Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Biological ActivityTerfenadine is a histamine 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 (IKr) in guinea pig ventricular myocytes (IC50 = 50 nM). Activity prolongs QT and induces Torsades de pointes (TdP); cardiotoxic in vivo.
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Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions.
Mechanism of terfenadine block of ATP-sensitive K+ channels.
Zunkler et al.
State dependent dissociation of HERG channel inhibitors.
Stork et al.
Citations for Terfenadine
The citations listed below are publications that use Tocris products. Selected citations for Terfenadine include:
3 Citations: Showing 1 - 3
A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia.
Authors: Pérez-G?mez Et al.
Nat Commun 2018;9:5272
Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice.
Authors: Klingerman Et al.
Schizophr Bull 2014;40:327
Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma.
Authors: Francis Et al.
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Terfenadine was used to assess its action on BK channels, which are Calcium activated voltage-gated potassium channels that conduct large amounts of potassium ions (K+) across the cell membrane. Results were reliable and reproducible.