artery and aorta from young and aged rats.

作者信息

O'Donnell S R, Wanstall J C

出版信息

J Pharmacol Exp Ther. 1984 Mar;228(3):733-8.

PMID:6323680
Abstract

Rat pulmonary artery contains both alpha adrenoceptors mediating contraction and beta-1 and beta-2 adrenoceptors mediating relaxation. Neither alpha nor beta adrenoceptor-mediated responses of this vessel to norepinephrine or epinephrine were potentiated by cocaine, despite evidence for the presence of some adrenergic nerves. Beta adrenoceptor-mediated relaxation of pulmonary artery, but not aorta, modulated alpha adrenoceptor-mediated contractions to epinephrine but not norepinephrine. Rat aorta also contains both beta-1 and beta-2 adrenoceptors mediating relaxation, in that Schild plots for atenolol (beta-1 selective antagonist) using a beta-1 selective agonist (norepinephrine) and a beta-2 selective agonist (fenoterol), respectively, were not superimposed. The Schild plot data for lCl 118,551 (beta-2 selective) indicated that the minor population (beta-1) was less important in aorta than in pulmonary artery. On preparations from 18-month-old rats, the maximum relaxation to isoproterenol (20.4%, aorta and 67.9%, pulmonary artery) was less than in preparations from young rats (79.8%, aorta and 96.9%, pulmonary artery), i.e., aging had reduced the beta adrenoceptor-mediated relaxation in both vessels, but particularly in aorta. Also, the negative log EC50 of fenoterol, but not of isoproterenol or norepinephrine, was less than in preparations from young rats. This could indicate that aging had affected beta-2 more than beta-1 adrenoceptor-mediated responses and may explain why aging depressed the maximum relaxation of aorta more than that of pulmonary artery.

摘要

大鼠肺动脉同时含有介导收缩的α肾上腺素能受体以及介导舒张的β-1和β-2肾上腺素能受体。尽管有证据表明存在一些肾上腺素能神经,但该血管对去甲肾上腺素或肾上腺素的α和β肾上腺素能受体介导的反应均未被可卡因增强。β肾上腺素能受体介导的肺动脉舒张(而非主动脉舒张)可调节α肾上腺素能受体介导的对肾上腺素而非去甲肾上腺素的收缩反应。大鼠主动脉也含有介导舒张的β-1和β-2肾上腺素能受体,因为分别使用β-1选择性激动剂(去甲肾上腺素)和β-2选择性激动剂(非诺特罗)绘制的阿替洛尔(β-1选择性拮抗剂)的希尔德图并不重叠。lCl 118,551(β-2选择性)的希尔德图数据表明,在主动脉中,次要群体(β-1)的重要性低于肺动脉。在18月龄大鼠的制备物上,对异丙肾上腺素的最大舒张反应(主动脉为20.4%,肺动脉为67.9%)低于年轻大鼠制备物(主动脉为79.8%,肺动脉为96.9%),即衰老降低了这两种血管中β肾上腺素能受体介导的舒张反应,但在主动脉中尤为明显。此外,非诺特罗的负对数EC50(而非异丙肾上腺素或去甲肾上腺素的)低于年轻大鼠制备物。这可能表明衰老对β-2肾上腺素能受体介导的反应的影响大于对β-1的影响,并且可以解释为什么衰老对主动脉最大舒张的抑制作用大于肺动脉。

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