Bohmer K, Raper C
Clin Exp Pharmacol Physiol. 1977 Jul-Aug;4(4):349-58. doi: 10.1111/j.1440-1681.1977.tb02672.x.
The beta-receptor stimulant effects of Sm220Cl, dl-N-(1,1-dimethyl-3-phenylpropyl)-2-hydroxy-2-(3,4-dihydroxy-2-methoxyphenyl)ethylamine, and (-)-isoprenaline have been compared in isolated atrial (beta1) and tracheal (beta2) preparations from guinea-pigs and cats. 2. The compounds were also tested for their ability to increase the heart rate (beta1), reduce serotonin-induced increases in pulmonary resistance (beta2), and decrease soleus muscle contractility (beta2) in vivo in the two species. 3. In all experiments cumulative concentration or dose-effect curves were established, EC50 or ED50 values obtained and molar activity-ratios (Sm220Cl: (-)-isoprenaline) calculated. 4. Calculated selectivity ratios [activity-ratio (heart):activity-ratio (bronchial smooth muscle)] from the in vitro experiments showed that Sm220Cl possessed beta2-receptor selectivity. This was more marked in guinea-pig than in cat preparations. 5. In the anaesthetized animals this species difference was more apparent; in cats Sm220Cl was non-selective in its actions for beta1- and beta2-receptor mediated responses, while marked beta2-receptor selectivity was obtained in the guinea-pig. 6. Since in both species the activity-ratios for beta2-receptor mediated actions are similar, the differences in the beta1/beta2-receptor selectivity of Sm220Cl are caused by the divergent cardiac effects produced by the drug.
已在豚鼠和猫的离体心房（β1）和气管（β2）标本中比较了Sm220Cl、dl-N-(1,1-二甲基-3-苯基丙基)-2-羟基-2-(3,4-二羟基-2-甲氧基苯基)乙胺和(-)-异丙肾上腺素的β受体激动作用。2. 还测试了这些化合物在这两个物种体内增加心率（β1）、降低5-羟色胺引起的肺阻力增加（β2）以及降低比目鱼肌收缩力（β2）的能力。3. 在所有实验中，均建立了累积浓度或剂量-效应曲线，获得了EC50或ED50值，并计算了摩尔活性比（Sm220Cl: (-)-异丙肾上腺素）。4. 体外实验计算的选择性比率[活性比（心脏）:活性比（支气管平滑肌）]表明，Sm220Cl具有β2受体选择性。在豚鼠标本中比在猫标本中更明显。5. 在麻醉动物中，这种物种差异更明显；在猫中，Sm220Cl对β1和β2受体介导的反应无选择性，而在豚鼠中获得了明显的β2受体选择性。6. 由于在两个物种中β2受体介导作用的活性比相似，Sm220Cl的β1/β2受体选择性差异是由该药物产生的不同心脏效应引起的。
