KILIANOVÁ, Anna, Markéta BÉBAROVÁ, Klára BERÁNKOVÁ, Radka OPATŘILOVÁ, Michal PÁSEK and Ladislava BARTOŠOVÁ. Effect of Newly Synthesized Compounds 44Bu and 444 on QRS-Complex Width and Fast Sodium Current: Differences between Isomers. Acta Veterinaria Brno. Brno, 2010, vol. 79, No 1, p. 41-49. ISSN 0001-7213. Available from: https://dx.doi.org/10.2754/avb201079010041.
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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
Original 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
Doi http://dx.doi.org/10.2754/avb201079010041
UT WoS 000276631000006
Keywords in English 444; 44Bu; isomer; QRS-complex; sodium current; rat
Tags International impact
Changed by Changed by: Mgr. Michal Petr, učo 65024. Changed: 20/4/2012 14:57.
Abstract
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).
Abstract (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)Name: Časná diagnostika a léčba kardiovaskulárních chorob
Investor: Ministry of Education, Youth and Sports of the CR, Early diagnostics and treatment of cardiovascular diseases
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