Terfenadine herg ic50
Web15 Aug 1996 · BackgroundAdministration of the antihistamine terfenadine (Seldane) to patients may result in acquired long QT syndrome and ventricular arrhythmias.One human cardiac target is Kv1.5, which expresses the ultrarapid outward K + current (I Kur) in atrium but may play only a minor role in ventricle.Another possible target is HERG, the human … WebFour general categories of drugs were identified: high-potency blockers (IC50 1 microM) included propafenone, loratadine, pyrilamine, lovastatin, and chlorpheniramine; and …
Terfenadine herg ic50
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WebHistamine H1 receptor antagonist. Also blocks KV11.1 (hERG) and Kir6 (KATP) channels (IC50 values are 204 nM and 1.2 μM respectively). Inhibits the delayed rectifier K+ current … 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 ...
Web1 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 ... WebTerfenadine directly blocked the hERG channel current but had no effect on trafficking of hERG channels to the cell membrane after application in culture medium for 2 d. In …
WebTerfenadine is a potent open-channel blocker of hERG (IC50=204 nM), formerly used for the treatment of allergic conditions. Specification. Purity. ≥98%. Appearance. White Solid. ... expressed in Escherichia coli indicated that marmoset P450 2J2 effectively catalyzed astemizole O-demethylation and terfenadine t-butyl hydroxylation, similar to ... 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 ((±)-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 …
Web23 Mar 2024 · Drug-induced cardiotoxicity represents one of the most critical safety concerns in the early stages of drug development. The blockade of the human ether-à-go-go-related potassium channel (hERG) is the most frequent cause of cardiotoxicity, as it is associated to long QT syndrome which can lead to fatal arrhythmias. Therefore, … atlantis sanya addressWeb21 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 : piso uhtWeb1 May 2024 · As the hERG model was parameterized by dynamic data collected at physiological temperature by a single laboratory, the predicted IC 50 s could be regarded … atlantis ruins bahamasWebTerfenadine ((±)-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 … piso venta aiaWebS. 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 ... atlantis sand dunes quad bikingWeb1 Mar 2008 · Amiodorone is not a potent hERG blocker (assessed by patch clamping) when compared to its clinical concentrations. Similarly, pimozide has been shown to have margin between efficacious clinical concentrations and the hERG IC50 of slightly higher than 30-fold (Redfern et al., 2003). Therefore, you would come to the conclusion that amiodorone and ... atlantis sahara desertWeb6 Jul 2024 · Introduction. Blockade of the human ether à-go-go related gene potassium channels is associated with drug-induced QT interval prolongation, which could cause arrhythmia and more severe heart failure [1–3].The inhibition of hERG has become the major reason for drug withdrawals in the late 1990s, as represented by the withdrawals of … piso tulum star