Haloperidol moderately inhibits cardiovascular L-type calcium current

Effects of haloperidol on L-type CaV1.2 channel were studied. Calcium current was measured in whole cell patch-clamp using calcium as a charge carrier. Inhibition by haloperidol was investigated in CaV1.2 channel natively expressed in rat cardiac myocytes and recombinant cardiac (CaV1.2a) and vascul...

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Published in:General physiology and biophysics 2009-09, Vol.28 (3), p.249-259
Main Authors: Tarabová, Bohumila, Nováková, Marie, Lacinová, L'ubica
Format: Article
Language:English
Subjects:
Action Potentials - drug effects
Animals
Antipsychotic Agents - administration & dosage
Antipsychotic Agents - pharmacology
Calcium - metabolism
Calcium Channel Blockers - administration & dosage
Calcium Channel Blockers - pharmacology
Calcium Channels, L-Type - metabolism
Cell Line
Dose-Response Relationship, Drug
Haloperidol - administration & dosage
Haloperidol - pharmacology
Heart Ventricles - drug effects
Humans
Male
Membrane Potentials - drug effects
Myocytes, Cardiac - drug effects
Myocytes, Cardiac - physiology
Protein Isoforms - metabolism
Rats
Rats, Wistar
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Summary:Effects of haloperidol on L-type CaV1.2 channel were studied. Calcium current was measured in whole cell patch-clamp using calcium as a charge carrier. Inhibition by haloperidol was investigated in CaV1.2 channel natively expressed in rat cardiac myocytes and recombinant cardiac (CaV1.2a) and vascular (CaV1.2b) splice variants of the channel expressed in HEK 293 cells. Haloperidol inhibited L-type calcium current in a concentration-dependent manner with a threshold of 1 nmol/l. 1 micromol/l haloperidol inhibited 20.6 +/- 3.6% of calcium current amplitude in cardiomyocytes, 25.4 +/- 2.6% of current amplitude through the CaV1.2b channel and 28.0 +/- 2.7% of current through the CaV1.2a channel. Inhibition was not accompanied by alteration of current waveform or by shift of current-voltage relation. In a current clamp haloperidol suppressed action potential generation. 1 micromol/l of the drug shortened the action potential duration in part of the cells and suppressed fully action potential in other cells. Moderate inhibition of the L-type calcium channels by haloperidol might cause shortening of action potential. Complete abolishment of action potential must have been mediated by inhibition of another, likely sodium channel.
ISSN:0231-5882
DOI:10.4149/gpb_2009_03_249