Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Schaffer, P; Pelzmann, B; Bernhart, E; Lang, P; Mächler, H; Rigler, B; Koidl, B.
The sulphonylurea glibenclamide inhibits voltage dependent potassium currents in human atrial and ventricular myocytes.
Br J Pharmacol. 1999; 128(6):1175-1180
Doi: 10.1038/sj.bjp.0702904
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- Führende Autor*innen der Med Uni Graz
- Pelzmann Brigitte
- Schaffer Peter
- Co-Autor*innen der Med Uni Graz
- Bernhart Eva Maria
- Koidl Bernd
- Lang Petra
- Mächler Heinrich
- Rigler Bruno
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- Abstract:
- 1 It was the aim of our study to investigate the effects of the sulphonylurea glibenclamide on voltage dependent potassium currents in human atrial myocytes. 2 The drug blocked a fraction of the quasi steady state current (ramp response) which was activated positive to -20 mV, was sensitive to 4-aminopyridine (500 microM) and was different from the ATP dependent potassium current IK(ATP). 3 Glibenclamide dose dependently inhibited both, the peak as well as the late current elicited by step depolarization positive to -20 mV. The IC50 for reduction in charge area of total outward current was 76 microM. 4 The double-exponential inactivation time-course of the total outward current was accelerated in the presence of glibenclamide with a tau(fast) of 12.7+/-1.5 ms and a tau(slow) of 213+/-25 ms in control and 5.8+/-1.9 ms (P<0.001) and 101+/-20 ms (P<0.05) under glibenclamide (100 microM). 5 Our data suggest, that both repolarizing currents in human atrial myocytes, the transient outward current (Ito1) and the ultrarapid delayed rectifier current (IKur) were inhibited by glibenclamide. 6 In human ventricular myocytes glibenclamide inhibited Ito1 without affecting the late current. 7 Our data suggest that glibenclamide inhibits human voltage dependent cardiac potassium currents at concentrations above 10 microM.
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- Adenosine Triphosphate - physiology
- Atrial Function -
- Dose-Response Relationship, Drug -
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- Glyburide - pharmacology
- Heart Atria - cytology Heart Atria - drug effects
- Heart Ventricles - cytology Heart Ventricles - drug effects
- Humans -
- Membrane Potentials - drug effects
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- Time Factors -
- Ventricular Function -
- Find related publications in this database (Keywords)
- Sulfonylurea
- Glibenclamide
- Human
- Cardiac
- Potassium Current
- Transient Outward Current