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

• Authors: BÉBAROVÁ Markéta; MATEJOVIČ Peter; PÁSEK Michal; JANSOVÁ Dagmar; ŠIMURDOVÁ Milena; NOVÁKOVÁ Marie; ŠIMURDA Jiří
• Year of publication: 2009
• Type: Article in Periodical
• Magazine / Source: Naunyn-Schmiedebergs Archives of Pharmacology
• MU Faculty or unit: Faculty of Medicine
• Field: Physiology
• Keywords: perphenazine; antipsychotic drug; sodium current; transient outward current; rat ventricular myocytes
• Description: Perphenazine reversibly blocked fast sodium current INa (reducing its amplitude; IC50 = 1.24 microM) and transient outward potassium current Ito (accelerating its apparent inactivation with a slight decrease of its amplitude; IC50 = 38.2 microM, evaluated from changes of the time integral). Both blocks were use- and frequency-dependent at 3.3 Hz. Computer simulations suggest that perphenazine interacts preferentially with INa channels in inactivated states and with Ito channels in both open and open-inactivated states.

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