Catalog Number: 3948
Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
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
  • M.Wt:
    471.67
  • Formula:
    C32H41NO2
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    50679-08-8
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.
Background References
  1. Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions.
    Crumb
    J.Pharmacol.Exp.Ther., 2000;292:261
  2. Mechanism of terfenadine block of ATP-sensitive K+ channels.
    Zunkler et al.
    Br.J.Pharmacol., 2000;130:1571
  3. State dependent dissociation of HERG channel inhibitors.
    Stork et al.
    Br.J.Pharmacol., 2007;151:136
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Terfenadine include:

2 Citations: Showing 1 - 2
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  1. 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
  2. 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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