Cat. No. 3489
Alternative Name: Hismanal
Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-
Biological ActivityOrally 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.
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 Datasheet
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.
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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