Terfenadine
Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Purity: ≥98%
Biological Activity
Terfenadine 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.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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Transfer of mitochondria from astrocytes to neurons after stroke
Nature, 2016;535(7613):551-5. -
Identification of compounds that suppress Toxoplasma gondii tachyzoites and bradyzoites
Y Murata, T Sugi, LM Weiss, K Kato
PLoS ONE, 2017;12(6):e0178203. -
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
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Citations for Terfenadine
The citations listed below are publications that use Tocris products. Selected citations for Terfenadine include:
5 Citations: Showing 1 - 5
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Cardioluminescence in Transgenic Zebrafish Larvae: A Calcium Imaging Tool to Study Drug Effects and Pathological Modeling.
Authors: Masafumi Et al.
Biomedicines 2021;9
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Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2.
Authors: Rui Et al.
Mol Cancer Ther 2020;19:2023-2033
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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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