Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
Biological ActivityAstemizole 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers.
Cavalli et al.
A clinical drug library screen identifies astemizole as an antimalarial agent.
Chong et al.
In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole.
Laduron et al.
Citation for Astemizole
The citations listed below are publications that use Tocris products. Selected citations for Astemizole include:
1 Citation: Showing 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 2014;40:327
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Average Rating: 5 (Based on 1 Review)
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Astemizole is a great well known histaminic drug which shows Kv channel blocking at high concentrations. It was used on our lab to identify other potential Kv blockers. While using it as a standard, it worked ideally all during the study period.