BÉBAROVÁ, Markéta, Peter MATEJOVIČ, Michal PÁSEK, Dagmar JANSOVÁ, Milena ŠIMURDOVÁ, Marie NOVÁKOVÁ and Jiří ŠIMURDA. Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study. Analysis of Biomedical Signals and Images. Brno: Vutium Press, 2008, vol. 19, No 1, p. 1-5. ISSN 1211-412X.
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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
Original language English
Type of outcome Article in a journal
Field of Study 30105 Physiology
Country of publisher Czech Republic
Confidentiality degree is not subject to a state or trade secret
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 potassium outward current, simulation, sodium current
Tags International impact, Reviewed
Changed by Changed by: doc. MUDr. Markéta Bébarová, Ph.D., učo 15000. Changed: 19/1/2013 22:00.
Abstract
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.
Abstract (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 projectName: 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
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