Donepezil is a strong antagonist of voltage-gated calcium and potassium channels in molluscan neurons

Comp Biochem Physiol C Toxicol Pharmacol. 2007 Jan;144(4):319-26. doi: 10.1016/j.cbpc.2006.10.001. Epub 2006 Oct 19.

Abstract

Donepezil is an acetylcholinesterase inhibitor used in Alzheimer's disease therapy. The neuroprotective effect of donepezil has been demonstrated in a number of different models of neurodegeneration including beta-amyloid toxicity. Since the mechanisms of neurodegeneration involve the activation of both Ca(2+)- and K(+)-channels, the study of donepezil action on voltage-gated ionic currents looked advisable. In the present study, the action of donepezil on voltage-gated Ca(2+)- and K(+)-channels was investigated on isolated neurons of the edible snail (Helix pomatia) using the two-microelectrodes voltage-clamp technique. Donepezil rapidly and reversibly inhibited voltage activated Ca(2+)-current (I(Ca)) (IC(50)=7.9 microM) and three types of high threshold K(+)-current: Ca(2+)-dependent K(+)-current (I(C)) (IC(50)=6.4 microM), delayed rectifier K(+)-current (I(DR)) (IC(50)=8.0 microM) and fast transient K(+)-current (I(Adepol)) (IC(50)=9.1 microM). The drug caused a dual effect on low-threshold fast transient K(+)-current (I(A)), potentiating it at low (5 microM) concentration, but inhibiting at higher (7 microM and above) concentration. Donepezil also caused a significant hyperpolarizing shift of the voltage-current relationship of I(Ca) (but not of any type of K(+)-current). Results suggest the possible contribution of the blocking effect of donepezil on the voltage-gated Ca(2+)- and K(+)-channels to the neuroprotective effect of the drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / physiology
  • Cholinesterase Inhibitors / pharmacology
  • Donepezil
  • Helix, Snails / physiology
  • In Vitro Techniques
  • Indans / pharmacology*
  • Neurons / drug effects*
  • Neurons / physiology
  • Piperidines / pharmacology*
  • Potassium Channel Blockers / pharmacology*
  • Potassium Channels, Voltage-Gated / physiology

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Cholinesterase Inhibitors
  • Indans
  • Piperidines
  • Potassium Channel Blockers
  • Potassium Channels, Voltage-Gated
  • Donepezil