RESUMO
The synthesis of the title compounds starting from 2-Chlormethylbenzdioxan and Tetrahydroisochinolines is presented. Their actions on the platelet aggregation and the inhibition of alpha-adrenoceptors at the isolated rabbit aorta and the vas deferens of the guinea pig were investigated.
Assuntos
Antagonistas Adrenérgicos alfa/síntese química , Dioxanos/síntese química , Dioxinas/síntese química , Isoquinolinas/síntese química , Antagonistas Adrenérgicos alfa/farmacologia , Animais , Aorta Torácica/efeitos dos fármacos , Fenômenos Químicos , Química , Dioxanos/farmacologia , Epinefrina/farmacologia , Cobaias , Humanos , Técnicas In Vitro , Isoquinolinas/farmacologia , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Norepinefrina/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Coelhos , Ducto Deferente/efeitos dos fármacosRESUMO
Propranolol is a well-known powerful betareceptor-blocking agent. Its quaternary dimethyl derivative, designated as pranolium was firstly prepared by Lucchesi. Compared to propranolol it possesses no betareceptor-blocking activity and no local anaesthetic properties but shows the same antiarrhythmic action as the starting material. The synthesis of pranolium and its optical isomers starting from the corresponding propranolol derivatives is described. Their pharmacological activities have been tested. No significant differences regarding the pharmacological action could be observed.