About: Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study     Goto   Sponge   NotDistinct   Permalink

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  • 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.
  • 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. (en)
Title
  • Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study
  • Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study (en)
skos:prefLabel
  • Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study
  • Perphenazine-Induced block of sodium and transient outward potassium current: experimental and simulation study (en)
skos:notation
  • RIV/00216224:14110/08:00024258!RIV10-GA0-14110___
http://linked.open...avai/riv/aktivita
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  • P(GA305/04/1385), Z(AV0Z20760514), Z(MSM0021622402)
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  • 1
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  • 386309
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  • RIV/00216224:14110/08:00024258
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  • sodium current; potassium outward current; simulation (en)
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  • CZ - Česká republika
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  • [3D65B39A32F0]
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  • Analysis of Biomedical Signals and Images
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  • 19
http://linked.open...iv/tvurceVysledku
  • Bébarová, Markéta
  • Pásek, Michal
  • Šimurda, Jiří
  • Nováková, Marie
  • Šimurdová, Milena
  • Jansová, Dagmar
  • Matejovič, Peter
http://linked.open...n/vavai/riv/zamer
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  • 1211-412X
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  • 14110
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