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

  • Pharmacol Rep. 2012;64(3):739-44. doi: 10.1016/s1734-1140(12)70869-1.
Yuk-Man Leung  1 ,  Kar-Lok Wong ,  Ka-Shun Cheng ,  Chang-Shin Kuo ,  Tzu-Hui Su ,  Yu-Wen Chen ,  Tzu-Hurng Cheng
Affiliations
  • 1. Graduate Institute of Neural and Cognitive Sciences, China Medical University, Taichung 40402, Taiwan. [email protected]
PMID: 22814027 DOI: 10.1016/s1734-1140(12)70869-1
Abstract

Background: 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.

Methods: Electrophysiological experiments were performed to study ion channel activities in two neuronal cell lines, namely, neuroblastoma N2A cells and differentiated NG108-15 cells.

Results: Diphenidol inhibited voltage-gated K(+) channels and CA(2+) channels, but did not affect store-operated CA(2+) channels.

Conclusion: Diphenidol is a non-specific inhibitor of voltage-gated ion channels in neuronal cells.

Products