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Astemizole is a 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.
| Molecular Weight | 458.57 |
| Formula | C28H31FN4O |
| CAS Number | 68844-77-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 45.86 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histamine Receptor Products |
|---|
| Ciproxifan maleate
Ciproxifan is an orally bioavailable, extremely potent histamine H3 inverse agonist/antagonist. |
| Antazoline hydrochloride
Antazoline hydrochloride is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. |
| Azacyclonol
Azacyclonol, also known as γ-pipradol, which diminishes hallucinations in psychotic individuals. |
| Azatadine dimaleate
Azatadine dimaleate is an antihistamine and anticholinergic compound with IC50 of 6.5nM and 10nM, respectively. |
| Bepotastine Besilate
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
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