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

作者：Li, Xiang-Yuan; Zhang, Jian; Dai, Jia-Pei; Liu, Xiang-Ming^*; Li, Zhi-Wang

来源：Brain Research, 2010, 1318: 23-32.

DOI：10.1016/j.brainres.2009.12.047

• Bis(7)-tacrine
• Tacrine
• K(V)4.2 encoded potassium channel
• A-type K+ channel
• Xenopus oocyte
• Dorsal root ganglion
• Rat

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 IC50 value of 0.53 +/- 0.13 mu M. Tacrine also inhibited Kv4.2 channels, but with a much lower potency (IC50 74 +/- 15 mu M). 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.

• 出版日期2010-3-8
• 单位深圳大学; 中南民族大学