2010
Effect of Newly Synthesized Compounds 44Bu and 444 on QRS-Complex Width and Fast Sodium Current: Differences between Isomers
KILIANOVÁ, Anna; Markéta BÉBAROVÁ; Klára BERÁNKOVÁ; Radka OPATŘILOVÁ; Michal PÁSEK et. al.Basic information
Original name
Effect of Newly Synthesized Compounds 44Bu and 444 on QRS-Complex Width and Fast Sodium Current: Differences between Isomers
Name in Czech
Účinek nově syntetizovaných látek 44Bu a 444 na šíři QRS-komplexu a na rychlý sodíkový proud: rozdíly mezi izomery
Authors
KILIANOVÁ, Anna (203 Czech Republic, belonging to the institution); Markéta BÉBAROVÁ (203 Czech Republic, guarantor, belonging to the institution); Klára BERÁNKOVÁ (203 Czech Republic); Radka OPATŘILOVÁ (203 Czech Republic); Michal PÁSEK (203 Czech Republic, belonging to the institution) and Ladislava BARTOŠOVÁ (203 Czech Republic)
Edition
Acta Veterinaria Brno, Brno, 2010, 0001-7213
Other information
Language
English
Type of outcome
Article in a journal
Field of Study
30104 Pharmacology and pharmacy
Country of publisher
Czech Republic
Confidentiality degree
is not subject to a state or trade secret
Impact factor
Impact factor: 0.534
RIV identification code
RIV/00216224:14110/10:00051343
Organization unit
Faculty of Medicine
UT WoS
000276631000006
Keywords in English
444; 44Bu; isomer; QRS-complex; sodium current; rat
Tags
International impact
Changed: 20/4/2012 14:57, Mgr. Michal Petr
V originále
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).
In Czech
Všechny varianty látek 44Bu a 444 (1,5 mg/kg) způsobily signifikantní prodloužení QRS-komplexu s maximem v 1. nebo 2. minutě po jejich intravenózním podání. Racemát látky 44Bu prodloužil QRS-komplex o 57%, signifikantně více než R- (o 33%) and S-izomer (o 36%). Racemát látky 444 prodloužil QRS-komplex o 66%, srovnatelně s S-izomerem (o 63%), nicméně více než R-izomer (rozšíření o 49%). Co se týká vlivu na INa, látka 44Bu způsobila statisticky významně hlubší blokádu INa ve srovnání s látkou 444 při podání ve stejné koncentraci 3,0 micromol/l (0,1 mg/kg). Racemát a R-izomer látky 44Bu blokovali INa stejně (blokáda 91,7% respektive 91,8%), avšak signifikantně více než S-izomer (82,4%). R-izomer látky 444 blokoval INa méně než racemát a S-izomer (31,7% oproti 48,3 a 50,2%).
Links
| MSM0021622402, plan (intention) |
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