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March 15, 1995Circulation

Ibutilide, a Methanesulfonanilide Antiarrhythmic, Is a Potent Blocker of the Rapidly Activating Delayed Rectifier K+Current (IKr) in AT-1 Cells

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Key result

Ibutilide and dofetilide were both potent IKr blockers in mouse atrial tumor myocytes, with EC50 values of 20 nmol/L and 12 nmol/L, respectively.

Authors

TYTao YangSun Yat-sen UniversityDSDirk J. SnydersUniversity of AntwerpDan M. RodenDan M. RodenElectrophysiology

Discussion

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Implication

These EC50 values in murine AT-1 cells warrant no clinical change; leaves open translation to human IKr and arrhythmia risk.

PICO

P
Population
In vitro study on 20 mouse atrial tumor myocytes (AT-1 cells) comparing the IKr blocking effects of ibutilide and dofetilide.
I
Intervention / Comparator
Ibutilide vs Dofetilide
O
Primary Outcome
EC50 for IKr block at +20 mV (nmol/L)

Main Result

Absolute Event Rate: 20% vs 12%

Limitations

  • An effect on inward currents is not excluded.

Cite This Study

Yang et al. (1995) studied this question. Ibutilide vs. Dofetilide was evaluated on EC50 for IKr block at +20 mV (nmol/L). Ibutilide and dofetilide were both potent IKr blockers in mouse atrial tumor myocytes, with EC50 values of 20 nmol/L and 12 nmol/L, respectively.

synapsesocial.com/papers/6a23791c003b3cd7fea5d8behttps://doi.org/10.1161/01.cir.91.6.1799
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents.1990 · 1,472 citations
  2. 2Rate-dependent prolongation of cardiac action potentials by a methanesulfonanilide class III antiarrhythmic agent. Specific block of rapidly activating delayed rectifier K+ current by dofetilide.1993 · 519 citations
  3. 3Suppression of time-dependent outward current in guinea pig ventricular myocytes. Actions of quinidine and amiodarone.1991 · 169 citations
  4. 4K+ currents and K+ channel mRNA in cultured atrial cardiac myocytes (AT-1 cells).1994 · 76 citations
  5. 5Comparative Assessment of Ibutilide, D-Sotalol, Clofilium, E-4031, and UK-68, 798 in a Rabbit Model of Proarrhythmia1993 · 98 citations