[Pharmacological characteristics of the silyl derivatives of alpha-pyrrolidone]

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.