3978-86-7
Azatadine dimaleate
CAS: 3978-86-7
Molecular Formula: C28H30N2O8
3978-86-7 - Names and Identifiers
3978-86-7 - Physico-chemical Properties
| Molecular Formula | C28H30N2O8 |
| Molar Mass | 522.5464 |
| Melting Point | 152-154° |
| Solubility | DMSO 105 mg/mL Water 105 mg/mL Ethanol <1 mg/mL |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | Sealed in dry,Room Temperature |
| Use | An antihistaminic. |
| In vitro study | 95% Azatadine bioconverted to two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine, within 72 hours in Sabouraud glucose broth. |
| In vivo study | Azatadine delayed the onset of nebulization histamine, acetylcholine and serotonin induction by Dyspnea in conscious guinea pigs with PD50 of 0.01 mg/kg,0.739 mg/kg and 0.86 mg/kg. Azatadine protects against histamine-induced death by intravenous administration with oral PD50 of 0.009 mg/kg and 0.22 mg/kg in conscious guinea pigs and mice, respectively. In fasted volunteers, 4.2 hours after a single oral dose of Azatadine (4 mg), RIA 4.2 measurements showed a C max of 3 μg/L. Azatadine is almost completely metabolized by hydroxylation, demethylation, and formation of the zwitterion isomer upon opening of the oxidative ring. The Csub>max in healthy volunteers after 8.8 hours of treatment with Azatadine (5.3 mg orally) was 5.9 μg/L with a bioavailability of 80%. Azatadine (1 mg twice daily for 14 days) is effective in reducing symptoms of histamine-mediated seasonal allergic rhinitis. |
3978-86-7 - Risk and Safety
| HS Code | 2933399090 |
3978-86-7 - Introduction
Azatadine dimaleate is an antihistamine and anticholinergic drug with IC50 of 6.5nM and 10nM respectively.
Last Update：2022-10-16 17:41:39
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