Hoefle M L, Blouin L T, Fleming R W, Hastings S, Hinkley J M, Mertz T E, Steffe T J, Stratton C S, Werbel L M
Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.
J Med Chem. 1991 Jan;34(1):7-12. doi: 10.1021/jm00105a002.
A series of alpha-[(diarylmethoxy)methyl]-1-piperidineethanols was evaluated for antiarrhythmic activity in the coronary artery ligated dog model. Structure-activity relationship studies indicated that the 2,6-dimethylpiperidine group afforded the best antiarrhythmic agents in this series and was essential for long duration of action. This investigation indicated that quaternary ammonium salts were not essential for a long duration of action. It was also shown that the antiarrhythmic activity could be separated from the tachycardia frequently caused by this type of agent.
在冠状动脉结扎犬模型中评估了一系列α-[(二芳基甲氧基)甲基]-1-哌啶乙醇的抗心律失常活性。构效关系研究表明，2,6-二甲基哌啶基团产生了该系列中最佳的抗心律失常药物，并且对于长效作用至关重要。该研究表明，季铵盐对于长效作用并非必不可少。还表明抗心律失常活性可以与这类药物经常引起的心动过速相分离。
