DELAYED RECTIFIER CURRENT ASSAYS

hERG CHANNEL TAIL CURRENT

EFFECTS OF E-4031 ON THE hERG CHANNEL TAIL CURRENT

Figure 1  Effects of E-4031 on the hERG channel tail current.

Figure 1 shows an example of typical hERG channel tail currents recorded by scientists at OCP, under our standard whole-cell patch-clamp conditions for the measurement of hERG channel tail currents in a stably transfected cell line.

Figure 1 shows superimposed hERG channel tail current records in the absence (black) and presence (red) of E-4031 (3 鮍

 

Figure 2   Time course for the effect of E-4031 on the amplitude hERG channel tail current.

 
 

Figure 2  shows hERG channel tail current amplitude (denoted by black symbols) is stable over the 4 minute control recording period. Application of E-4031  (3 頣aused a time dependent decrease in the outward tail current consistent with block of IKr.


 

Figure 3   Determination of the IC50 of E-4031 on hERG channel tail current measured in a stably transfected cell line.


Figure 3   shows the percentage decrease in the peak amplitude of hERG channel tail current plotted as a function of concentration of dofetilide.

The left hand panel shows the data points taken from individual experiments.

The right hand panel shoes mean孠data for these experiment.  These data points can be fit by a sigmoid curve (logistic function) which produces and IC50 value of 6.8�

 


 

 
  All data 㯰yright to OCP Ltd. 2006. All Rights Reserved. Design by OCP