WebE-4031 acts on a specific class of voltage-gated potassium channels mainly found in the heart, the hERG channels. hERG channels (Kv11.1) mediate the I Kr current, which repolarizes the myocardial cells. [3] [4] The hERG channel is encoded by ether-a-go-go related gene (hERG). WebTerfenadine is a potent open-channel blocker of hERG with a mean IC50 of 204 nM.;IC50 value: 204 nM;Target: HERG;Terfenadine normally undergoes extensive first-pass …
Variability in the measurement of hERG potassium channel …
WebTerfenadine is an antihistamine formerly used for the treatment of allergic conditions. It was brought to market by Hoechst Marion Roussel (now Sanofi) and was marketed under … Webfaimily of tail currents, I-V relationships, and IC50 determinations of two positive blockers (Figures 1-4). Fig. 1. Family of tail currents from whole-cell patch clamping of CHO-hERG cells ... 50 plots of terfenadine and E-4031 using the CHO-hERG cell line as determined by patch clamp. CHO-hERG Cell Line 1001 E. Pender St. Vancouver BC Canada ... conversion of ice vehicle to electric
Validation and Clinical Utility of the hERG IC50:Cmax …
Web6 Feb 2008 · HERG tail currents (IHERG) following test pulses to +20 mV were inhibited by imipramine with an IC50 of 3.4±0.4 μM (mean±s.e.mean) and a Hill coefficient of 1.17±0.03 (n=5). 3 μM ... Webinhibit hERG channels can cause LQTS (acquired or drug-induced LQTS) and an increased risk of Torsades de Pointes. This was first demonstrated in the late 1980s and 1990s for … Web21 Jul 2009 · Terfenadine: Class: Small Molecule: ... Lysenkova LN, Miroshnikova OV, Hendrix J, Rampe D: Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches. Bioorg Med Chem Lett. 2003 May 19;13(10):1829-35. ... IC50: 0.32 uM: Not Available: BindingDB 50017376 : conversion of image to jpeg