Bee D, Emery C J, Howard P
Section of Experimental Medicine, University of Sheffield Medical School.
Exp Physiol. 1992 Nov;77(6):819-28. doi: 10.1113/expphysiol.1992.sp003648.
Chronically hypoxic (CH) and normoxic control rats were used to assess the action of S9581, a water-soluble analogue of almitrine bismesylate. S9581 increased ventilation (Ve) by 34% in control and 20% in CH rats. During acute hypoxia Ve was raised and S9581 caused a further increase of 20% in both groups. Low doses of S9581 and almitrine enhanced the hypoxic ventilatory response in CH rats while high doses depressed it in both groups. Effects of S9581 on the pulmonary circulation were assessed in the isolated perfused lung of rats. As with almitrine a complex relationship of dose-dependent vasoconstriction and dilatation was revealed. In low doses, S9581 enhanced the hypoxic pulmonary vasoconstrictor response to 2% O2 whilst this was attenuated by high doses in both control and CH rats. S9581 seemed to act like almitrine bismesylate on both the ventilation (peripheral chemoreceptor) and the pulmonary circulation. For studying almitrine-like activity the water solubility of S9581 provides considerable advantages for the researcher.
使用慢性低氧（CH）大鼠和常氧对照大鼠来评估甲磺酸阿米三嗪的水溶性类似物S9581的作用。S9581使对照大鼠的通气量（Ve）增加34%，使CH大鼠的通气量增加20%。在急性低氧期间，两组大鼠的Ve均升高，且S9581使其进一步增加20%。低剂量的S9581和阿米三嗪增强了CH大鼠的低氧通气反应，而高剂量则使两组大鼠的该反应受到抑制。在大鼠离体灌注肺中评估了S9581对肺循环的影响。与阿米三嗪一样，发现了剂量依赖性血管收缩和扩张的复杂关系。低剂量时，S9581增强了对2%氧气的低氧肺血管收缩反应，而高剂量时，对照大鼠和CH大鼠的该反应均减弱。S9581在通气（外周化学感受器）和肺循环方面的作用似乎与甲磺酸阿米三嗪相似。对于研究阿米三嗪样活性而言，S9581的水溶性为研究人员提供了相当大的优势。
