Dzurba A, Vrbjar N, Breier A, Ziegelhöffer A
Institute for Heart Research, Slovak Academy of Sciences, Bratislava, Slovakia.
Gen Physiol Biophys. 1996 Feb;15(1):71-5.
The effect of Benfluron on the heart sarcolemmal (Na+, K+)-ATPase and Mg(2+)-ATPase activities was studied in crude membrane fraction as well as in purified sarcolemmal membranes isolated from rat heart. Benfluron in concentration range 10(-7) -5 x 10(-5) mol.l-1 did not exert any effect on ATPase activities studied. 10(-4) mol.l-1 Benfluron was stimulatory towards (Na+, K+)-ATPase, while Mg(2+)-ATPase activity was depressed. Kinetic analysis of interaction of Benfluron with (Na+, K+)-ATPase revealed an increase in the Vmax and decrease in the K(m) values for ATP. The possible mechanism of interaction of the drug with (Na+, K+)-ATPase is discussed.
研究了苯氟隆对大鼠心脏粗膜组分以及从大鼠心脏分离得到的纯化肌膜中肌膜（Na⁺，K⁺）-ATP酶和Mg²⁺-ATP酶活性的影响。浓度范围为10⁻⁷ - 5×10⁻⁵ mol·L⁻¹的苯氟隆对所研究的ATP酶活性没有任何影响。10⁻⁴ mol·L⁻¹的苯氟隆对（Na⁺，K⁺）-ATP酶有刺激作用，而Mg²⁺-ATP酶活性则受到抑制。对苯氟隆与（Na⁺，K⁺）-ATP酶相互作用的动力学分析表明，ATP的Vmax增加而Km值降低。讨论了该药物与（Na⁺，K⁺）-ATP酶相互作用的可能机制。
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