Rozhanets V V, Kozlova V P, Rodina R I, Shvets V I, Glebov R N
Biokhimiia. 1978 May;43(5):892-8.
The distribution pattern of marker enzymes (Na, K-ATPase, acetylcholinesterase) in three fractions of synaptic membranes (SM) of rat brain were studied. The effects of three anticonvulsive agents on Na, K-ATPase from the total fraction of rat brain SM and purified membrane preparation from ox brain were estimated by different methods. Under optimal conditions (Na/K = 5) diphenylhydantoin (DPH) at a concentration of 0,1 mM activates Na, K-ATPase from the total SM fraction only in the absence of ouabain, whereas carbamazepine and pyrroxane taken at the same concentrations have no effect on Na, K-ATPase, irrespective of the type of the enzyme assay. DPH seems to compete with ouabain. Under non-optimal ionic conditions (Na/K = 250) all the anticonvulsive substances studied inhibit Na, K-ATPase of the total SM fraction. The mixture of hydrophobic agents (propylene glycol and ethanol) used to dissolve carbamazepine inhibits Na, K-ATPase from the total SM fraction only under non-optimal conditions. The inhibiting effect of the anticonvulsive substances under study on Na, K-ATPase from the purified membrane preparations is maximal at the concentration of 10(-6) M; at higher concentrations the effect is less pronounced.
研究了大鼠脑突触膜(SM)三个组分中标记酶(钠钾ATP酶、乙酰胆碱酯酶)的分布模式。通过不同方法评估了三种抗惊厥药物对大鼠脑SM总组分以及牛脑纯化膜制剂中钠钾ATP酶的影响。在最佳条件下(钠/钾 = 5),浓度为0.1 mM的苯妥英(DPH)仅在不存在哇巴因的情况下激活SM总组分中的钠钾ATP酶,而相同浓度的卡马西平和吡罗昔康对钠钾ATP酶没有影响,无论酶测定类型如何。DPH似乎与哇巴因竞争。在非最佳离子条件下(钠/钾 = 250),所有研究的抗惊厥物质均抑制SM总组分中的钠钾ATP酶。用于溶解卡马西平的疏水试剂混合物(丙二醇和乙醇)仅在非最佳条件下抑制SM总组分中的钠钾ATP酶。所研究的抗惊厥物质对纯化膜制剂中钠钾ATP酶的抑制作用在浓度为10^(-6) M时最大;在更高浓度下,作用不太明显。