Tsareva T A, Kramarova E P, Zharkovskiĭ A M
Farmakol Toksikol. 1982 Jul-Aug;45(4):20-3.
It was shown in experiments on mice that the silil derivatives of alpha-pyrrolidone, I-methyl (3-trimethylsilil) pyrrolidone-2 (1A) and 1-vinyl(3 trimethylsilil) pyrrolidone-2 (2A) in doses of 6.25-25 mg/kg exert a tranquilizing effect on emotional behavior of the animals in conflict situation and decrease shock-induced emotional reactions. At the same time IA activates the orienting response and locomotor activity of mice. In the doses that exert the tranquilizing effect the compounds under test increased the content of GABA and speeded up dopamine metabolism in the rat anterior brain. The starting products of the synthesis, 1-methylpyrrolidone-2 and trimethylsilanol given in the test doses produced no tranquilizing effect on the animals' emotional behavior and neuromediator turnover in the brain. It is suggested that the appearance of marked pharmacological activity of the silil derivatives of alpha-pyrrolidone-2 is related to a better penetration of these substances via the hematoencephalic barrier and to their effect on GABA- and dopaminergic processes in the central nervous system.
在对小鼠的实验中表明，α-吡咯烷酮的硅烷基衍生物，即1-甲基（3-三甲基硅烷基）吡咯烷酮-2（1A）和1-乙烯基（3-三甲基硅烷基）吡咯烷酮-2（2A），剂量为6.25 - 25毫克/千克时，对处于冲突情境下动物的情绪行为具有镇静作用，并可减少电击诱发的情绪反应。同时，1A激活小鼠的定向反应和运动活动。在发挥镇静作用的剂量下，受试化合物增加了大鼠前脑γ-氨基丁酸（GABA）的含量并加速了多巴胺代谢。合成的起始产物，即测试剂量下的1-甲基吡咯烷酮-2和三甲基硅烷醇，对动物的情绪行为和脑中神经递质周转没有产生镇静作用。有人认为，α-吡咯烷酮-2的硅烷基衍生物显著药理活性的出现与这些物质通过血脑屏障的更好渗透及其对中枢神经系统中GABA和多巴胺能过程的影响有关。
