Publication detail

Effect of antipsychotic drug perphenazine on fast sodium current and transient outward potassium current in rat ventricular myocytes

BÉBAROVÁ, M. MATĚJOVIČ, P. PÁSEK, M. ŠIMURDOVÁ, M. NOVÁKOVÁ, M. ŠIMURDA, J.

Original Title

Effect of antipsychotic drug perphenazine on fast sodium current and transient outward potassium current in rat ventricular myocytes

Type

journal article - other

Language

English

Original Abstract

Antipsychotic drug perphenazine belongs to the phenothiazine group commonly reported to induce ECG changes and tachyarrhythmias. Data about its effect on ionic membrane currents in cardiomyocytes are missing. We analyzed the effect of perphenazine (0.1-100 uM) on fast sodium current INa and transient outward potassium current Ito in enzymatically isolated rat right ventricular myocytes by the whole-cell patch-clamp technique at room temperature. Perphenazine reversibly blocked INa (reducing its amplitude; IC50=1.24+-0.10 uM) and Ito (accelerating its apparent inactivation with a slight decrease of its amplitude; IC50=38.2+-3.5 uM, evaluated from changes of the time integral). The fast time constant of Ito inactivation was significantly decreased in a concentration-dependent manner (IC50=30.0+-6.6 uM). Both blocks were use and frequency dependent at 3.3 Hz. We conclude that perphenazine causes concentration-, use-, and frequency-dependent block of INa

Keywords

Perphenazine; Sodium current; Transient outward potasium current; Mathematical simulations; Ventricular myocytes

Authors

BÉBAROVÁ, M.; MATĚJOVIČ, P.; PÁSEK, M.; ŠIMURDOVÁ, M.; NOVÁKOVÁ, M.; ŠIMURDA, J.

RIV year

2009

Released

9. 5. 2009

Publisher

Springer -Verlag

ISBN

0028-1298

Periodical

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Year of study

380

Number

5

State

Federal Republic of Germany

Pages from

125

Pages to

133

Pages count

9

BibTex

@article{BUT49584,
  author="Markéta {Bébarová} and Peter {Matějovič} and Michal {Pásek} and Milena {Šimurdová} and Marie {Nováková} and Jiří {Šimurda}",
  title="Effect of antipsychotic drug perphenazine on fast sodium current and transient outward potassium current in rat ventricular myocytes",
  journal="NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY",
  year="2009",
  volume="380",
  number="5",
  pages="125--133",
  issn="0028-1298"
}