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Submit ReviewAstemizole
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% (HPLC)
Biological Activity for Astemizole
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 for Astemizole
| M. Wt | 458.57 |
| Formula | C28H31FN4O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 68844-77-9 |
| PubChem ID | 2247 |
| InChI Key | GXDALQBWZGODGZ-UHFFFAOYSA-N |
| Smiles | FC(C=C5)=CC=C5CN2C1=CC=CC=C1N=C2NC3CCN(CCC4=CC=C(OC)C=C4)CC3 |
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.
Solubility Data for Astemizole
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.86 | 100 | |
| ethanol | 11.46 | 25 |
Preparing Stock Solutions for Astemizole
The following data is based on the product molecular weight 458.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.18 mL | 10.9 mL | 21.81 mL |
| 5 mM | 0.44 mL | 2.18 mL | 4.36 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.18 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for Astemizole
References for Astemizole
References are publications that support the biological activity of the product.
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
Chong et al (2006) A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2 415 PMID: 16816845
Laduron et al (1981) In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol.Pharmacol. 21 294 PMID: 6124876
If you know of a relevant reference for Astemizole, please let us know.
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Keywords: Astemizole, 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, Hismanal, Voltage-Gated, 3489, Tocris Bioscience
1 Citation for Astemizole
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
Do you know of a great paper that uses Astemizole from Tocris? Please let us know.
Reviews for Astemizole
Average Rating: 5 (Based on 1 Review.)
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Astemizole was used to identify other potential Kv blockers.
By
Anonymous on 10/31/2018
Assay Type: In Vitro
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.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.