Deliconstantinos G
Neurochem Res. 1983 Sep;8(9):1143-52. doi: 10.1007/BF00964928.
The binding of [14C]phenobarbital into synaptosomal plasma membranes of dog brain follows a sigmoid path. The "best fit" curve of this binding is the one described by the Hill equation (r2 less than 0.93 and Hill coefficient, n = 1.32). (Na+, K+)-stimulated ATPase and Ca2+-stimulated ATPase activities are modulated by phenobarbital. Arrhenius plots of (Na+, K+, Mg2+)-dependent ATPase revealed that phenobarbital (2 mM) lowered the transition temperature and altered the Arrhenius activation energies of this enzyme. The allosteric inhibition by F- of the (Na+, K+)-stimulated ATPase was studied in control and phenobarbital-treated membranes. The lowering of the transition temperature and changes in Arrhenius activation energy about the transition temperature in combination with changes observed in the allosteric properties of the (Na+, K+)-stimulated ATPase by F-, produced by phenobarbital, would be expected if it is assumed that phenobarbital "fluidizes" synaptosomal plasma membranes.
[14C]苯巴比妥与犬脑突触体细胞膜的结合呈S形曲线。这种结合的“最佳拟合”曲线是由希尔方程描述的曲线(r2小于0.93,希尔系数n = 1.32)。苯巴比妥可调节(Na +,K +)刺激的ATP酶和Ca2 +刺激的ATP酶活性。(Na +,K +,Mg2 +)依赖性ATP酶的阿伦尼乌斯曲线表明,苯巴比妥(2 mM)降低了转变温度并改变了该酶的阿伦尼乌斯活化能。在对照和苯巴比妥处理的膜中研究了F-对(Na +,K +)刺激的ATP酶的变构抑制作用。如果假设苯巴比妥使突触体细胞膜“流化”,则预期苯巴比妥会降低转变温度,并改变转变温度附近的阿伦尼乌斯活化能,同时结合F-对(Na +,K +)刺激的ATP酶变构性质的观察变化。