Dahmen M, Greeff K
Arzneimittelforschung. 1981;31(1a):161-5.
When comparing the positive-inotropic effect of 2-[(2-methoxy-4-methylsulfinyl)phenyl]-1H-imidazo[4,5-b]pyridine (AR-L 115 BS) on the isolated guinea pig atria with those of theophylline, orciprenaline and strophanthin G, the following results were obtained: 1. In left atria the maximum effective concentration of AR-L 115 BS is 3.16 x 10(-4), of theophylline 10(-3), of strophanthin G 6.81 x 10(-7) and of orciprenaline 10(-5) mol/l. The increase in the contractile force thereby obtained was 192, 111, 158 and 277%, respectively (extracellular calcium concentration 1.2 mmol/l). Therefore AR-L 115 BS is somewhat less effective than orciprenaline but more effective than theophylline and strophanthin G. 2. AR-L 115 BS is also effective in atria isolated from animals pretreated with reserpine and its effect is not reduced in the presence of bupranolol. 3. Contrary to strophanthin G, AR-L 115 BS has a shorter time of onset of activity and is less dependent on the extracellular calcium concentration. 4. Similar to theophylline, AR-L 115 BS inhibits the positive-inotropic effect of orciprenaline dose-dependently, while strophanthin G increases the positive-inotropic effect of orciprenaline. 5. The effect of AR-L 115 BS differs from that of orciprenaline in having only little effect on the contraction rate in isolated right atrial preparations.
将2-[(2-甲氧基-4-甲基亚磺酰基)苯基]-1H-咪唑并[4,5-b]吡啶（AR-L 115 BS）对离体豚鼠心房的正性肌力作用与茶碱、奥西那林和毒毛花苷G的正性肌力作用进行比较时，得到以下结果：1. 在左心房中，AR-L 115 BS的最大有效浓度为3.16×10⁻⁴，茶碱为10⁻³，毒毛花苷G为6.81×10⁻⁷，奥西那林为10⁻⁵mol/L。由此获得的收缩力增加分别为192%、111%、158%和277%（细胞外钙浓度为1.2 mmol/L）。因此，AR-L 115 BS的效果略低于奥西那林，但高于茶碱和毒毛花苷G。2. AR-L 115 BS对用利血平预处理的动物分离出的心房也有效，并且在存在布普萘洛尔的情况下其效果不会降低。3. 与毒毛花苷G相反，AR-L 115 BS的起效时间较短，并且对细胞外钙浓度的依赖性较小。4. 与茶碱类似，AR-L 115 BS剂量依赖性地抑制奥西那林的正性肌力作用，而毒毛花苷G则增强奥西那林的正性肌力作用。5. AR-L 115 BS的作用与奥西那林不同，对离体右心房标本的收缩速率影响很小。
