Catalog # Availability Size / Price Qty
Astemizole | CAS No. 68844-77-9 | Histamine H1 Receptor Antagonists
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Description: Orally active, potent H1 antagonist; also KV11.1 (hERG) channel blocker
Alternative Names: Hismanal

Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

Purity: ≥99%

Product Details
Citations (1)
Supplemental Products
Reviews (1)

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

Soluble to 100 mM in DMSO and to 25 mM in ethanol
Store at +4°C

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. 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

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Citation for Astemizole

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Astemizole was used to identify other potential Kv blockers
By Anonymous on 10/31/2018
Application: Species: Human

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.

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