Benzi G, Gorini A, Ghigini B, Arnaboldi R, Villa R F
Istituto di Farmacologia, Università di Pavia, Italia.
Neurochem Res. 1993 Jun;18(6):719-26. doi: 10.1007/BF00966787.
Energy-using non-mitochondrial ATPases were assayed in rat cerebral cortex synaptosomes and synaptosomal subfractions, namely synaptosomal plasma membranes and synaptic vesicles. The following enzyme activities were evaluated: Na+, K+ -ATPase; high- and low-affinity Ca2+ -ATPase; basal Mg(2+)-ATPase; Ca2+, Mg(2+)-ATPase. The evaluations were performed after four week-treatment with saline [controls] or alpha-adrenergic agents (delta-yohimbine, clonidine), energy-metabolism interfering compound (theniloxazine), and oxygen-partial pressure increasing agent (almitrine), in order to define the plasticity and the selective changes in individual ATPases. In rat cerebral cortex, the enzyme adaptation to four-week-treatment with delta-yohimbine or clonidine was characterized by increase in both high- and low-affinity Ca2+ -ATPase activities. The action involves the enzyme form located in the synaptic plasma membranes. The enzyme adaptation to the subchronic treatments with theniloxazine or almitrine was characterized by increase in Na+, K(+)-ATPase or Mg(2+)-ATPase activities, respectively. The action involves the enzymatic forms located in the synaptic plasma membranes. Thus, the pharmacodynamic effects of the agents tested should also be related to the changes induced in the activity of some specific synaptosomal non-mitochondrial ATPases.
在大鼠大脑皮层突触体和突触体亚组分(即突触体质膜和突触小泡)中检测了耗能的非线粒体ATP酶。评估了以下酶活性:钠钾ATP酶;高亲和力和低亲和力钙ATP酶;基础镁ATP酶;钙镁ATP酶。在用生理盐水[对照组]或α-肾上腺素能药物(δ-育亨宾、可乐定)、能量代谢干扰化合物(替尼洛嗪)和氧分压升高剂(阿米三嗪)进行四周治疗后进行评估,以确定各个ATP酶的可塑性和选择性变化。在大鼠大脑皮层中,用δ-育亨宾或可乐定进行四周治疗后酶的适应性表现为高亲和力和低亲和力钙ATP酶活性均增加。该作用涉及位于突触质膜中的酶形式。用替尼洛嗪或阿米三嗪进行亚慢性治疗后酶的适应性分别表现为钠钾ATP酶或镁ATP酶活性增加。该作用涉及位于突触质膜中的酶形式。因此,所测试药物的药效学效应也应与某些特定突触体非线粒体ATP酶活性的变化有关。