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

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14110%2F08%3A00024258" target="_blank" >RIV/00216224:14110/08:00024258 - isvavai.cz</a>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

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

Original language description

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.

Czech name

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

Czech description

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.

Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

ED - Physiology

OECD FORD branch

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Project

<a href="/en/project/GA305%2F04%2F1385" target="_blank" >GA305/04/1385: Modulatory role of sigma signalling in electromechanical coupling of isolated cardiomyocyte and heart</a><br>

Continuities

Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2008

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Analysis of Biomedical Signals and Images

ISSN

1211-412X

e-ISSN

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Volume of the periodical

19

Issue of the periodical within the volume

1

Country of publishing house

CZ - CZECH REPUBLIC

Number of pages

5

Pages from-to

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UT code for WoS article

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EID of the result in the Scopus database

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