抗惊厥药和惊厥药对突触体及其组分ATP酶活性的影响。
Effects of anticonvulsant and convulsant drugs on the ATPase activities of synaptosomes and their components.
作者信息
Gilbert J C, Wyllie M G
出版信息
Br J Pharmacol. 1976 Jan;56(1):49-57. doi: 10.1111/j.1476-5381.1976.tb06958.x.
Abstract
- The effects of anticonvulsants, and other drugs on the Na+, K+-adenosine triphosphatase (ATPase) (ouabain-sensitive) and Mg++-ATPase activities of synaptosomes and their components have been determined. 2. The Mg++-ATPase activity of synaptosomes was not affected by the drugs but the Na+, K+-ATPase activity was inhibited by phenytoin (diphenylhydantoin), ethosuximide and diazepam. 3. Fractions containing mainly membranes, mitochondria or synaptic vesicles, were prepared from synaptosomes by osmotic shock and subsequent density gradient centrifugation. Inhibition of Na+, K+-ATPase activity by phenytoin, ethosuximide and diazepam was apparent only in the membrane fraction. 4. The fraction containing synaptic vesicles exhibited pronounced Md++-ATPase but no Na+, K+-ATPase activity. In contrast to the enzymes of the membranes and mitochondria, the Mg++-ATPase of the vesicles was inhibited by diazepam and all of the anticonvulsants tested.
摘要
- 已测定抗惊厥药及其他药物对突触体及其组分的钠、钾 - 腺苷三磷酸酶（ATP酶）（哇巴因敏感型）和镁离子 - ATP酶活性的影响。2. 突触体的镁离子 - ATP酶活性不受这些药物影响，但钠、钾 - ATP酶活性受到苯妥英（二苯乙内酰脲）、乙琥胺和地西泮的抑制。3. 通过渗透休克及随后的密度梯度离心从突触体中制备主要含膜、线粒体或突触小泡的组分。苯妥英、乙琥胺和地西泮对钠、钾 - ATP酶活性的抑制仅在膜组分中明显。4. 含突触小泡的组分表现出显著的镁离子 - ATP酶活性，但无钠、钾 - ATP酶活性。与膜和线粒体的酶不同，突触小泡的镁离子 - ATP酶受到地西泮及所有 tested 抗惊厥药的抑制。（注：“tested”此处原英文有误，推测可能是“tested”，翻译为“经测试的” ）
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