Effects of bupivacaine enantiomers and ropivacaine on vasorelaxation mediated by adenosine Triphosphate-sensitive K+ channels in the rat aorta
Effects of bupivacaine enantiomers and ropivacaine on vasorelaxation mediated by adenosine Triphosphate-sensitive K+ channels in the rat aorta
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DOI：
10.1097/00000542-200407000-00040
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发表时间：
2004-07-01
期刊：
影响因子：
8.8
通讯作者：
Hatano, Y
中科院分区：
文献类型：
--
作者：
Dojo, M;Kinoshita, H;Hatano, Y
据报道，局部麻醉剂对神经系统的作用与它们对神经元中K+和Na+通道的影响有关。重要的是，在神经系统的这些K+通道中，电压不敏感的闪烁K+通道被发现比Na+通道对亲脂性，酰胺连接的局部麻醉剂更敏感，特别是对哌啶衍生物布比卡因和罗哌卡因。（2,3）闪烁的K+通道主要存在于薄的有髓神经纤维中，它可能是产生这些纤维静息电位的候选通道。因此，这些结果表明，抑制K+通道有助于布比卡因和罗比卡因对神经系统的作用。累积的研究结果表明，K+通道在生理和病理生理血管扩张中起着至关重要的作用。（5-7）尽管S(-)-布比卡因对心功能或中枢神经系统的毒性比外消旋布比卡因小（8,9），但布比卡因对映体对血管平滑肌K+通道的影响尚未被研究。此外，S（-）对映体罗哌卡因是否影响血管平滑肌的这些通道尚不清楚。因此，本研究旨在通过检测布比卡因对映体和罗哌卡因是否能改变离体大鼠主动脉中三磷酸腺苷（ATP）敏感的K+通道打开剂诱导的血管松弛，来确定酰胺连接的长效局麻药物对血管平滑肌K+通道的效价。
THE actions of local anesthetics on the nervous system are reportedly related to their effects on K+ as well as Na+ channels in neurons.' Importantly, among these K+ channels in the nervous system, a voltage-insensitive flickering K+ channels has been found to be more sensitive than the Na+ channel to lipophilic, amide-linked local anesthetics, especially to the piperidine derivatives bupivacaine and ropivacaine.(2,3) The flickering K+ channel was mostly found in thin, myelinated nerve fibers, and it is a possible candidate for generating the resting potential of these fibers. Therefore, these results indicate that the inhibition of K+ channels contributes to the action of bupivacaine and ropivacaine on the nervous system.Cumulative findings have demonstrated that K+ channels play crucial roles in physiologic and pathophysiologic vasodilation.(5-7) Although S(-)-bupivacaine is less toxic on cardiac function or the central nervous system than racemic bupivacaine,(8,9) the effects of bupivacaine enantiomers on K+ channels of vascular smooth muscle have not been studied. In addition, whether the S(-)enantiomer ropivacaine affects these channels of vascular smooth muscle has been unknown.Therefore, the current study was designed to determine the potency of amide-linked long-acting local anesthetic drugs on K+ channels of vascular smooth muscle, by examining whether bupivacaine enantiomers as well as ropivacaine modify vasorelaxation induced by an adenosine triphosphate (ATP)-sensitive K+ channel opener in the isolated rat aorta.