Catalog Number: 3489
Alternate Names: Hismanal
Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
Biological Activity
Orally active, potent histamine H1 antagonist (IC50 = 4 nM) that displays 20-fold, > 250-fold and > 250-fold selectivity over 5-HT, dopamine and muscarinic acetylcholine receptors respectively. Exhibits antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM). Also potent KV11.1 (hERG) channel blocker (IC50 = 0.9 nM) that displays cardiotoxicity in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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. Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers.
    Cavalli et al.
    J.Med.Chem., 2002;45:3844
  2. A clinical drug library screen identifies astemizole as an antimalarial agent.
    Chong et al.
    Nat.Chem.Biol., 2006;2:415
  3. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole.
    Laduron et al.
    Mol.Pharmacol., 1981;21:294

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

Showing Results 1 - 1 of 1

  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
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