Original title:
Perphenazine-induced block of sodium and transient outward potassium current: experimental and simulation study
Translated title:
Blokáda sodíkového a přechodného draslíkového proudu perfenazinem: experimentální a simulační studie
Authors:
Bébarová, M. ; Matejovič, P. ; Pásek, Michal ; Jansová, D. ; Šimurdová, M. ; Nováková, M. ; Šimurda, J. Document type: Papers Conference/Event: Biosignál, Brno (CZ), 2008-06-29 / 2008-07-01
Year:
2008
Language:
eng Abstract:
[eng][cze] 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 μmol/l, nH =0.99 +/- 0.08) and Ito (accelerating its apparent inactivation with a slight decrease of its amplitude; IC50 = 38.2 +/- 3.5 μmol/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 μmol/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.Práce prezentuje výsledky experimentálních měření účinků psychofarmaka perfenazinu na rychlý sodíkový proud (INa) a přechodný draslíkový proud (Ito) u komorových buněk potkana. Mechanizmus blokády obou proudů je vyšetřován prostřednictvím matematických modelů.
Keywords:
potassium outward current; simulation; sodium current Project no.: CEZ:AV0Z20760514 (CEP) Host item entry: Analysis of Biomedical Signals and Images, ISBN 978-80-214-3612-1, ISSN 1211-412X
Institution: Institute of Thermomechanics AS ČR
(web)
Document availability information: Fulltext is available at the institute of the Academy of Sciences. Original record: http://hdl.handle.net/11104/0165307