Mennini T, Ceci A, Caccia S, Garattini S, Masturzo P, Salmona M
FEBS Lett. 1984 Jul 23;173(1):255-8. doi: 10.1016/0014-5793(84)81058-3.
Diazepam in vitro produced a concentration-dependent increase of membrane fluidity in crude synaptic membranes from rat hippocampus, but not cerebellum. Similar effects were obtained with higher concentrations of Ro 15-1788 and PK 11195, while zopiclone was completely inactive. In vivo acute treatment with diazepam and Ro 15-1788 gave results similar to those in vitro. The specific benzodiazepine antagonist also significantly increased membrane fluidity and was not able to reverse diazepam's effect. The data are discussed in terms of a possible role of protein kinase inhibition by the drugs not mediated by the 'central' or 'peripheral' type of benzodiazepine receptors.
地西泮在体外可使大鼠海马而非小脑的粗制突触膜中的膜流动性呈浓度依赖性增加。较高浓度的Ro 15 - 1788和PK 11195也有类似效果,而佐匹克隆则完全无活性。地西泮和Ro 15 - 1788的体内急性治疗结果与体外相似。特异性苯二氮䓬拮抗剂也显著增加膜流动性,且无法逆转地西泮的作用。从药物对蛋白激酶的抑制作用(并非由“中枢”或“外周”型苯二氮䓬受体介导)的可能作用方面对这些数据进行了讨论。