O'Donnell S R, Wanstall J C
Br J Pharmacol. 1984 Apr;81(4):637-44. doi: 10.1111/j.1476-5381.1984.tb16129.x.
Relaxant responses to the beta-adrenoceptor agonists isoprenaline, fenoterol, noradrenaline or procaterol were obtained on isolated ring preparations of canine coronary arteries contracted with KCl (20 mM) or 5-hydroxytryptamine (3 microM). On left circumflex arterial preparations, Schild plots for the selective antagonists atenolol (beta 1-selective) or ICI 118,551 (beta 2-selective), when using noradrenaline or fenoterol as agonist, were superimposed. This suggested that only one subtype of beta-adrenoceptor was involved in the responses. The pA2 values on left circumflex artery preparations were: atenolol, noradrenaline as agonist 6.98, fenoterol as agonist 6.71; ICI 118, 551, noradrenaline as agonist 6.66, fenoterol as agonist 7.04. These data indicated that the beta-adrenoceptor subtype was beta 1. The relative potencies of isoprenaline: noradrenaline: fenoterol were left circumflex 100: 10.0: 2.3, left ventricular branch 100: 9.7: 2.0, septal branch 100: 10.9: 2.5. These data confirmed that beta 1-adrenoceptors were involved in the responses of all three arterial preparations. On preparations of left circumflex artery, left ventricular branch and septal branch, responses were obtained to high concentrations (1 to 100 microM) but not to low concentrations (0.001 to 0.1 microM) of procaterol. This observation confirmed the absence of beta 2-adrenoceptors in these arteries. Responses of left circumflex artery to isoprenaline were potentiated by the extraneuronal uptake inhibitor drugs, corticosterone and metanephrine. 7 It is concluded (a) that responses of canine left circumflex artery, left ventricular branch and septal branch are mediated by a homogeneous population of beta 1-adrenoceptors, and (b) that modulation of responses to isoprenaline by extraneuronal uptake is not confined to responses mediated by beta 2-adrenoceptors.
在氯化钾(20 mM)或5-羟色胺(3 microM)收缩的犬冠状动脉离体环制备物上,观察到对β-肾上腺素能受体激动剂异丙肾上腺素、非诺特罗、去甲肾上腺素或丙卡特罗的舒张反应。在左旋支动脉制备物上,当使用去甲肾上腺素或非诺特罗作为激动剂时,选择性拮抗剂阿替洛尔(β1选择性)或ICI 118,551(β2选择性)的希尔德图相互重叠。这表明在这些反应中仅涉及一种β-肾上腺素能受体亚型。左旋支动脉制备物上的pA2值为:以去甲肾上腺素为激动剂时阿替洛尔的pA2值为6.98,以非诺特罗为激动剂时为6.71;以去甲肾上腺素为激动剂时ICI 118,551的pA2值为6.66,以非诺特罗为激动剂时为7.04。这些数据表明β-肾上腺素能受体亚型为β1。左旋支、左心室支、间隔支中异丙肾上腺素:去甲肾上腺素:非诺特罗的相对效价分别为100:10.0:2.3、100:9.7:2.0、100:10.9:2.5。这些数据证实β1-肾上腺素能受体参与了所有三种动脉制备物的反应。在左旋支动脉、左心室支和间隔支的制备物上,对高浓度(1至100 microM)但不对低浓度(0.001至0.1 microM)的丙卡特罗有反应。这一观察结果证实了这些动脉中不存在β2-肾上腺素能受体。左旋支动脉对异丙肾上腺素的反应被非神经元摄取抑制剂皮质酮和间甲肾上腺素增强。结论为:(a)犬左旋支动脉、左心室支和间隔支的反应由同质的β1-肾上腺素能受体群体介导;(b)非神经元摄取对异丙肾上腺素反应的调节并不局限于β2-肾上腺素能受体介导的反应。