Astemizole
Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
Purity: ≥99%
Biological Activity
Astemizole is an 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
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
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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 -
A clinical drug library screen identifies astemizole as an antimalarial agent.
Chong et al.
Nat.Chem.Biol., 2006;2:415
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Citation for Astemizole
The citations listed below are publications that use Tocris products. Selected citations for Astemizole include:
1 Citation: Showing 1 - 1
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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
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