Evidence for inhibitory effects of flupirtine, a centrally acting analgesic, on delayed rectifier K + currents in motor neuron-like cells

Sheng Nan Wu, Ming Chun Hsu, Yu Kai Liao, Fang Tzu Wu, Yuh Jyh Jong, Yi Ching Lo

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37 引文 斯高帕斯(Scopus)

摘要

Flupirtine (Flu), a triaminopyridine derivative, is a centrally acting, non-opiate analgesic agent. In this study, effects of Flu on K + currents were explored in two types of motor neuron-like cells. Cell exposure to Flu decreased the amplitude of delayed rectifier K + current (I K (DR)) with a concomitant raise in current inactivation in NSC-34 neuronal cells. The dissociation constant for Flu-mediated increase of I K (DR) inactivation rate was about 9.8M. Neither linopirdine (10M), NMDA (30M), nor gabazine (10M) reversed Flu-induced changes in I K (DR) inactivation. Addition of Flu shifted the inactivation curve of I K (DR) to a hyperpolarized potential. Cumulative inactivation for I K (DR) was elevated in the presence of this compound. Flu increased the amplitude of M-type K + current (I K (M)) and produced a leftward shift in the activation curve of I K (M). In another neuronal cells (NG108-15), Flu reduced I K (DR) amplitude and enhanced the inactivation rate of I K (DR). The results suggest that Flu acts as an open-channel blocker of delayed-rectifier K + channels in motor neurons. Flu-induced block of I K (DR) is unlinked to binding to NMDA or GABA receptors and the effects of this agent on K + channels are not limited to its action on M-type K + channels.

原文English
文章編號148403
期刊Evidence-based Complementary and Alternative Medicine
2012
DOIs
出版狀態Published - 2012

All Science Journal Classification (ASJC) codes

  • 補充和替代醫學

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