Inhibition of voltage-gated cationic channels in rat embryonic hypothalamic neurones and C1300 neuroblastoma cells by triphenylethylene antioestrogens

FEBS Lett. 1998 Sep 4;434(3):236-40. doi: 10.1016/s0014-5793(98)00974-0.


The effect of the non-steroidal antioestrogens tamoxifen and toremifene on voltage-gated cationic currents was examined in primary cultures of rat hypothalamic neurones and the C1300 mouse neuroblastoma cell line using the whole-cell patch clamp technique. When applied to the external bathing solution both tamoxifen and toremifene were able to inhibit TTX-sensitive sodium currents with IC50 values of 1-2 microM and delayed rectifier type potassium currents (IC50, 2-3 microM). However, only toremifene showed a significant inhibition of the I(A) current (IC50 3 microM). Inhibition of voltage-gated cationic currents was significantly impaired when tamoxifen was applied in a serum-containing solution. The steroidal antioestrogen ICI 182,780 did not inhibit any of the currents at 10 microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Estrogen Antagonists / pharmacology*
  • Hypothalamus / drug effects*
  • Hypothalamus / embryology
  • Hypothalamus / physiology
  • Ion Channel Gating
  • Mice
  • Neuroblastoma / pathology
  • Neuroblastoma / physiopathology
  • Neurons / cytology
  • Neurons / drug effects
  • Neurons / physiology
  • Potassium Channel Blockers*
  • Potassium Channels / physiology
  • Rats
  • Rats, Sprague-Dawley
  • Sodium Channel Blockers*
  • Sodium Channels / physiology
  • Tamoxifen / pharmacology*


  • Estrogen Antagonists
  • Potassium Channel Blockers
  • Potassium Channels
  • Sodium Channel Blockers
  • Sodium Channels
  • Tamoxifen