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Effect of newly synthesized compounds 44Bu and 444 on QRS -complex width and fast sodium current
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SYSNO ASEP 0351888 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Effect of newly synthesized compounds 44Bu and 444 on QRS -complex width and fast sodium current Author(s) Kilianová, A. (CZ)
Bébarová, M. (CZ)
Beránková, K. (CZ)
Opatřilová, R. (CZ)
Pásek, Michal (UT-L) RID, ORCID
Bartošová, L. (CZ)Number of authors 6 Source Title Acta veterinaria Brno. - : Veterinární a farmaceutická univerzita Brno - ISSN 0001-7213
Roč. 79, č. 1 (2010), s. 41-49Number of pages 9 s. Language eng - English Country CZ - Czech Republic Keywords 444 ; 44Bu ; QRS-complex ; sodium current ; rat Subject RIV BO - Biophysics CEZ AV0Z20760514 - UT-L (2005-2011) UT WOS 000276631000006 DOI https://doi.org/10.2754/avb201079010041 Annotation In this study, we explored the effect of both racemates and particular isomers of 44Bu and 444 on the QRS-complex width in vivo in rats and on INa in isolated rat ventricular myocytes. All variants of 44Bu and 444 (1.5 mg/kg) caused a significant QRS-widening reaching the peak effect at the 1st or 2nd min after their intravenous administration. 44Bu racemate widened the QRS-complex by 57%, significantly more than R- (33%-widening) and S-isomer (36%-widening). 444 racemate widened the QRS-complex by 64%, which was comparable to S-isomer (63%-widening), however, substantially more than R-isomer (40%-widening). Regarding the effect on INa, 44Bu caused a significantly deeper INa-block compared to 444 in the same concentration of 3.0 micromol/l (0.1 mg/kg). 44Bu racemate and R-isomer blocked INa similarly (91.7 and 91.8%-block, respectively), significantly more than S-isomer (82.4%-block). 444 R-isomer blocked INa less than racemate and S-isomer (by 31.7% vs. 48.3 and 50.2%, respectively). 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 2011
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