Abstract
The Ca 2+ channel antagonist action of the antipsychotic haloperidol was investigated using two functional assays of Ca 2+ channel activity. Haloperidol dose dependently attenuated the rise in intracellular free Ca 2+ ([Ca 2+] i) evoked by 50 mM extracellular K + in Fura-2 loaded cultured rat hippocampal neurones with an IC 50 (± S.E.M.) of 7.8 ± 0.5 μM and similarly reduced whole-cell Ba 2+ currents ( I Ba) in voltage-clamped mouse hippocampal neurones with an IC 50 value of 15.6 ± 1.1 μM. Block of whole-cell I Ba 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 Ca 2+ channels at micromolar concentrations.
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