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Effect of antipsychotic drug perphenazine on fast sodium current and transient outward potassium current in rat ventricular myocytes
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SYSNO ASEP 0330554 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Effect of antipsychotic drug perphenazine on fast sodium current and transient outward potassium current in rat ventricular myocytes Title Vliv antipsychotika perfenazinu na rychlý sodíkový proud a přechodný draslíkový proud u komorových srdečních buněk potkana Author(s) Bébarová, M. (CZ)
Matejovič, P. (CZ)
Pásek, Michal (UT-L) RID, ORCID
Jansová, D. (CZ)
Šimurdová, M. (CZ)
Nováková, M. (CZ)
Šimurda, J. (CZ)Source Title Naunyn-Schmiedeberg's Archives of Pharmacology. - : Springer - ISSN 0028-1298
Roč. 380, č. 2 (2009), s. 125-133Number of pages 9 s. Language eng - English Country DE - Germany Keywords perphenazine ; antipsychotic drug ; sodium current ; transient outward current ; rat ventricular myocytes Subject RIV ED - Physiology CEZ AV0Z20760514 - UT-L (2005-2011) UT WOS 000266926900004 DOI 10.1007/s00210-009-0420-1 Annotation The effect of antipsychotic drug perphenazine (0.1–100 ?M) on fast sodium current INa and on transient outward potassium current Ito was analysed in enzymatically isolated rat right ventricular myocytes by the whole-cell patch-clamp technique at room temperature. Perphenazine reversibly blocked INa (reducing its amplitude; IC50=1.24±0.10 ?M) and Ito (accelerating its apparent inactivation with a slight decrease of its amplitude; IC50=38.2±3.5 ?M, evaluated from changes of the time integral). The fast time constant of Ito inactivation was significantly decreased in a concentration-dependent manner (IC50=30.0±6.6 ?M). Both blocks were use and frequency dependent at 3.3 Hz. We conclude that perphenazine cause concentration-,use-,and frequency-dependent block of INa and Ito. Computer simulations suggest that perphenazine interacts preferentially with INa channels in inactivated states and with Ito channels in both open and open-inactivated s tates. Workplace Institute of Thermomechanics Contact Marie Kajprová, kajprova@it.cas.cz, Tel.: 266 053 154 ; Jana Lahovská, jaja@it.cas.cz, Tel.: 266 053 823 Year of Publishing 2010
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