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Terfenadine

3948 3 Citations 1 Review Datasheet / COA / SDS
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3948/50
Terfenadine | CAS No. 50679-08-8 | Histamine H1 Receptor Antagonists
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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 Technical Data Background Product Datasheets Calculators

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

  1. A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia.
    Authors: Pérez-G?mez Et al.
    Nat Commun  2018;9:5272
  2. 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
  3. Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma.
    Authors: Francis Et al.
    Gut  2012;61:753

FAQs

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VersaClone cDNA Plasmids

Mouse Histamine H1 R (NP_032311) VersaClone cDNA

RDC0392

Human Histamine H1 R (AAH60802) VersaClone cDNA

RDC0341

Reviews for Terfenadine

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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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