Actions of bis(7)-tacrine and tacrine on transient potassium current in rat DRG neurons and potassium current mediated by K(V)4.2 expressed in Xenopus oocyte

  • Brain Res. 2010 Mar 8;1318:23-32. doi: 10.1016/j.brainres.2009.12.047.
Xiang-Yuan Li  1 ,  Jian Zhang ,  Jia-Pei Dai ,  Xiang-Ming Liu ,  Zhi-Wang Li
Affiliations
  • 1. Institute for Electronics and Informatics, South-Central University for Nationalities, Wuhan 430074, PR China.
PMID: 20043893 DOI: 10.1016/j.brainres.2009.12.047
Abstract

Bis(7)-tacrine [bis(7)-tetrahydroaminacrine] is a dimeric AChE Inhibitor derived from tacrine with a potential to treat Alzheimer's disease. Actions of bis(7)-tacrine on ligand-gated ion channels and voltage-gated cation channels have been identified on neurons of both central and peripheral nervous systems. In the present study, the effect of bis(7)-tacrine was investigated on the K(V)4.2 encoded potassium currents expressed in Xenopus oocytes and the transient A-type potassium current (I(K(A))) on rat DRG neurons. Bis(7)-tacrine suppressed recombinant Kv4.2 potassium channels in a concentration-dependent manner, with IC(50) value of 0.53+/-0.13 muM. Tacrine also inhibited Kv4.2 channels, but with a much lower potency (IC(50) 74+/-15 muM).The possible mechanisms underlying the inhibition on potassium currents by bis(7)-tacrine/tacrine could be that inactivation of the transient potassium currents was accelerated and recovery of the native or Kv4.2 expressed potassium currents was suppressed by bis(7)-tacrine/tacrine.

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