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MedicaPharma distributes high-quality active pharmaceutical ingredients (APIs) to hospitals, commercial (compounding) pharmacies, research institutes, and universities worldwide.
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Let us handle your sourcing / supply activities. Highly experienced in sourcing specialty raw pharmaceutical ingredients from niche GMP manufacturers around the world.
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Product Description
Mechanism of action
Astemizole is a second-generation H histamine receptor antagonist with high affinity and prolonged receptor occupancy. It competitively inhibits histamine binding at peripheral H receptors, thereby attenuating histamine- induced vasodilation, increased vascular permeability and sensory nerve stimulation. Astemizole is highly lipophilic, undergoes extensive first-pass metabolism and exhibits a long half-life, resulting in sustained antihistaminic activity.
Benefits and advantages
In preclinical and in vitro settings, astemizole is widely used as a reference compound for assessing cardiotoxicity because it potently blocks the cardiac delayed rectifier potassium current (IKr) via hERG (K⁺v11.1) channel inhibition. This property makes it valuable in safety pharmacology assays, channel-binding studies, and structureactivity relationship analyses related to QT prolongation.
Side effects and risks
The major risk is dose-dependent QT interval prolongation with potential torsades de pointes and sudden cardiac death, which led to its withdrawal from many clinical markets. Other adverse effects include headache, fatigue and rare hepatic injury. Laboratory use requires strict control of exposure and careful waste management due to its hERG-blocking potency.
Only GMP materials will be supplied, logistics all according to GDP.
Datasheet
| Molecular Formula | C28H31FN4O |
|---|---|
| Molecular Weight | 458.6 g/mol |
| CAS Number | 68844-77-9 |
| Storage Condition | Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), in a well closed container, unless otherwise specified … . Protect from freezing. |
| Solubility | Solubility depends on solvent and conditions (e.g., pH). Please contact us for solvent-specific guidance. |
| Purity | Purity information is available upon request (COA). |
| Synonym | astemizole; 68844-77-9; Hismanal; Paralergin; Histamen |
| IUPAC/Chemical Name | 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine |
| InChl Key | GXDALQBWZGODGZ-UHFFFAOYSA-N |
| InChl Code | InChI=1S/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) |
| References |
3D Conformer.
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