[Pharmacological characteristics of the silyl derivatives of alpha-pyrrolidone]. / Farmakologicheskaia kharakteristika silil'nykh proizvodnykh al'fa-pirrolidona.

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.

[Dopaminergic component in the mechanism of action of gamma-aminobutyric acid derivatives and structural analogs]. / Dofaminergicheskii komponent v mekhanizme deistviia proizvodnykh i strukturnykh analogov gamma-aminomaslianoi kisloty.

In experiments on rats and male mice the GABA derivatives fenibut, fepiron and the organosilicon compound N-methyl (3-trimethylsilil)pyrrolidone (IA) antagonized apomorphine sterotypy and aggressiveness. Fenibut and IA potentiated haloperidol catalepsy. Fenibut, fepiron, sodium hydroxybutyrate and IA also antagonized the effects of phenamine. The biochemical investigations have shown that fenibut and IA produce acceleration of the intraneuronal synthesis and catabolism of DA. It is suggested that the behavioral effects of the GABA derivatives are partly relative to inhibition of the dopamin--ergic system.