Zamkova A. Neuropharmacological properties of new arylpiperazine derivatives

The dissertation is devoted to the experimental searching for potential drugs with neurotropic action (anxiolytic, The dissertation is devoted to the experimental searching for potential drugs with neurotropic action (anxiolytic, antipsychotic, antidepressive) of 40 new arylpiperazine derivatives with different substituents in arylpiperazine and terminal fragments of molecule. Acute toxicity study has shown, according to Sidorof's classification the compounds investigated may be attributed to the low and moderate toxic compounds. In result of pharmacological study it is shown that naphthalimido(alkyl)piperazine and phenylpiperazinylbarbituric acid derivatives have demonstrated the most high anxiolytic activity. Some of the compounds demonstrate anxiogenic activity. Some of norbornene derivatives in dose 5 mg/kg, demonstrate high anxiolytic activity. In dose 10 mg/kg all of these compounds possessed the strong antipsychotic effect (all compounds in this series, in dose 10 mg/kg remove on 35 - 90 % apomorphine-induced stereotypy) as haloperidol, may be these compounds are ligands of dopamine D2- receptors. The study of phenylpiperazinylbarbituric acid derivatives has shown, that some of them, have anxiolytic, anticonvulsant, sedative and hypnotic properties.