J 2008

Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study

BÉBAROVÁ, Markéta, Peter MATEJOVIČ, Michal PÁSEK, Dagmar JANSOVÁ, Milena ŠIMURDOVÁ et. al.

Basic information

Original name

Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study

Name in Czech

Perfenazinem způsobená blokáda sodíkového proudu a přechodného proudu draslíku z buňky: experimentální a simulační studie

Authors

BÉBAROVÁ, Markéta (203 Czech Republic, guarantor, belonging to the institution), Peter MATEJOVIČ (703 Slovakia, belonging to the institution), Michal PÁSEK (203 Czech Republic), Dagmar JANSOVÁ (203 Czech Republic, belonging to the institution), Milena ŠIMURDOVÁ (203 Czech Republic, belonging to the institution), Marie NOVÁKOVÁ (203 Czech Republic, belonging to the institution) and Jiří ŠIMURDA (203 Czech Republic, belonging to the institution)

Edition

Analysis of Biomedical Signals and Images, Brno, Vutium Press, 2008, 1211-412X

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30105 Physiology

Country of publisher

Czech Republic

Confidentiality degree

není předmětem státního či obchodního tajemství

RIV identification code

RIV/00216224:14110/08:00024258

Organization unit

Faculty of Medicine

UT WoS

000303717200018

Keywords in English

sodium current;potassium outward current;simulation

Tags

International impact, Reviewed
Změněno: 19/1/2013 22:00, doc. MUDr. Markéta Bébarová, Ph.D.

Abstract

V originále

The effect of a neuroleptic drug perphenazine on sodium current INa and transient outward potassium current Ito was studied in rat ventricular myocytes at room temperature. Perphenazine reversibly blocked INa (reducing its amplitude; IC50 = 1.24+/-0.10 micromol/l, nH = 0.99+/-0.08) and Ito (accelerating its apparent inactivation with a slight decrease of its amplitude; IC50 = 38.2+/-3.5 micromol/l, nH = 0.75+/-0.07, evaluated from the changes of time integral). Both INa- and Ito-block was use- and frequency-dependent (20%-increase of INablock and 10%-increase of Ito-block under 0.3 and 10 micromol/l perphenazine, respectively, at the stimulation frequency of 3.3 Hz applied after a 15-s rest). The results of quantitative modelling suggest that perphenazine interacts with INa-channels in inactivated states, and with Ito-channels in both open and open-inactivated states.

In Czech

The effect of a neuroleptic drug perphenazine on sodium current INa and transient outward potassium current Ito was studied in rat ventricular myocytes at room temperature. Perphenazine reversibly blocked INa (reducing its amplitude; IC50 = 1.24+/-0.10 micromol/l, nH = 0.99+/-0.08) and Ito (accelerating its apparent inactivation with a slight decrease of its amplitude; IC50 = 38.2+/-3.5 micromol/l, nH = 0.75+/-0.07, evaluated from the changes of time integral). Both INa- and Ito-block was use- and frequency-dependent (20%-increase of INablock and 10%-increase of Ito-block under 0.3 and 10 micromol/l perphenazine, respectively, at the stimulation frequency of 3.3 Hz applied after a 15-s rest). The results of quantitative modelling suggest that perphenazine interacts with INa-channels in inactivated states, and with Ito-channels in both open and open-inactivated states.

Links

GA305/04/1385, research and development project
Name: Modulační úloha sigma signalizace na elektromechanické vztahy izolovaného kardiomyocytu a srdce
Investor: Czech Science Foundation, Modulatory role of sigma signalling in electromechanical coupling of isolated cardiomyocyte and heart
MSM0021622402, plan (intention)
Name: Časná diagnostika a léčba kardiovaskulárních chorob
Investor: Ministry of Education, Youth and Sports of the CR, Early diagnostics and treatment of cardiovascular diseases