Astemizole

Cat. No. 3489

Astemizole C28H31FN4O [68844-77-9]

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Alternative Name: 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:
458.57
Formula:
C28H31FN4O
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
68844-77-9

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Chong et al (2006) A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2 415. PMID: 16816845.

Cavalli et al (2002) Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers. J.Med.Chem. 45 3844. PMID: 12190308.

Laduron et al (1981) In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol.Pharmacol. 21 294.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Astemizole include:

Klingerman et al (2014) Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice. Schizophr Bull 40 327. PMID: 23328157.

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Keywords: Astemizole, supplier, Potent, hERG, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Orally, active, potent, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Receptors, Histamine, KV11.1, Tocris Bioscience, Histamine H1 Receptor Antagonist products

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