product name Azatadine dimaleate
Description: Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice
References: Agents Actions. 1974 Oct;4(4):264-70; Clin Pharmacokinet. 1991 Nov;21(5):372-93.
522.55
Formula
C20H22N2.2C4H4O4
CAS No.
3978-86-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 105 mg/mL (200.9 mM)
Water: 105 mg/mL (200.9 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
SCH10649
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427775
| In Vitro |
In vitro activity: 95% of Azatadine is biotransformed in Sabouraud dextrose broth within 72 hours treatment with two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a Cmax of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation, demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine (8.8 mg oral) in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. |
| Animal model | |
| Formulation & Dosage | |
| References | Agents Actions. 1974 Oct;4(4):264-70; Clin Pharmacokinet. 1991 Nov;21(5):372-93. |
