Terfenadine herg ic50
WebTerfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. - Mechanism of Action & … Web1 Jul 2013 · Terfenadine is concordant and verapamil is discordant with the hypothesis that potent hERG blockers are torsadogenic. (a) IC50 values for hERG, Nav1.5 and Cav1.2 and the maximum effective free ...
Terfenadine herg ic50
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WebTerfenadine itself, however, is cardiotoxic at higher doses, while its major active metabolite is not. Terfenadine, in addition to its antihistamine effects, also acts as a potassium channel blocker (K v 11.1 encoded by the gene hERG). Since its active metabolite is not a potassium channel blocker, no cardiotoxicity is associated with fexofenadine. WebTerfenadine (3 microM) caused a marked (approximately 80%) inhibition of IHERG in SH-SY5Y cells, whereas loratadine, at the same concentration, caused a 40% blockade. …
Web301 Moved Permanently. nginx 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 ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC 50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer … WebThe Predictor™ hERG Fluoresence Polarization assay uses a proprietary fluorescent tracer and membrane preparation to create a highly reproducible assay. Using the assay, IC50 values for over 10 known hERG channel blockers compared well to published patch clamp and radioligand binding data (Figure 1 and Table 1). Figure 1.
WebS. Kongsamut et al. 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 concentration to HERG IC50 ([Total plasma]/HERG IC50 )appeared to correspond well with the observed changes in QTc. This ratio ranged from ...
WebTerfenadine inhibits the release of leukotrienes C4/D4 (IC50: 8 mumol), B4 (IC50: 9.9 mumol), tumor necrosis factor alpha (IC50: 6.1 mumol) and granulocyte/macrophage … incyte foundationWeb1 Sep 2000 · On the other hand, terfenadine and astemizole effectively blocked HERG K+ channels with nanomolar affinities (the estimated IC50 values were 330 and 480 nM, respectively), whereas loratadine was ... incyte fundingWeb1 Sep 2004 · In vitro hERG IC50 values were shown to vary as a function of cell culture conditions, patch clamp protocol, data fitting approach [13][14][15], and temperature [14]. ... Terfenadine (n = 459 ... incyte h1bWeb(IC50). HERG current is measured as the peak outward current during the ramp down phase. To ... For the hERG current, we recommend cisapride, terfenadine, or dofetilide. For CaV1.2 currents, we ... include graphics sizeWeb21 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 : incyte grantsWebDownload Table Summary of hERG IC 50 values and safety margins from publication: Predicting QT prolongation in humans during early drug development using hERG … incyte gvhdWebfaimily 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 ... incyte hamilton