Azatadine dimaleate

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

马来酸阿扎他定；Azatadine maleate

白色至淡奶油色粉末

DMSO ：97 mg/mL (185.6 mM)

Water ：96 mg/mL (183.7 mM)

Histamine receptor,Cholinergic

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.

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.

The pharmacology of azatadine, a potential antiallergy drug.
Tozzi S,et al. Agents Actions. 1974 Oct;4(4):264-70. PMID: 4155594.
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