Brazier M, Lefebvre C, Robert H, Reynaud P, Nguyen-Tri-Xuong E, Arnould-Guérin M L, Pieri F
Laboratoire de Pharmacie Galénique et Biopharmacie, Faculté de Pharmacie, Amiens.
Farmaco. 1990 Dec;45(12):1351-9.
Several compounds derived from benzamidines and nicotinic pyridinic amidines with a structure similar to that of procainamide, exhibit notable antiarrhythmic properties after injection into animals. The diffusion rate of these different compounds through a solid lipidic artificial membrane was studied with Dibbern's apparatus. A statistical relation was established between the diffusion rate and the principal pharmacological parameters obtained after intraperitoneal injection (toxicity and anthiarrhythmic activity). Essential structural elements seem to determine a better bioavailability than procainamide: character of the substitution (in para) of the benzenic cycle; length of the lateral chain.
几种结构与普鲁卡因酰胺相似的苯甲脒和烟碱吡啶酰胺衍生物，在注入动物体内后表现出显著的抗心律失常特性。使用迪伯恩仪器研究了这些不同化合物通过固体脂质人工膜的扩散速率。建立了扩散速率与腹腔注射后获得的主要药理学参数（毒性和抗心律失常活性）之间的统计关系。基本结构元素似乎决定了比普鲁卡因酰胺更好的生物利用度：苯环对位取代的特征；侧链长度。
