Chatelain P, Laruel R, Gillard M
Biochem Biophys Res Commun. 1985 May 31;129(1):148-54. doi: 10.1016/0006-291x(85)91415-9.
In rat-brain synaptic membranes at a fixed temperature (37 degrees C), amiodarone dose-dependently inhibits the Na+/K+ ATPase activity (IC50 approximately equal to 2.10(-5)M) and produces a linear increase in the degree of fluorescence depolarization (P) of 1,6-diphenylhexatriene embedded in the lipid matrix. Amiodarone has no effect on Mg++ ATPase and K+PNPase activity up to 3.10(-4)M. Studies carried out at different temperatures indicate that 10(-5)M amiodarone inhibits the Na+/K+ ATPase and decreases the lipid fluidity at all the temperatures studied (9 - 40 degrees C). The compound significantly displaces the temperature of transition observed around 20 degrees C in both Na+/K+ ATPase activity and lipid fluidity to 24 degrees C with no changes in slopes. The results suggest that part of the selective inhibition of Na+/K+ ATPase activity by amiodarone could be due to the effects of the drug on lipid dynamics.
在固定温度（37摄氏度）下的大鼠脑突触膜中，胺碘酮剂量依赖性地抑制钠钾ATP酶活性（半数抑制浓度约等于2.×10⁻⁵M），并使嵌入脂质基质中的1,6 - 二苯基己三烯的荧光去极化程度（P）呈线性增加。在浓度高达3×10⁻⁴M时，胺碘酮对镁ATP酶和钾PNP酶活性无影响。在不同温度下进行的研究表明，10⁻⁵M胺碘酮在所有研究温度（9 - 40摄氏度）下均抑制钠钾ATP酶并降低脂质流动性。该化合物显著将在20摄氏度左右观察到的钠钾ATP酶活性和脂质流动性的转变温度位移至24摄氏度，斜率无变化。结果表明，胺碘酮对钠钾ATP酶活性的部分选择性抑制可能归因于该药物对脂质动力学的影响。
