Electrophysiologic effects of pirmenol, its metabolite 2, and enantiomers, on cardiac Purkinje fibers.
Electrophysiologic effects of pirmenol, its metabolite 2, and enantiomers, on cardiac Purkinje fibers.
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pirmenol、其代谢物 2 和对映体对心脏浦肯野纤维的电生理作用。
DOI：
10.1097/00005344-199309000-00011
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发表时间：
1993
影响因子：
3
通讯作者：
Rosen,MR
中科院分区：
文献类型：
--
作者：
Lee,JH;Rosen,MR
我们使用标准微电极技术研究了薄荷醇、其顺式-(+)和顺式-(-)对映体及其代谢物2对犬浦肯野纤维的电生理效应。母体化合物和两种对映体均能显著降低动作电位（AP）第0相的振幅和最大电位，缩短动作电位持续时间。三种化合物对AP特性的浓度依赖性无显著差异。代谢物2引起第0期振幅和vmax的变化，但幅度较小。与母体化合物相比，代谢物2明显延长了复极时间。研究了杉木酚及其代谢物2的用药依赖性。在10-5 M时，吡门酚的使用依赖性阻滞（T on）发生的时间常数为10.4$ pM 0.4（平均$ pM SEM）次；代谢物2为7.4$ pM 0.8次（p< 0.05）。使用依赖性阻滞（T off）的恢复时间常数具有可比性：吡门酚18$ pM 2 s和代谢物2 21$ pM 6 s （p< 0.05）。吡美诺及其对映体具有相当的局部麻醉作用。与薄荷醇相比，其代谢物2延长AP持续时间。
We used standard microelectrode techniques to study the electrophysiologic effects of pirmenol, its cis-(+) and cis-(-) enantiomers, and its metabolite 2 on canine Purkinje fibers. The parent compound and both enantiomers significantly reduced the amplitude and V max of phase 0 of the action potential (AP) and shortened AP duration (APD). No significant differences were detected in the concentration-dependent effects on AP characteristics among these three compounds. Metabolite 2 caused similar changes in the amplitude and V max of phase 0, but they were of lesser magnitude. In contrast to the parent compound, metabolite 2 markedly prolonged repolarization. The use-dependent effects of pirmenol and metabolite 2 were studied. At 10-5 M, the time constant of onset of use-dependent block (T on) for pirmenol was 10.4$ pM 0.4 (mean $ pM SEM) beats; for metabolite 2, it was 7.4$ pM 0.8 beats (p< 0.05). The time constants of recovery from use-dependent block (T off) were comparable: pirmenol 18$ pM 2 s and metabolite 2 21$ pM 6 s (p< 0.05). Pirmenol and its enantiomers have comparable local anesthetic effects. In contrast to pirmenol, its metabolite 2 prolongs AP duration.