Inhibition of voltage-gated K+ channels and Ca2+ channels by diphenidol.

Although diphenidol has long been deployed as an anti-emetic and anti-vertigo drug, its mechanism of action remains unclear. In particular, little is known as to how diphenidol affects neuronal ion channels. Recently, we showed that diphenidol blocked neuronal voltage-gated Na(+) channels, causing spinal blockade of motor function, proprioception and nociception in rats. In this work, we investigated whether diphenidol could also affect voltage-gated K(+) and Ca(2+) channels. Electrophysiological experiments were performed to study ion channel activities in two neuronal cell lines, namely, neuroblastoma N2A cells and differentiated NG108-15 cells. Diphenidol inhibited voltage-gated K(+) channels and Ca(2+) channels, but did not affect store-operated Ca(2+) channels. Diphenidol is a non-specific inhibitor of voltage-gated ion channels in neuronal cells.

Citation

Yuk-Man Leung, Kar-Lok Wong, Ka-Shun Cheng, Chang-Shin Kuo, Tzu-Hui Su, Yu-Wen Chen, Tzu-Hurng Cheng. Inhibition of voltage-gated K+ channels and Ca2+ channels by diphenidol. Pharmacological reports : PR. 2012;64(3):739-44

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PMID: 22814027

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