Wunderlich H, Stark A, Carstens E, Lohmann D, Grizenko A N, Skoldinov A P
Pharmazie. 1985 Dec;40(12):827-30.
After 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.
在介绍了10,11-二氢-5H-二苯并[b,f]氮杂卓系统对药物研究的重要性之后，并根据吩噻嗪碱领域中通过二烷基氨基酰基取代产生药效学效应变化的经验，在以下报告中描述了一些新的3-烷氧羰基氨基-5-ω-氨基酰基-10,11-二氢-5H-二苯并[b,f]氮杂卓及其合成中间体。药理研究结果显示具有抗心律失常活性，选择了3-乙氧羰基氨基-5-二甲基氨基乙酰基-10,11-二氢-5H-二苯并[b,f]氮杂卓盐酸盐（GS 015，AWD 19-166，Bonnecor）进行临床试验。为了研究该物质的生物转化，通过化学合成制备了预期的主要代谢物。
