Neurotropic activity of phenylpyrrolidone-2 isomers

Abstract

Pyrrolidone-2 (P 2) is a cyclic form of gamma-aminobutyric acid (GABA). In experiments on mice and rats the pharmacological activity of three isomers of phenyl derivatives of P 2 was investigated. All the compounds inhibited motor activity, lowered muscle tone and body temperature, potentiated the action of hexobarbital, and possessed anticonvulsive (electrical shock, strychnine, metrazol, thiosemicarbazide, audiogenic convulsions) and narcotic activity. The most active isomer was 4-phenylpyrrolidone-2 (phepyron). Comparison of the pharmacological activity of phenyl derivatives of P 2 and analogous derivatives of GABA showed that the GABA derivatives have no anticonvulsive or narcotic activity and are less toxic. It is suggested that the phenyl derivatives of P 2 are not converted into the analogous GABA derivatives in vivo.