In our experiments, verapamil caused high-affinity block of HERG current (IC505143
Evaluation of Possible Proarrhythmic Potency: Comparison of the Effect of Dofetilide
Verapamil (hERG IC 50 = 250 nM; Cav IC 50 = 200 nM) and clozapine
Verapamil is not associated with QT prolongation and TdP in humans, but inhibits hERG
We find that quinidine and verapamil produce substantial disagreement between
European Journal of Pharmacology 450 (2002) 37-41 have examined the influence of HERG affinity on QT-prolongation, and found for a series of antipsychotic drugs, the ratio of total plasma
4) for verapamil
In our experiments, verapamil caused high-affinity block of HERG current (IC 50 =143
Located in human ventricles and human atria, the hERG encodes the potassium channel responsible for the delayed rectifier current Ikr [9,10]
Drugs associated with QT prolongation and/or Torsades-de-Pointes (dofetilide, cisapride, and terfenadine, examples of overt hERG blocking drugs) have IC 50 values for hERG block overlapping drug exposures
[ 1] The name of hERG is frequently used to refer to the channel protein, whereas the official gene name of the hERG channel is KCNH2, and K v 11
1999; 84:989–998
The origin of this offset is due mainly to the following property of the LFA assay: K + efflux is coupled to H + influx and for some channels such as hERG the latter
Certain physicochemical properties of molecules have been recognized as early indicators of potential problems with early drug discovery compounds [ 19 ]
Development of Drug Block by Verapamil
AbstractAim:The objectives of this study were to investigate the inhibitory action of verapamil on wild-type(WT) and mutation HERG K+ channel current