Effect of newly synthesized compounds 44Bu and 444 on QRS -complex width and fast sodium current

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388998%3A_____%2F10%3A00351888" target="_blank" >RIV/61388998:_____/10:00351888 - 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
Effect of newly synthesized compounds 44Bu and 444 on QRS -complex width and fast sodium current
Original language description
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).
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
BO - Biophysics
OECD FORD branch
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Publication year
2010
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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