Takeo S, Daly M J, Tuana B S, Somani P, Dhalla N S
Arzneimittelforschung. 1980;30(9):1511-3.
Effects of dl-erythro-1-phenoxy-3-[(3,4-dimethoxyphenethyl)-amino]-butan-2-ol (PS-6) on ATPase and calcium binding activities of rat heart sarcolemma as well as adenylate cyclase of both sarcolemma and heart washed particles were studied under in vitro conditions. PS-6 at concentrations of 10(-7) mol/l or higher inhibited Na+-K+ ATPase and calcium binding activities significantly. The inhibition of calcium binding activity was dependent upon the concentration of calcium in the incubation medium with greater percentage inhibition seen at lower concentrations. While basal adenylate cyclase activity was not affected by 10(-7)--10(-4) mol/l, isoprenaline stimulated adenylate cyclase activity was inhibited by 10(-6) mol/l or higher concentrations of PS-6. At 10(-3) mol/l PS-6 a more generalized inhibitory effect was seen, with all parameters studied being inhibited. These results suggest that sarcolemma is one of the sites for the cardiac actions of PS-6.
在体外条件下，研究了dl-赤藓醇-1-苯氧基-3-[(3,4-二甲氧基苯乙基)-氨基]-丁-2-醇（PS-6）对大鼠心肌肌膜ATP酶和钙结合活性以及肌膜和心脏洗涤颗粒中腺苷酸环化酶的影响。浓度为10(-7)mol/L或更高的PS-6显著抑制Na+-K+ATP酶和钙结合活性。钙结合活性的抑制取决于孵育介质中钙的浓度，在较低浓度下抑制百分比更高。虽然基础腺苷酸环化酶活性不受10(-7)--10(-4)mol/L的影响，但异丙肾上腺素刺激的腺苷酸环化酶活性受到10(-6)mol/L或更高浓度PS-6的抑制。在10(-3)mol/L的PS-6时，观察到更广泛的抑制作用，所有研究参数均受到抑制。这些结果表明，肌膜是PS-6心脏作用的部位之一。
