Battistini B, Filep J G, Cragoe E J, Fournier A, Sirois P
Department of Pharmacology, Faculty of Medicine, University of Sherbrooke, (PQ), Canada.
Biochem Biophys Res Commun. 1991 Mar 15;175(2):583-8. doi: 10.1016/0006-291x(91)91605-c.
Endothelin-1-induced contractions of guinea pig tracheal and bronchial strips were dose-dependently attenuated by the amiloride analogues 5-(N-ethyl-N-isopropyl)amiloride (EIPA, 1-10 microM) and 5-(N,N-hexamethylene)amiloride (HMA, 1-10 microM). The calculated Ki values for EIPA and HMA were 0.11 +/- 0.02 microM and 0.06 +/- 0.02 microM in the trachea, and 0.28 +/- 0.11 microM and 0.70 +/- 0.25 microM in the bronchus, respectively. These values are in the same order of magnitude as those reported for inhibition of the Na+/H+ exchange in cells. Amiloride (1-10 microM) was ineffective. These data suggest that activation of the Na+/H+ exchange by ET-1 may be involved in mediating its myotropic action in guinea pig airway smooth muscle.
内皮素-1诱导的豚鼠气管和支气管条收缩，被氨氯地平类似物5-(N-乙基-N-异丙基)氨氯地平（EIPA，1 - 10微摩尔）和5-(N,N-六亚甲基)氨氯地平（HMA，1 - 10微摩尔）剂量依赖性地减弱。在气管中，EIPA和HMA的计算Ki值分别为0.11±0.02微摩尔和0.06±0.02微摩尔；在支气管中，分别为0.28±0.11微摩尔和0.70±0.25微摩尔。这些值与报道的细胞中Na+/H+交换抑制值处于同一数量级。氨氯地平（1 - 10微摩尔）无效。这些数据表明，ET-1激活Na+/H+交换可能参与介导其在豚鼠气道平滑肌中的肌otropic作用。 （注：“myotropic”这个词可能有误，推测可能是“myotrophic”，“营养性肌的”，但按照原文翻译为“肌otropic”）
