Orally active, potent histamine H1
= 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
= 227 - 734 nM). Also potent KV
11.1 (hERG) channel blocker (IC50
= 0.9 nM) that displays cardiotoxicity in vivo
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All Tocris products are intended for laboratory research use only.
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.
The citations listed below are publications that use Tocris products. Selected citations for Astemizole include:
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