RESUMEN

The relationship between the chemical structure and the antiarrhythmic activity of phenothiazine derivatives--ethacizine and its analogues--was estimated quantitatively by the value of the antiarrhythmic effect on aconitine model in conscious rats. The lengthening of the side chain of nitrogen atom in position 10 of phenothiazine cycle by one methylene group as well as the substitution of demethylamine radical for diethylamine one increased the antiarrhythmic activity; the toxicity of the compound being also increased. Ethacizine was found to possess the highest antiarrhythmic activity and the greatest antiarrhythmic index.

Asunto(s)

Antiarrítmicos/farmacología , Fenotiazinas/farmacología , Aconitina , Animales , Antiarrítmicos/química , Antiarrítmicos/uso terapéutico , Arritmias Cardíacas/inducido químicamente , Arritmias Cardíacas/tratamiento farmacológico , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Fenotiazinas/química , Fenotiazinas/uso terapéutico , Ratas , Relación Estructura-Actividad