Cat. No. 3948
Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(h
Biological ActivityHistamine 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Stork et al (2007) State dependent dissociation of HERG channel inhibitors. Br.J.Pharmacol. 151 136.
Crumb (2000) Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions. J.Pharmacol.Exp.Ther. 292 261. PMID: 10604956.
Zunkler et al (2000) Mechanism of terfenadine block of ATP-sensitive K+ channels. Br.J.Pharmacol. 130 1571. PMID: 10928959.
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Citations are publications that use Tocris products. Selected citations for Terfenadine include:
Klingerman et al (2014) Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice. Schizophr Bull 40 327. PMID: 23328157.
Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753. PMID: 21873469.
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Keywords: Terfenadine, supplier, hERG, Human, Ether-A-Go-Go, Gene, KV11.1, KIR6, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Potassium, KV, KATP, Channels, voltage-gated, voltage-dependent, Receptors, a-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, Tocris Bioscience, Histamine H1 Receptor Antagonist products