Herzig J W, Feile K, Rüegg J C
Arzneimittelforschung. 1981;31(1a):188-91.
2-[(2-Methoxy-4-methylsulfinyl)phenyl]-1H-imidazo[4,5-b]pyridine (AR-L 115 BS), a new positive inotropic substance, is shown to have direct activating effects upon the Ca2+ sensitive force, stiffness and unloaded shortening velocity of membrane-free, detergent-treated myocardial fibres. At pCa 6.2, application of 7--350 mumol/l AR-L 115 BS (concentrations which are also effective in living papillary muscle) led to a 30-50% increase in force and stiffness and even more in Vmax. A possible intracellular action of the drug on the contractile structures directly is discussed in comparison with the known influences of c-AMP dependent phosphorylation of myocardial regulatory proteins.
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）是一种新型正性肌力物质，已证明它对无膜、经去污剂处理的心肌纤维的钙敏感性张力、硬度和无负荷缩短速度具有直接激活作用。在pCa 6.2时，应用7 - 350 μmol/l AR-L 115 BS（这些浓度在活体乳头肌中也有效）可使张力和硬度增加30 - 50%，Vmax增加更多。与心肌调节蛋白的c-AMP依赖性磷酸化的已知影响相比，讨论了该药物可能直接对收缩结构产生的细胞内作用。
