ABSTRACT
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.
Subject(s)
Adrenergic alpha-Antagonists/chemical synthesis , Dioxanes/chemical synthesis , Dioxins/chemical synthesis , Isoquinolines/chemical synthesis , Adrenergic alpha-Antagonists/pharmacology , Animals , Aorta, Thoracic/drug effects , Chemical Phenomena , Chemistry , Dioxanes/pharmacology , Epinephrine/pharmacology , Guinea Pigs , Humans , In Vitro Techniques , Isoquinolines/pharmacology , Male , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Muscle, Smooth, Vascular/drug effects , Norepinephrine/pharmacology , Platelet Aggregation/drug effects , Rabbits , Vas Deferens/drug effectsABSTRACT
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.
