| Identification | |
| Name: | Astemizole |
| Synonyms: | Astemisan;Hismanal;Histamen;Histaminos;Histazol;Kelp;Laridal;Metodik;NSC 329963;Novo-Nastizol A;Paralergin;R 43512;Retolen;Waruzol; |
| CAS: | 68844-77-9 |
| EINECS: | 272-441-9 |
| Molecular Formula: | C28H31FN4O |
| Molecular Weight: | 458.63 |
| InChI: | InChI=1/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) |
| Molecular Structure: |  |
| Properties | |
| Density: | 1.2 g/cm3 |
| Stability: | No data. |
| Refractive index: | 1.623 |
| Solubility: | Insoluble |
| Appearance: | White powder |
| Specification: |
?Astemizole , its cas register number is 68844-77-9. It also can be called?1-((4-Fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)ethyl)-4-piperidinyl)- 1H-benzimidazol-2-amine ; 1-(p-Fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole ; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole ; 1H-Benzimidazol-2-amine, 1-((4-fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)eth l)-4-piperidinyl)- ; 1H-Benzimidazol-2-amine, 1-((4-fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)ethyl)-4-piperidinyl)- ; Alermizol ; Astemison ; Astemizol .It is a?crystalline solid. |
| Biological Activity: | Orally active, potent histamine H 1 antagonist (IC 50 = 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 (IC 50 = 227 - 734 nM). Also potent hERG K + channel blocker (IC 50 = 0.9 nM) that displays cardiotoxicity in vivo . |
| Storage Temperature: | Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage. |
| Color: | White crystals |
| Usage: | Nonsedating-type histamine H1-receptor antagonist. Potential for combination therapy with antivancer drugs such as doxorubicin in resistant leukemia. Antihistaminic |
| Safety Data | |
| Hazard Symbols |
Xn: Harmful
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