Effects of SZV-2649, a new multiple ion channel inhibitor mexiletine analogue
The antiarrhythmic and cardiac electrophysiological effects of SZV-2649 that contains a 2,6-diiodophenoxy moiety but lacks the benzofuran ring system present in amiodarone, were studied in mammalian cell line, rat and dog cardiac preparations. SZV-2649 exerted antiarrhythmic effects against coronary...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2024
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| Sorozat: | SCIENTIFIC REPORTS
14 No. 1 |
| Tárgyszavak: | |
| doi: | 10.1038/s41598-024-73576-5 |
| mtmt: | 35438124 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/34843 |
| LEADER | 02777nab a2200421 i 4500 | ||
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| 024 | 7 | |a 10.1038/s41598-024-73576-5 |2 doi | |
| 024 | 7 | |a 35438124 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a eng | ||
| 100 | 1 | |a Mohammed Aiman | |
| 245 | 1 | 0 | |a Effects of SZV-2649, a new multiple ion channel inhibitor mexiletine analogue |h [elektronikus dokumentum] / |c Mohammed Aiman |
| 260 | |c 2024 | ||
| 300 | |a 18 | ||
| 490 | 0 | |a SCIENTIFIC REPORTS |v 14 No. 1 | |
| 520 | 3 | |a The antiarrhythmic and cardiac electrophysiological effects of SZV-2649 that contains a 2,6-diiodophenoxy moiety but lacks the benzofuran ring system present in amiodarone, were studied in mammalian cell line, rat and dog cardiac preparations. SZV-2649 exerted antiarrhythmic effects against coronary artery occlusion/reperfusion induced ventricular arrhythmias in rats and in acetylcholine- and burst stimulation induced atrial fibrillation in dogs. SZV-2649 inhibited hERG and GIRK currents in HEK cells (IC 50 : 342 and 529 nM, respectively). In canine ventricular myocytes, SZV-2649 (10 µM) decreased the densities of I Kr , and I to outward and I NaL and I CaL inward currents. The compound (2.5–10 µM) elicited Class IB type V max reducing and Class III type action potential duration prolonging effects in dog right ventricular muscle preparations. In canine atrial muscle, SZV-2629 (2.5–10 µM) moderately prolonged action potential duration and this effect was greatly augmented in preparations pretreated with 1 µM carbachol. In conclusion, SZV-2649, has antiarrhythmic effects based on its multiple ion channel blocking properties. Since its chemical structure substantially differs from that of amiodarone, it is expected that SZV-2649 would exhibit fewer adverse effects than the currently used most effective multichannel inhibitor drug amiodarone and may be a promising molecule for further development. | |
| 650 | 4 | |a Általános orvostudomány | |
| 650 | 4 | |a Klinikai orvostan | |
| 700 | 0 | 1 | |a Naveed Muhammad |e aut |
| 700 | 0 | 1 | |a Szabados Tamara |e aut |
| 700 | 0 | 1 | |a Szatmári István |e aut |
| 700 | 0 | 1 | |a Lőrinczi Bálint |e aut |
| 700 | 0 | 1 | |a Mátyus Péter |e aut |
| 700 | 0 | 1 | |a Czompa Andrea |e aut |
| 700 | 0 | 1 | |a Orvos Péter |e aut |
| 700 | 0 | 1 | |a Husti Zoltán |e aut |
| 700 | 0 | 1 | |a Hornyik Tibor |e aut |
| 700 | 0 | 1 | |a Topal Leila |e aut |
| 700 | 0 | 1 | |a Déri Szilvia |e aut |
| 700 | 0 | 1 | |a Jost Norbert László |e aut |
| 700 | 0 | 1 | |a Virág László |e aut |
| 700 | 0 | 1 | |a Bencsik Péter |e aut |
| 700 | 0 | 1 | |a Baczkó István |e aut |
| 700 | 0 | 1 | |a Varró András |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/34843/1/SciRep_23188_Mohammed_2024.pdf |z Dokumentum-elérés |