RESUMEN
Effects of the analogs of transmitter amino acids on the level of biogenic amines and their metabolism in various structures of brain and on the life span of rats have been studied.
Asunto(s)
Asparagina/farmacología , Aminas Biogénicas/metabolismo , Encéfalo , Glicinérgicos/farmacología , Glicina/farmacología , Longevidad/efectos de los fármacos , Animales , Asparagina/análogos & derivados , Encéfalo/citología , Encéfalo/metabolismo , Química Encefálica/efectos de los fármacos , Glicina/análogos & derivados , Masculino , RatasRESUMEN
In continuation of the study of pharmacological properties of the new drug VMA-99-82 (9-[2-(4-isopropylphenoxy)ethyl]adenine), the influence of this drug on the psycho-emotional status of rats was evaluated using a voluntary alcoholization model. It is established that VMA-99-82 administered at doses of 10 and 50 mg/kg produces a positive effect on impaired cognitive functions in alcoholized rats and eliminated the depression caused by the consumption of excess ethanol.
Asunto(s)
Adenina/análogos & derivados , Adenina/farmacología , Cognición/efectos de los fármacos , Depresión/tratamiento farmacológico , Alcohólicos , Animales , Depresión/inducido químicamente , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Masculino , RatasRESUMEN
The psychotropic activity of a series of new aminouracil derivatives was studied on the widely applied models of pharmacological screening in rats. The most expressed antidepressant effect at the stage of primary pharmacological screening was been revealed for compound PIR-03-52 in a dose of 10 mg/kg. A profound study of the antidepressant activity on models of pathological states, PIR-03-52 exhibited a pronounced antidepressant effect that was comparable with that of a reference drug (imipramine). The given effect is related to the positive influence of PIR-03-52 on the serotoninergic and dopaminergic systems.
Asunto(s)
Antidepresivos/farmacología , Piridinas/farmacología , Uracilo/análogos & derivados , Animales , Antidepresivos/química , Depresión/tratamiento farmacológico , Depresión/etiología , Depresión/psicología , Femenino , Masculino , Actividad Motora/efectos de los fármacos , Piridinas/química , Ratas , Estrés Psicológico/complicaciones , Estrés Psicológico/tratamiento farmacológico , Relación Estructura-Actividad , Uracilo/química , Uracilo/farmacologíaRESUMEN
We have studied the influence of the new adenine derivative VMA-99-82 on the exchange of monoamines and their metabolites in the brain of Wistar rats. In addition, the effect of VMA-99-82 on binding of 5-HT1A and 5-HT2A serotonin receptors and the system of 3H-serotonin reuptake in the brain synaptosomes has been studied in vitro. It is established that VMA-99-82 at a dose of 10 mg/kg has no affinity to 5-HT1A and 5-HT2A serotonin receptors and produces no effect on the reuptake of [3H]-5-HT. It is suggested that VMA-99-82 has a modulating effect on ion channel NMDA receptor complex of the glutamatergic system, which leads to the manifestation of antidepressant activity.
