Detail publikace

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.

Originální název

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

Typ

článek v časopise - ostatní, Jost

Jazyk

angličtina

Originální abstrakt

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

Klíčová slova

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

Autoři

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

Rok RIV

2009

Vydáno

9. 5. 2009

Nakladatel

Springer -Verlag

ISSN

0028-1298

Periodikum

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Ročník

380

Číslo

5

Stát

Spolková republika Německo

Strany od

125

Strany do

133

Strany počet

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"
}