Caramiphen-induced block of sodium currents and spinal anesthesia

doi:10.1016/j.ejphar.2014.10.035

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標題:	Caramiphen-induced block of sodium currents and spinal anesthesia
作者:	Leung, Yuk-Man Tzeng, Jann-Inn Gong, Chi-Li Wang, Yu-Wen Chen, Yu-Wen Wang, Jhi-Joung
貢獻者:	食品科技系
關鍵字:	Caramiphen Lidocaine Sodium currents Intrathecal Spinal block Duration
日期:	2015-01
上傳時間:	2016-04-19 19:05:49 (UTC+8)
出版者:	Elsevier Science Bv
摘要:	The underlying mechanisms for the action of caramiphen used in local anesthesia are not well understood. The purpose of this study was to evaluate the block of caramiphen on voltage-gated Na+ channels and in spinal anesthesia. We investigated the effect of caramiphen on voltage gated sodium channels in differentiated neuronal NG108-15 cells as well as on rat motor function, proprioception, and pain behavior (when administered intrathecally). In in vitro experiments, lidocaine produced concentration- and state dependent effects on tonic block of voltage gated Na+ currents (IC50 of 66.2 and 212.9 mu M at holding potentials of -70 and -100 mV, respectively). Caramiphen exhibited a milder state dependence of block (IC50 of 52.1 and 99.5 mu M at holding potentials of -70 and -100 mV, respectively). Lidocaine showed a much stronger frequency-dependence of block than caramiphen: with high frequency stimulation (3.33 Hz), 50 mu M caramiphen elicited an additional 20% blockade, whereas the same concentration of lidocaine produced 50% more block. In in vivo experiments, caramiphen with a more sensory-selective action over motor blockade was more potent than lidocaine (P < 0.05) in spinal anesthesia. On an equipotent basis (25% effective dose (ED25), ED50, and ED75), the duration of caramiphen at producing spinal anesthesia was longer than that of lidocaine (P < 0.01). Our data revealed that caramiphen had a more potent, prolonged spinal blockade with a more sensory/nociceptive-selective action over motor blockade in comparison with lidocaine. Spinal anesthesia with caramiphen could be through the suppression of voltage-gated Na+ currents
關聯:	European Journal of Pharmacology, v.746, pp.213-220
顯示於類別:	[ 食品科技系 ] 期刊論文

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