Terfenadine
Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Purity: ≥98%
Biological Activity
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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions.
Crumb
J.Pharmacol.Exp.Ther., 2000;292:261 -
Mechanism of terfenadine block of ATP-sensitive K+ channels.
Zunkler et al.
Br.J.Pharmacol., 2000;130:1571 -
State dependent dissociation of HERG channel inhibitors.
Stork et al.
Br.J.Pharmacol., 2007;151:136
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Citations for Terfenadine
The citations listed below are publications that use Tocris products. Selected citations for Terfenadine include:
3 Citations: Showing 1 - 3
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A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia.
Authors: Pérez-G?mez Et al.
Nat Commun 2018;9:5272
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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
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Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma.
Authors: Francis Et al.
Gut 2012;61:753
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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.