Pharmacology of mitochondrial potassium channels: dark side of the field

FEBS Lett. 2010 May 17;584(10):2063-9. doi: 10.1016/j.febslet.2010.02.048. Epub 2010 Feb 20.


Mitochondrial potassium channels play an important role in cytoprotection. Potassium channels in the inner mitochondrial membrane are modulated by inhibitors and activators (potassium channel openers) previously described for plasma membrane potassium channels. The majority of mitochondrial potassium channel modulators exhibit a broad spectrum of off-target effects. These include uncoupling properties, inhibition of the respiratory chain and effects on cellular calcium homeostasis. Therefore, the rational application of channel inhibitors or activators is crucial to understanding the cellular consequences of mitochondrial channel inhibition or activation. Moreover, understanding their side-effects should facilitate the design of a specific mitochondrial channel opener with cytoprotective properties. In this review, we discuss the complex interactions of potassium channel inhibitors and activators with cellular structures.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Animals
  • Homeostasis / drug effects
  • Humans
  • Ion Channel Gating / drug effects
  • Mitochondria / drug effects*
  • Mitochondria / metabolism*
  • Potassium Channel Blockers / pharmacology*
  • Potassium Channels / agonists*
  • Potassium Channels / metabolism


  • Potassium Channel Blockers
  • Potassium Channels
  • Adenosine Triphosphate