The derivatives of a novel structure series of dibenzazepines dispose of intense antiarrhythmic properties. The relations between structure and effect in comparison with the antiarrhythmically active derivatives of phenothiazine (Ethmozine) are discussed. When substituting the beta-aminopropionyl chain with cyclic residue by means of a dimethylaminoacyl chain there appears a marked antifibrillatory action besides of the intense antiarrhythmic one.
View Article and Find Full Text PDFAfter an introduction about the importance of the 10, 11-Dihydro-5H-dibenz[b,f]azepine system for the drug research and according to experiences about the change of pharmacodynamic effects in the field of the phenothiazine bases by dialkylaminoacyl substitution in the following report some new 3-carbalkoxyamino-5-omega-aminoacyl-10,11-dihydro-5H-dibenz[b,f]++ +azepines and their intermediates for synthesis are described. In result of pharmacological investigations which showed antiarrhythmic activities the substance 3-carbethoxyamino-5-dimethylaminoacetyl-10,11-Dihydro-5H-dib enz[b, f]azepine X HCl (GS 015, AWD 19-166, Bonnecor) was selected for clinical tests. For studying the biotransformation of this substance the expected main metabolites were prepared by chemical synthesis.
View Article and Find Full Text PDFThe intense antifibrillatory and antiarrhythmic actions of GS 015, a derivative of the novel structure series of the 5-(beta-aminoacyl)-3-carbalkoxyamino-iminodibenzyles, are demonstrated on models of myocardial ischaemia: antifibrillatory action on the acute coronary occlusion in the conscious rat (1.0 mg/kg i.v.
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