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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 |
|---|
| Dimethindene
Dimethindene is a potent, selective histamine H1 antagonist. |
| ABT-288
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. |
| A-349821
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. |
| Betazole
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. |
| Tiotidine
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). |
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