Haloperidol blocks voltage-activated Ca2+ channels in hippocampal neurones

Eur J Pharmacol. 1994 Apr 15;267(2):249-52. doi: 10.1016/0922-4106(94)90178-3.

Abstract

The Ca2+ channel antagonist action of the antipsychotic haloperidol was investigated using two functional assays of Ca2+ channel activity. Haloperidol dose dependently attenuated the rise in intracellular free Ca2+ ([Ca2+]i) evoked by 50 mM extracellular K+ in Fura-2 loaded cultured rat hippocampal neurones with an IC50 (+/- S.E.M.) of 7.8 +/- 0.5 microM and similarly reduced whole-cell Ba2+ currents (IBa) in voltage-clamped mouse hippocampal neurones with an IC50 value of 15.6 +/- 1.1 microM. Block of whole-cell IBa by haloperidol was rapid, fully reversible, and was greater at more depolarized membrane potentials. Our data indicate that haloperidol non-selectively blocks neuronal voltage-gated Ca2+ channels at micromolar concentrations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Barium / pharmacology
  • Calcium Channel Blockers / pharmacology*
  • Cells, Cultured
  • Electrophysiology
  • Fluorescent Dyes
  • Haloperidol / pharmacology*
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Hippocampus / metabolism*
  • Membrane Potentials / drug effects
  • Mice
  • Neurons / drug effects
  • Neurons / metabolism*
  • Potassium / antagonists & inhibitors
  • Potassium / pharmacology
  • Rats

Substances

  • Calcium Channel Blockers
  • Fluorescent Dyes
  • Barium
  • Haloperidol
  • Potassium