Terfenadine

Catalog # Availability Size / Price Qty
3948/50
Histamine H1 Receptor Antagonists Small Molecule
1 Image
Description: H1 antagonist. Also KV11.1 (hERG) and Kir6 (KATP) channel blocker

Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol

Purity: ≥98%

Product Details
Citations (3)
Supplemental Products
Reviews (1)

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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

Product Datasheets

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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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Terfenadine was used to assess its action on BK channels
By Anonymous on 12/03/2018
Species: Human

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.


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