Courtney K R
J Mol Cell Cardiol. 1983 Nov;15(11):749-57. doi: 10.1016/0022-2828(83)90334-6.
This report examines the blocking effects that several antiarrhythmic drugs have on rapid upstroke velocities of action potentials recorded from guinea-pig papillary muscle. A mathematical analysis is developed, that measures an effective "blocking rate' that acts during the action potential with the purpose being to compare these blocking rates for different drug structures. There is a systematic, inverse relationship observed between the concentration of amide-linked drug that must be applied in order to produce a given blocking effect and the lipid distribution capability of each drug. Ether-linked drug structures are relatively more potent than amide-linked drugs in this context.
本报告研究了几种抗心律失常药物对豚鼠乳头肌记录的动作电位快速上升速度的阻断作用。开展了一项数学分析,该分析测量了在动作电位期间起作用的有效“阻断率”,目的是比较不同药物结构的这些阻断率。观察到,为产生给定阻断效果而必须应用的酰胺连接药物浓度与每种药物的脂质分布能力之间存在系统性的反比关系。在这种情况下,醚连接的药物结构比酰胺连接的药物相对更有效。